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Budén, María E., Javier I. Bardagí, Marcelo Puiatti, and Roberto A. Rossi. "Initiation in Photoredox C–H Functionalization Reactions. Is Dimsyl Anion a Key Ingredient?" Journal of Organic Chemistry 82, no. 16 (June 6, 2017): 8325–33. http://dx.doi.org/10.1021/acs.joc.7b00822.
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Atencio, Sharmaine, Tom Bernaerts, Danyang Liu, Kai Reineke, Marc Hendrickx, and Ann Van Loey. "Impact of processing on the functionalization of pumpkin pomace as a food texturizing ingredient." Innovative Food Science & Emerging Technologies 69 (May 2021): 102669. http://dx.doi.org/10.1016/j.ifset.2021.102669.
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Kinner, Alina, Philipp Nerke, Regine Siedentop, Till Steinmetz, Thomas Classen, Katrin Rosenthal, Markus Nett, Jörg Pietruszka, and Stephan Lütz. "Recent Advances in Biocatalysis for Drug Synthesis." Biomedicines 10, no. 5 (April 21, 2022): 964. http://dx.doi.org/10.3390/biomedicines10050964.
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Biocatalysis is constantly providing novel options for the synthesis of active pharmaceutical ingredients (APIs). In addition to drug development and manufacturing, biocatalysis also plays a role in drug discovery and can support many active ingredient syntheses at an early stage to build up entire scaffolds in a targeted and preparative manner. Recent progress in recruiting new enzymes by genome mining and screening or adapting their substrate, as well as product scope, by protein engineering has made biocatalysts a competitive tool applied in academic and industrial spheres. This is especially true for the advances in the field of nonribosomal peptide synthesis and enzyme cascades that are expanding the capabilities for the discovery and synthesis of new bioactive compounds via biotransformation. Here we highlight some of the most recent developments to add to the portfolio of biocatalysis with special relevance for the synthesis and late-stage functionalization of APIs, in order to bypass pure chemical processes.
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Lv, Xiaoyu, Kaihong Chen, Guiling Shi, Wenjun Lin, Hongzhen Bai, Haoran Li, Guping Tang, and Congmin Wang. "Design and tuning of ionic liquid–based HNO donor through intramolecular hydrogen bond for efficient inhibition of tumor growth." Science Advances 6, no. 45 (November 2020): eabb7788. http://dx.doi.org/10.1126/sciadv.abb7788.
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Developing ionic liquid (IL) drugs broaden new horizons in pharmaceuticals. The tunable nature endows ILs with capacity to delivery active ingredients. However, the tunability is limited to screen ionic components, and none realizes the kinetic tuning of drug release, which is a key challenge in the design of IL drugs. Here, a series of ILs are developed using biocompatible ionic components, which realizes absorption of gaseous NO to yield IL-NONOates. These IL-NONOates serve as HNO donors to release active ingredient. The release kinetics can be tuned through configuring the geometric construction of ILs (release half-lives, 4.2 to 1061 min). Mechanism research indicates that the tunability depends on the strength of intramolecular hydrogen bond. Furthermore, the IL-based HNO donors exert pharmacological potential to inhibit tumor progression by regulating intratumoral redox state. Coupled with biosafety, these IL-based HNO donors with facile preparation and tunable functionalization can be promising candidates for pharmaceutical application.
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Turaga, Uday, Vinitkumar Singh, Anna Gibson, Shahrima Maharubin, Carol Korzeniewski, Steven Presley, Ernest Smith, Ronald J. Kendall, and Seshadri S. Ramkumar. "Functionalized Antimicrobial Electrospun Poly (vinyl alcohol) Nanowebs." Journal of Engineered Fibers and Fabrics 11, no. 2 (June 2016): 155892501601100. http://dx.doi.org/10.1177/155892501601100208.
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Electrospun poly (vinyl alcohol) [PVA] nanowebs functionalized with a commercially available microbiocidal solution Reputex™ 20 were prepared. The active ingredient of Reputex™ 20 is polyhexamethylene biguanides, a safe antiseptic. Fourier Transform Infrared spectroscopy confirmed the functionalization of PVA nanowebs. Functionalized nanowebs were characterized by evaluating their antimicrobial properties, breathability characteristics and tensile properties. Functionalized nanowebs demonstrated significant antimicrobial activity against both Gram positive and Gram negative bacteria. Nanowebs developed from biocompatible polymers like PVA, and functionalized with safe antiseptics, could find many biomedical applications such as wound bandages.
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De Bruno, Alessandra, Rosa Romeo, Antonio Gattuso, Amalia Piscopo, and Marco Poiana. "Functionalization of a Vegan Mayonnaise with High Value Ingredient Derived from the Agro-Industrial Sector." Foods 10, no. 11 (November 3, 2021): 2684. http://dx.doi.org/10.3390/foods10112684.
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This work aimed to evaluate the antioxidant effect determined by the addition of phenolic extract on the oxidative stability and quality of vegan mayonnaise. Two different antioxidant extracts containing 100 mg L−1 of hydroxytyrosol and obtained by olive mill wastewater were used in the preparation. After preliminary studies, already evaluated in other works, on hydrophilic and lipophilic food matrices, the results of this study could contribute to understanding the effects of the enrichment on emulsified food systems with phenolic extracts. The functionalized mayonnaise samples were monitored up to 45 days of storage at 10 °C in comparison with a control sample for microbiological, physicochemical, antioxidant, sensory properties and for oxidative stability. The results achieved through this work showed the efficacy of the use of phenolic extract as ingredients for its positive effect on chemical properties of mayonnaise. The adding extracts lead to the increase of oxidative stability with an induction period higher (about 24 h) than the control sample (about 12 h).
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Campeau, Louis-Charles, and Tomislav Rovis. "Preface: Modern Heterocycle Synthesis and Functionalization." Synlett 32, no. 02 (January 2021): 140–41. http://dx.doi.org/10.1055/s-0040-1706679.
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obtained his PhD degree in 2008 with the late Professor Keith Fagnou at the University of Ottawa in Canada as an NSERC Doctoral Fellow. He then joined Merck Research Laboratories at Merck-Frosst in Montreal in 2007, making key contributions to the discovery of Doravirine (MK-1439) for which he received a Merck Special Achievement Award. In 2010, he moved from Quebec to New Jersey, where he has served in roles of increasing responsibility with Merck ever since. L.-C. is currently Executive Director and the Head of Process Chemistry and Discovery Process Chemistry organizations, leading a team of smart creative scientists developing innovative chemistry solutions in support of all discovery, pre-clinical and clinical active pharmaceutical ingredient deliveries for the entire Merck portfolio for small-molecule therapeutics. Over his tenure at Merck, L.-C. and his team have made important contributions to >40 clinical candidates and 4 commercial products to date. Tom Rovis was born in Zagreb in former Yugoslavia but was largely raised in southern Ontario, Canada. He earned his PhD degree at the University of Toronto (Canada) in 1998 under the direction of Professor Mark Lautens. From 1998–2000, he was an NSERC Postdoctoral Fellow at Harvard University (USA) with Professor David A. Evans. In 2000, he began his independent career at Colorado State University and was promoted in 2005 to Associate Professor and in 2008 to Professor. His group’s accomplishments have been recognized by a number of awards including an Arthur C. Cope Scholar, an NSF CAREER Award, a Fellow of the American Association for the Advancement of Science and a Katritzky Young Investigator in Heterocyclic Chemistry. In 2016, he moved to Columbia University where he is currently the Samuel Latham Mitchill Professor of Chemistry.
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Wu, Lei, Weifeng Wang, Rong Liu, Gang Wu, and Huaxin Chen. "Impact of the functionalization onto structure transformation and gas adsorption of MIL-68(In)." Royal Society Open Science 5, no. 12 (December 2018): 181378. http://dx.doi.org/10.1098/rsos.181378.
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A series of functionalization –NH 2 , –Br and –NO 2 has been performed on MIL-68(In) material in order to improve the porosity features of the pristine material. The functional groups grafted onto the ligand and the molar ratios of the ingredient indicate a profound influence on product formation. With the incremental amount of metal source, product structures undergo the transformation from MIL-68 to MIL-53 or QMOF-2. The situation is different depending on the variation of the ligands. Gas (N 2 , Ar, H 2 and CO 2 ) adsorption–desorption isotherms were systematically investigated to explore the impact of the functionalization on the porous prototypical framework. Comparison of adsorption behaviour of N 2 and Ar indicates that the polar molecule exhibits striking interaction to N 2 molecule, which has a considerable quadrupole moment. Therefore, as a probe molecule, Ar with no quadrupole moment is more suitable to characterize the surface area with the polar groups. Meanwhile, Ar adsorption result confirms that the negative influence on the surface area stems from the size of the substituting groups. The uptake of H 2 and CO 2 indicates that the introduction of appropriate polar organic groups can effectively enhance the adsorption enthalpy of relative gases and improve the gas adsorption capacity apparently at low pressure. The introduction of –NO 2 is in favour of improving the H 2 adsorption capacity, while the grafted –NH 2 groups can most effectively enhance the CO 2 adsorption capacity.
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Zanardi, Franca, Claudio Curti, Andrea Sartori, and Lucia Battistini. "Exploring the Remote Reactivity of π-Extended Carbonyl Compounds: The Vinylogous Alkylidene Malononitrile Activation Strategy." Synlett 29, no. 03 (November 15, 2017): 266–81. http://dx.doi.org/10.1055/s-0036-1589125.
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The installation of malononitrile into π-extended carbonyl compounds gives rise to vinylogous alkylidene malononitriles (also known as π-extended dicyanovinylidenes), the direct functionalization of which at remote C(sp3) pronucleophilic sites becomes possible and viable. Starting from easily accessible representative polyunsaturated malononitriles, mild conditions were found to directly couple them to complementary enal acceptors. In all cases, the malononitrile handle proved an indispensable (and optionally traceless) activating ingredient for the vinylogous reactions to proceed efficiently and selectively. Merging the vinylogy concept with the malononitrile HOMO-raising activation strategy and complementary organocatalytic activation modalities (i.e. LUMO-lowering iminium ion activation) turned out to be a successful option, as demonstrated by the number of diverse carbocyclic and heterocyclic chiral products that were (stereo)selectively accessed through this chemistry.1 Introduction2 Reactions of Cyclohexenylidene Malononitriles with Enals3 Reactions of Allylidene Malononitriles with Enals4 Reactions of Indolylmethylene Malononitriles with Enals5 Conclusion
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Battistin, Mattia, Elisa Durini, Valeria Dissette, Alessandro Bonetto, Antonio Marcomini, Elisa Casagrande, Andrea Brunetta, et al. "Synthesis and Characterization of New Multifunctional Self-Boosted Filters for UV Protection: ZnO Complex with Dihydroxyphenyl Benzimidazole Carboxylic Acid." Molecules 24, no. 24 (December 12, 2019): 4546. http://dx.doi.org/10.3390/molecules24244546.
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The incidence of skin cancer is increasing both because of climate change and the increase in pollution than people’s incorrect habits of sun exposure. In these regards, sunscreen and photoprotection are essential tools in consenting the benefits induced by safe solar light exposition and skin cancer prevention. In this work, a new class of sunscreen filter was synthesized by chemical combination of a physical filter (ZnO) and Oxisol (dihydroxyphenyl benzimidazole carboxylic acid), an antioxidant molecule with booster effect. In this work, a new class of filters with new properties was achieved by direct functionalization of particles surface. A full characterization of this multifunctional ingredient (ZnO–Ox) was conducted: Compared with the simple mixture, the new filter acts as a multifunctional molecule showing a higher Sun Protection Factor (SPF), a better cytotoxic profile (MTT and NRU assay), and anti-acne activity. A strong reduction of photocatalytic activity of ZnO was observed, also improving the safety profile.
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ALBERT, HELEN MERINA, and Alosious Gonsago C. "GREEN SYNTHESIS OF ZINC OXIDE NANOPARTICLES USING SOLANUM NIGRUM LEAF EXTRACT AND OVERVIEW OF THEIR ANTIBACTERIAL ACTIVITIES." Journal of Advanced Scientific Research 14, no. 05 (May 31, 2023): 26–30. http://dx.doi.org/10.55218/jasr.202314505.
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In the current study, we have detailed the green synthesis of ZnO nanoparticles (Zn-NPs) employing the capping ingredient Solanum Nigrum. With the use of X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy, UV-Vis absorption, and antibacterial investigations, the functionalization of ZnO particles through Solanum Nigrum leaves extract induced bio-reduction of ZnO was examined. According to XRD analysis, the produced NPs have a wurtzite hexagonal structure and an average grain size of 27.6 nm. The functional groups are further shown by FT-IR spectra. The indirect band gap is estimated to be 3.38 eV based on UV-Vis DRS studies. It has been proven that the particle size variations and surface area-to-volume ratios of ZnO-NPs are responsible for significantly higher antibacterial activities. According to the antibacterial study, the ZnO-NPs inhibit the growth of both normal as well as pathogenic bacterium and hence might be used for coating surgical equipment for performing aseptic operators in the medical field.
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Chauhan, Vanvirsinh, Jayashree Bijwe, and Ashish Darpe. "Functionalization of alumina particles to improve the performance of eco-friendly brake-pads." Friction 9, no. 5 (February 3, 2021): 1213–26. http://dx.doi.org/10.1007/s40544-020-0461-5.
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AbstractAbrasives, such as oxides of alumina (Al), silica (Si), zirconia (Zr), chromium (Cr) etc., are added to raise the friction level and also to remove the glaze on the disc so that surface will be rejuvenated continuously during braking and will contribute to maintain the desired friction level. However, these inorganic particles have less adhesion with the resin/binder and hence are easily dug out during wearing process contributing to higher wear. If efforts are made to enhance the filler-matrix adhesion, not only the wear of friction material (FM) should reduce, the particles may stay for a longer time on the tribo-surface of the pads to contribute fully towards controlling the coefficient of friction (μ). In the present study, alumina particles were selected for siloxane treatment to improve the filler-matrix adhesion. Two types of eco-friendly (free from asbestos and Cu) brake-pads were developed using alumina as a theme ingredient (treated and untreated) keeping all the parent formulation identical. An additional type of brake-pads without alumina particles was also developed to observe the effect of abrasive particles on the tribo-performance. The performance properties (physical, mechanical, and tribological) of brake-pads were compared when evaluated in identical conditions. The tribo-testing was done on full-scale brake inertia dynamometer following the procedure in Japanese automobile standard (JASO C 406). It was observed that siloxane treatment affected both friction and wear of brake-pads in a beneficial way. Wear resistance got increased 35% for siloxane treated pads. Worn surfaces were analysed using scanning electron microscopy (SEM) and energy dispersive X-ray (EDAX) technique.
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Rhyaf, Atiaf, Hala Naji, Hassan Al-Karagoly, Salim Albukhaty, Ghassan M. Sulaiman, Abdulaziz Arif A. Alshammari, Hamdoon A. Mohammed, Majid Jabir, and Riaz A. Khan. "In Vitro and In Vivo Functional Viability, and Biocompatibility Evaluation of Bovine Serum Albumin-Ingrained Microemulsion: A Model Based on Sesame Oil as the Payload for Developing an Efficient Drug Delivery Platform." Pharmaceuticals 16, no. 4 (April 12, 2023): 582. http://dx.doi.org/10.3390/ph16040582.
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Combination of bovine serum albumin with microemulsions as constituting ingredient biopolymer has long been regarded an innovative method to address the surface functionalization and stability issues in the targeted payload deliveries, thereupon producing effectively modified microemulsions, which are superior in loading capacity, transitional and shelf-stability, as well as site-directed/site-preferred delivery, has become a favored option. The current study aimed to develop an efficient, suitable and functional microemulsion system encapsulating sesame oil (SO) as a model payload towards developing an efficient delivery platform. UV-VIS, FT-IR, and FE-SEM were used to characterize, and analyze the developed carrier. Physicochemical properties assessments of the microemulsion by dynamic light scattering size distributions, zeta-potential, and electron micrographic analyses were performed. The mechanical properties for rheological behavior were also studied. The HFF-2 cell line and hemolysis assays were conducted to ascertain the cell viability, and in vitro biocompatibility. The in vivo toxicity was determined based on a predicted median lethal dose (LD50) model, wherein the liver enzymes’ functions were also tested to assess and confirm the predicted toxicity.
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Conceição, Natália, Bianca R. Albuquerque, Carla Pereira, Rúbia C. G. Corrêa, Camila B. Lopes, Ricardo C. Calhelha, Maria José Alves, Lillian Barros, and Isabel C. F. R. Ferreira. "By-Products of Camu-Camu [Myrciaria dubia (Kunth) McVaugh] as Promising Sources of Bioactive High Added-Value Food Ingredients: Functionalization of Yogurts." Molecules 25, no. 1 (December 24, 2019): 70. http://dx.doi.org/10.3390/molecules25010070.
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Camu-camu (Myrciaria dubia (Kunth) McVaugh) is a fruit economically relevant to the Amazon region, mostly consumed in the form of processed pulp. Our aim was to perform an unprecedented comparative study on the chemical composition and bioactivities of the camu-camu pulp and industrial bio-residues (peel and seed), and then the most promising fruit part was further explored as a functionalized ingredient in yogurt. A total of twenty-three phenolic compounds were identified, with myricetin-O-pentoside and cyanindin-3-O-glucoside being the main compounds in peels, followed by p-coumaroyl hexoside in the pulp, and ellagic acid in the seeds. The peel displayed the richest phenolic profile among samples, as well as the most significant antibacterial (MICs = 0.625–10 mg/mL) and anti-proliferative (GI50 = 180 µg/mL against HeLa cells) activities. For this reason, it was selected to be introduced in a food system (yogurt). Taken together, our results suggest the possibility of using the camu-camu peel as a source of food additives.
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Wahyuni, N. I., A. T. Sanna, Pirman, M. Yusuf, and J. Langkong. "Effect of functionalization of raw materials on the quality of instant chocolate drink with sensory, physicochemical and anti-diabetic parameters." IOP Conference Series: Earth and Environmental Science 1230, no. 1 (September 1, 2023): 012159. http://dx.doi.org/10.1088/1755-1315/1230/1/012159.
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Abstract The cocoa bean is a component of the cocoa pod, which is frequently used as an ingredient in foods and drinks. Numerous healthy substances, such as polyphenols, which act as antioxidants, antiaging, anti-inflammatory, antidiabetic, and antihypertensive agents, are found in cocoa beans. The goal of this study is to create a useful instant beverage that acts as an antidiabetic. This study involved the creation of a combined instant chocolate powder and cocoa liquid. According to the findings, the Forastero variety processed cocoa powder had the highest total polyphenol content, namely 425.179 pm 0.01 mg GAE/g and the lowest polyphenol content was owned by Kalla cocoa, namely 172.768 pm 2.93 mg GAE/g. The formulation’s overall polyphenol content ranged from 3.125 pm 1.89 to 150.446 pm 17.04 mg GAE/g. The highest inhibition percentage with the lowest IC50 value was found in the formulation A31 sample and the lowest inhibition percentage with the highest IC50 value was in the formulation B32 sample. The higher the value of the total polyphenol content of the cocoa powder sample, the higher the percentage of inhibition of alpha-amylase activity. The physicochemical analysis is carried out by measuring the color. The color change in cocoa powder is due to changes in the structure of the cocoa anthocyanin-type polyphenols during the fermentation, drying and roasting processes. The sensory analysis of the ranking method showed the best formulations of B23 and B33, according to the panelists.
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Zheng, Xiaoxiao, Rongli Zhai, Zihao Zhang, Baoqing Zhang, Jiangwei Liu, Aamir Razaq, Muhammad Ashfaq Ahmad, et al. "Graphene-Oxide-Based Fluoro- and Chromo-Genic Materials and Their Applications." Molecules 27, no. 6 (March 21, 2022): 2018. http://dx.doi.org/10.3390/molecules27062018.
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Composite materials and their applications constitute a hot field of research nowadays due to the fact that they comprise a combination of the unique properties of each component of which they consist. Very often, they exhibit better performance and properties compared to their combined building blocks. Graphene oxide (GO), as the most widely used derivative of graphene, has attracted widespread attention because of its excellent properties. Abundant oxygen-containing functional groups on GO can provide various reactive sites for chemical modification or functionalization of GO, which in turn can be used to develop novel GO-based composites. This review outlines the most recent advances in the field of novel dyes and pigments encompassing GO as a key ingredient or as an important cofactor. The interactions of graphene with other materials/compounds are highlighted. The special structure and unique properties of GO have a great effect on the performance of fabricated hybrid dyes and pigments by enhancing the color performance of dyes, the anticorrosion properties of pigments, the viscosity and rheology of inks, etc., which further expands the applications of dyes and pigments in dyeing, optical elements, solar-thermal energy storage, sensing, coatings, and microelectronics devices. Finally, challenges in the current development as well as the future prospects of GO-based dyes and pigments are also discussed. This review provides a reference for the further exploration of novel dyes and pigments.
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Jiménez-Moreno, Cimminelli, Volpe, Ansó, Esparza, Mármol, Rodríguez-Yoldi, and Ancín-Azpilicueta. "Phenolic Composition of Artichoke Waste and its Antioxidant Capacity on Differentiated Caco-2 Cells." Nutrients 11, no. 8 (July 25, 2019): 1723. http://dx.doi.org/10.3390/nu11081723.
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Artichoke waste represents a huge amount of discarded material. This study presents the by-products (bracts, exterior leaves, and stalks) of the “Blanca de Tudela” artichoke variety as a potential source of phenolic compounds with promising antioxidant properties. Artichoke residues were subjected to different extraction processes, and the antioxidant capacity and phenolic composition of the extracts were analyzed by spectrophotometric methods and high performance liquid chromatography (HPLC) analyses, respectively. The most abundant polyphenols in artichoke waste were chlorogenic acid, luteolin-7-O-rutinoside, and luteolin-7-O-glucoside. Minor quantities of cynarin, luteolin, apigenin-7-O-glucoside, apigenin-7-O-rutinoside, and naringenin-7-O-glucoside were also found. The antioxidant activity of the obtained extracts determined by ABTS [2, 2’-azinobis (3-ethylbenzothiazoline-6-sulphonic acid)], DPPH (2,2-diphenyl-1-pycrilhydracyl), and FRAP (Ferric Ion Reducing Antioxidant Power) was highly correlated with the total concentration of phenolic compounds. Chlorogenic acid, luteolin-7-O-glucoside, and luteolin-7-O-rutinoside, the most abundant compounds in 60% methanol extracts, are the components most responsible for the antioxidant activity of the artichoke waste extracts. The extract with the best antioxidant capacity was selected to assay its antioxidant potential on a model intestinal barrier. This action of the hydroxycinnamic acids on intestinal cells (Caco-2) was confirmed. In summary, artichoke waste may be considered a very interesting ingredient for food functionalization and for therapeutic purposes.
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Das, Ram P., Vishwa V. Gandhi, Beena G. Singh, and Amit Kunwar. "Passive and Active Drug Targeting: Role of Nanocarriers in Rational Design of Anticancer Formulations." Current Pharmaceutical Design 25, no. 28 (October 21, 2019): 3034–56. http://dx.doi.org/10.2174/1381612825666190830155319.
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Background: Cancer is the major public health problem in developing countries. The treatment of cancer requires a multimodal approach and chemotherapy is one of them. Chemotherapeutic drug is administered to cancer patients in the form of a formulation which is prepared by mixing an active ingredient (drug) with the excipient. The role of excipient in a formulation is to regulate the release, bio-distribution, and selectivity of drug within the body. Methods: In this context, selectivity of an anticancer formulation is achieved through two mechanisms like passive and active targeting. The passive targeting of a formulation is generally through enhanced permeation retention (EPR) effect which is dictated by physical properties of the carrier such as shape and size. On the contrary, active targeting means surface functionalization of excipient with target-specific ligands and/or receptors to increase its selectivity. Results: Over the past several decades, remarkable progress has been made in the development and application of an engineered excipient or carrier to treat cancer more effectively. Especially nanoparticulate systems composed of metal/liposomes/polymeric material/proteins have received significant attention in the rational design of anticancer drug formulations; for example, therapeutic agents have been integrated with nanoparticles of optimal sizes, shapes and surface properties to improve their solubility, circulation half-life, and bio-distribution. In this review article, recent literature is included to discuss the role of physicochemical properties of excipients in achieving tumour targeting through passive and active approaches. Conclusion: The selection of an excipient/carrier and targeting ligand plays a very important role in rational design and development of anticancer drug formulations.
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Han, Jinju, Lei Liu, Zhanhua Fan, Zhaolun Zhang, Shuyan Yang, and Ying Tang. "Grafting Cosmetic Active Ingredients for the Functionalization of Cosmetotextiles." IOP Conference Series: Materials Science and Engineering 782 (April 15, 2020): 022026. http://dx.doi.org/10.1088/1757-899x/782/2/022026.
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Souza, Iane M. S., Fátima García-Villén, César Viseras, and Sibele B. C. Perger. "Zeolites as Ingredients of Medicinal Products." Pharmaceutics 15, no. 5 (April 28, 2023): 1352. http://dx.doi.org/10.3390/pharmaceutics15051352.
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Development of new medicinal products for particular therapeutic treatment or for better manipulations with better quality and less side effects are possible as a result of advanced inorganic and organic materials application, among which zeolites, due to their properties and versatility, have been gaining attention. This paper is an overview of the development in the use of zeolite materials and their composites and modifications as medicinal products for several purposes such as active agents, carriers, for topical treatments, oral formulations, anticancer, the composition of theragnostic systems, vaccines, parenteral dosage forms, tissue engineering, etc. The objective of this review is to explore the main properties of zeolites and associate them with their drug interaction, mainly addressing the advances and studies related to the use of zeolites for different types of treatments due to their zeolite characteristics such as molecule storage capacity, physical and chemical stability, cation exchange capacity, and possibility of functionalization. The use of computational tools to predict the drug—zeolite interaction is also explored. As conclusion was possible to realize the possibilities and versatility of zeolite applications as being able to act in several aspects of medicinal products.
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Zare, Mina, Karolina Dziemidowicz, Gareth R. Williams, and Seeram Ramakrishna. "Encapsulation of Pharmaceutical and Nutraceutical Active Ingredients Using Electrospinning Processes." Nanomaterials 11, no. 8 (July 30, 2021): 1968. http://dx.doi.org/10.3390/nano11081968.
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Electrospinning is an inexpensive and powerful method that employs a polymer solution and strong electric field to produce nanofibers. These can be applied in diverse biological and medical applications. Due to their large surface area, controllable surface functionalization and properties, and typically high biocompatibility electrospun nanofibers are recognized as promising materials for the manufacturing of drug delivery systems. Electrospinning offers the potential to formulate poorly soluble drugs as amorphous solid dispersions to improve solubility, bioavailability and targeting of drug release. It is also a successful strategy for the encapsulation of nutraceuticals. This review aims to briefly discuss the concept of electrospinning and recent progress in manufacturing electrospun drug delivery systems. It will further consider in detail the encapsulation of nutraceuticals, particularly probiotics.
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Wagschal, Simon, and Diego Broggini. "Academia / Industry Collaborations towards the Functionalization of Aryl Azoles." CHIMIA 78, no. 3 (March 27, 2024): 104–7. http://dx.doi.org/10.2533/chimia.2024.104.
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Aryl azoles can be found in numerous active pharmaceutical ingredients (APIs). Milvexian is a Factor Xia inhibitor currently in phase III for the treatment of thrombotic events containing an ortho-substituted 1-aryl-1H-1,2,3-triazole moiety. During the process development of Milvexian, we assessed multiple approaches for the preparation of 4-chloro-1,2,3-triazole, intermediate 1. In this review article, we will detail how we initiated several academic collaborations to speed up the selection of the best synthesis for commercial manufacturing. Ultimately, those results not only helped us to achieve our goal but yielded general methodologies for the functionalization of azoles that extended even beyond our initial scope.
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Sbehat, Maram, Gianluigi Mauriello, and Mohammad Altamimi. "Microencapsulation of Probiotics for Food Functionalization: An Update on Literature Reviews." Microorganisms 10, no. 10 (September 30, 2022): 1948. http://dx.doi.org/10.3390/microorganisms10101948.
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Functional foods comprise the largest growing food category due to both consumer demands and health claims by manufacturers. Probiotics are considered one of the best choices for meeting these demands. Traditionally, the food vehicle for introducing probiotics to consumers was dairy products, and to expand the benefits of probiotics for a wider range of consumers, the need to use other food items was essential. To achieve this goal while maximising the benefits of probiotics, protection methods used during food processing were tackled. The microencapsulation of probiotics is a promising methodology for achieving this function. This review highlights the use of the microencapsulation of probiotics in order to functionalise food items that initially were not considered suitable for probiotication, such as baked products, or to increase their functionality such as dairy products. The co-microencapsulation of probiotics with other functional ingredients such polyphenol, prebiotics, or omega-3 is also highlighted.
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Goscianska, Joanna, Aleksander Ejsmont, Anita Kubiak, Dominika Ludowicz, Anna Stasiłowicz, and Judyta Cielecka-Piontek. "Amine-Grafted Mesoporous Carbons as Benzocaine-Delivery Platforms." Materials 14, no. 9 (April 24, 2021): 2188. http://dx.doi.org/10.3390/ma14092188.
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Smart porous carriers with defined structure and physicochemical properties are required for releasing the therapeutic drug with precise control of delivery time and location in the body. Due to their non-toxicity, ordered structure, and chemical and thermal stability, mesoporous carbons can be considered modern carriers for active pharmaceutical ingredients whose effectiveness needs frequent dosing algorithms. Here, the novel benzocaine delivery systems based on ordered mesoporous carbons of the cubic structure were obtained with the use of a hard template method and functionalization with amine groups at 40 °C for 8 h. It has been shown that amine grafting strongly modifies the surface chemistry and textural parameters of carbons. All samples indicated good sorption ability towards benzocaine, with evident improvement following the functionalization with the amine groups. The sorption capacity and drug release kinetics were strongly affected by the porosity of carbon carriers and the surface functional groups. The smallest amount of benzocaine (~12%) was released from pristine mesoporous carbon, which could be correlated with strong API–carrier interactions. Faster and more efficient release of the drug was observed in the case of triethylenetetramine modified carbon (~62%). All benzocaine delivery platforms based on amine-grafted mesoporous carbons revealed high permeability through the artificial membrane.
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González-Reza, Ricardo, Claudia García-Betanzos, Liliana Sánchez-Valdes, David Quintanar-Guerrero, María Cornejo-Villegas, and María Zambrano-Zaragoza. "The Functionalization of Nanostructures and Their Potential Applications in Edible Coatings." Coatings 8, no. 5 (April 26, 2018): 160. http://dx.doi.org/10.3390/coatings8050160.
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Nowadays, edible coatings incorporated with nanostructures as systems of controlled release of flavors, colorants and/or antioxidants and antimicrobial substances, also used for thermal and environmental protection of active compounds, represent a gap of opportunity to increase the shelf life of food highly perishable, as well as for the development of new products. These functionalized nanostructures have the benefit of incorporating natural substances obtained from the food industry that are rich in polyphenols, dietary fibers, and antimicrobial substances. In addition, the polymers employed on its preparation, such as polysaccharides, solid lipids and proteins that are low cost and developed through sustainable processes, are friendly to the environment. The objective of this review is to present the materials commonly used in the preparation of nanostructures, the main ingredients with which they can be functionalized and used in the preparation of edible coatings, as well as the advances that these structures have represented when used as controlled release systems, increasing the shelf life and promoting the development of new products that meet the characteristics of functionality for fresh foods ready to eat.
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Kleemann, Kevin, and Michael Sander. "Water-soluble and Water-dispersible Polymers Used in Commercial Agricultural Formulations: Inventory of Polymers and Perspective on their Environmental Fate." CHIMIA 77, no. 11 (November 29, 2023): 764–72. http://dx.doi.org/10.2533/chimia.2023.764.
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Agricultural formulations contain water-soluble and water-dispersible polymers (WSPs and WDPs) to increase the application efficiency of the active ingredients (e.g. pesticides and fertilizers). Despite their direct release to soils and crops, there is currently no inventory of used polymers and their fate in soils is poorly studied and understood. Herein, we identify WSPs and WDPs used in agricultural formulations on the German and Swiss markets. By searching the scientific literature, patents, and manufacturer websites, we tentatively identified that 233 of the 1815 listed trade names of formulation additives contained polymers, the majority of which belonged to three main chemical classes: polyethylene glycol (PEG)-based (co)polymers, functionalized polysaccharides (PSacs), and vinylic (co)polymers (VCPs). We report information on their functionalization, molecular weights, and market significance. In 2015, their estimated combined annual application volume in Switzerland surpassed 100 tonnes. Low molecular weight PEGs and natural, unfunctionalized PSacs reportedly biodegrade, suggesting no accumulation in soils associated with their use as formulation additives. Conversely, high molecular weight functionalized PEGs, functionalized PSacs, and the majority of the VCPs have been reported to undergo only slow or no soil biodegradation. These polymers may thus persist and accumulate in agricultural soils, requiring more detailed investigations of their environmental fate and resulting exposure scenarios. There is a need for systematic studies on the effects of polymer structure, molecular weight, and functionalization on soil biodegradability.
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Albergamo, Ambrogina, Rossella Vadalà, Daniela Metro, Vincenzo Nava, Giovanni Bartolomeo, Rossana Rando, Antonio Macrì, et al. "Physicochemical, Nutritional, Microbiological, and Sensory Qualities of Chicken Burgers Reformulated with Mediterranean Plant Ingredients and Health-Promoting Compounds." Foods 10, no. 9 (September 9, 2021): 2129. http://dx.doi.org/10.3390/foods10092129.
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The quality of chicken burgers reformulated by the partial replacement of meat by Mediterranean plant ingredients and enriched with peculiar amounts of n-3 PUFAs, Mg, Fe, Se, and folic acid, was evaluated in comparison to conventional chicken burgers. Specifically, two types of burger were developed, namely the “Sicilian burger”—based on cherry tomato and rosemary—and the “Mediterranean burger”—with basil leaves and thyme essential oil—every recipe being differentially functionalized according to the nutritional requirements of consumers, such as children, pregnant women and elderly. Mediterranean ingredients were responsible for different pH, color, and cooking loss between conventional and functional burgers. Except for n-3 PUFAs resulting poorly fortified, the functionalization with Mg, Fe, Se, and vitamin B9 was successful in all products. Considering the target consumer categories, the daily consumption of the functional burger may assure an intake of Mg, Fe, and Se equal, respectively, to 37.31–59.90%, 17.76–46.81%, and 27.20–50.05%, and a cover of vitamin B9 of 31.98–48.31% of the relative population reference intakes. Fortified products kept a good microbiological quality during 5 days of refrigerated storage, and, according to the sensorial descriptive analysis and the hedonic test, they showed a higher acceptability than conventional burgers.
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Basnet, Sunita, Masaya Otsuka, Chizuru Sasaki, Chikako Asada, and Yoshitoshi Nakamura. "Functionalization of the active ingredients of Japanese green tea (Camellia sinensis) for the synthesis of bio-based epoxy resin." Industrial Crops and Products 73 (October 2015): 63–72. http://dx.doi.org/10.1016/j.indcrop.2015.03.091.
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Sugiarti, Sri, Charlena Charlena, and Nurul Afiati Aflakhah. "Zeolit Sintetis Terfungsionalisasi 3-(Trimetoksisilil)-1-Propantiol sebagai Adsorben Kation Cu(II) dan Biru Metilena." Jurnal Kimia VALENSI 3, no. 1 (May 31, 2017): 11–19. http://dx.doi.org/10.15408/jkv.v3i1.5144.
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The more commonly used method for making synthetic zeolite from kaolin is hydrothermal method. This research tested a sol-gel method in processing synthetic zeolit using kaolin as the basic ingrediant. The synthetic zeolite derived from the sol-gel method was then characterized using X-ray Difractometer and Scanning Electron Microscope, which found resulting products zeolite-A, zeolite Y and sodalite. The adsorption ability of the synthetic zeolites was tested using Cu(II) and methylene blue. Functionalization of the synthetic zeolites by 3-(trimetoksisilil)-1-propantiol was done to increase adsorption capacity. Zeolite A modified by 3-(trimetoksisilil)-1-propantiol had the greater capacity to adsorb methylene blue at 30.11 mg/g. The adsorption isotherms of all the synthetic zeolites approached the Langmuir form. The adsorption energy off all synthetic zeolites approached the chemical adsorption.DOI: http://dx.doi.org/10.15408/jkv.v0i0.5144
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Battistin, Mattia, Valeria Dissette, Alessandro Bonetto, Elisa Durini, Stefano Manfredini, Antonio Marcomini, Elisa Casagrande, et al. "A New Approach to UV Protection by Direct Surface Functionalization of TiO2 with the Antioxidant Polyphenol Dihydroxyphenyl Benzimidazole Carboxylic Acid." Nanomaterials 10, no. 2 (January 28, 2020): 231. http://dx.doi.org/10.3390/nano10020231.
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Skin cancer is the most common malignant cancer with an incidence of 1 million cases/year. It is well known that exposure to UV radiation from sunlight leads the most frequent risk factors for several skin disorders including skin cancer. Sunscreen filters represent a valid protection against dangerous effects derived from UV radiation, and they can be divided in organic and inorganic UV filters. Adding, at the product formulation, molecules with booster effect, or also substances that can increase the protecting effectiveness via synergic mechanisms, can further enhance their protection activity. Moreover, this approach leads to develop formulations with high SPF (Sun Protection Factor) with a reduced content of UV filters, this is in line with the recent decisions of yet a few countries (Palau, Thailand, Philippines, and Hawaii) to ban some sunscreen filters to preserve marine environments (i.e., reef). In this work, a new class of sunscreen UV filters has been synthesized, by means the combination of physical filter and Oxisol, an antioxidant molecule with booster effect. In this study, the synthesis of new physical multifunctional ingredients is reported, by means the direct surface functionalization of inorganic filters (in particular TiO2) with Oxisol. In this study, the full characterization of these multifunctional ingredients is also reported, in addition to the cytotoxicity tests, the photocatalytic activity and the rheological properties involved on skin application.
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Schmid, Vera, Antje Trabert, Judith (Schäfer) Keller, Mirko Bunzel, Heike P. Karbstein, and M. Azad Emin. "Functionalization of Enzymatically Treated Apple Pomace from Juice Production by Extrusion Processing." Foods 10, no. 3 (February 24, 2021): 485. http://dx.doi.org/10.3390/foods10030485.
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Food by-products can be used as natural and sustainable food ingredients. However, a modification is needed to improve the technofunctional properties according to the specific needs of designated applications. A lab-scale twin-screw extruder was used to process enzymatically treated apple pomace from commercial fruit juice production. To vary the range of the thermomechanical treatment, various screw speeds (200, 600, 1000 min−1), and screw configurations were applied to the raw material. Detailed chemical and functional analyses were performed to develop a comprehensive understanding of the impact of the extrusion processing on apple pomace composition and technofunctional properties as well as structures of individual polymers. Extrusion at moderate thermomechanical conditions increased the water absorption, swelling, and viscosity of the material. An increase in thermomechanical stress resulted in a higher water solubility index, but negatively affected the water absorption index, viscosity, and swelling. Scanning electron microscopy showed an extrusion-processing-related disruption of the cell wall. Dietary fiber analysis revealed an increase of soluble dietary fiber from 12.6 to 17.2 g/100 g dry matter at maximum thermo-mechanical treatment. Dietary fiber polysaccharide analysis demonstrated compositional changes, mainly in the insoluble dietary fiber fraction. In short, pectin polysaccharides seem to be susceptible to thermo-mechanical stress, especially arabinans as neutral side chains of rhamnogalacturonan I.
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Punz, Benjamin, Litty Johnson, Mark Geppert, Hieu-Hoa Dang, Jutta Horejs-Hoeck, Albert Duschl, and Martin Himly. "Surface Functionalization of Silica Nanoparticles: Strategies to Optimize the Immune-Activating Profile of Carrier Platforms." Pharmaceutics 14, no. 5 (May 21, 2022): 1103. http://dx.doi.org/10.3390/pharmaceutics14051103.
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Silica nanoparticles (SiNPs) are generally regarded as safe and may represent an attractive carrier platform for nanomedical applications when loaded with biopharmaceuticals. Surface functionalization by different chemistries may help to optimize protein loading and may further impact uptake into the targeted tissues or cells, however, it may also alter the immunologic profile of the carrier system. In order to circumvent side effects, novel carrier candidates need to be tested thoroughly, early in their development stage within the pharmaceutical innovation pipeline, for their potential to activate or modify the immune response. Previous studies have identified surface functionalization by different chemistries as providing a plethora of modifications for optimizing efficacy of biopharmaceutical (nano)carrier platforms while maintaining an acceptable safety profile. In this study, we synthesized SiNPs and chemically functionalized them to obtain different surface characteristics to allow their application as a carrier system for allergen-specific immunotherapy. In the present study, crude natural allergen extracts are used in combination with alum instead of well-defined active pharmaceutical ingredients (APIs), such as recombinant allergen, loaded onto (nano)carrier systems with immunologically inert and stable properties in suspension. This study was motivated by the hypothesis that comparing different charge states could allow tailoring of the binding capacity of the particulate carrier system, and hence the optimization of biopharmaceutical uptake while maintaining an acceptable safety profile, which was investigated by determining the maturation of human antigen-presenting cells (APCs). The functionalized nanoparticles were characterized for primary and hydrodynamic size, polydispersity index, zeta potential, endotoxin contamination. As potential candidates for allergen-specific immunotherapy, the differently functionalized SiNPs were non-covalently coupled with a highly purified, endotoxin-free recombinant preparation of the major birch pollen allergen Bet v 1 that functioned for further immunological testing. Binding efficiencies of allergen to SiNPs was controlled to determine uptake of API. For efficacy and safety assessment, we employed human monocyte-derived dendritic cells as model for APCs to detect possible differences in the particles’ APC maturation potential. Functionalization of SiNP did not affect the viability of APCs, however, the amount of API physisorbed onto the nanocarrier system, which induced enhanced uptake, mainly by macropinocytosis. We found slight differences in the maturation state of APCs for the differently functionalized SiNP–API conjugates qualifying surface functionalization as an effective instrument for optimizing the immune response towards SiNPs. This study further suggests that surface-functionalized SiNPs could be a suitable, immunologically inert vehicle for the efficient delivery of biopharmaceutical products, as evidenced here for allergen-specific immunotherapy.
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Putri, Arlina Prima, Francesco Picchioni, Sri Harjanto, and Mochamad Chalid. "Alginate Modification and Lectin-Conjugation Approach to Synthesize the Mucoadhesive Matrix." Applied Sciences 11, no. 24 (December 13, 2021): 11818. http://dx.doi.org/10.3390/app112411818.
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Alginates are natural anionic polyelectrolytes investigated in various biomedical applications, such as drug delivery, tissue engineering, and 3D bioprinting. Functionalization of alginates is one possible way to provide a broad range of requirements for those applications. A range of techniques, including esterification, amidation, acetylation, phosphorylation, sulfation, graft copolymerization, and oxidation and reduction, have been implemented for this purpose. The rationale behind these investigations is often the combination of such modified alginates with different molecules. Particularly promising are lectin conjugate macromolecules for lectin-mediated drug delivery, which enhance the bioavailability of active ingredients on a specific site. Most interesting for such application are alginate derivatives, because these macromolecules are more resistant to acidic and enzymatic degradation. This review will report recent progress in alginate modification and conjugation, focusing on alginate-lectin conjugation, which is proposed as a matrix for mucoadhesive drug delivery and provides a new perspective for future studies with these conjugation methods.
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Verma, Deepak, Manunya Okhawilai, Kheng Lim Goh, and Mohit Sharma. "Thermomechanical Analyses of Alkali-Treated Coconut Husk-Bagasse Fiber-Calcium Carbonate Hybrid Composites." Sustainability 15, no. 2 (January 16, 2023): 1686. http://dx.doi.org/10.3390/su15021686.
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Natural fiber-reinforced composites can contribute to reducing carbon footprint goals due to their ability to reduce overall product weight, bio-diverse feedstocks, and recyclability potential. In this work, natural fiber-based composites containing the reinforcement of coconut husk and bagasse fiber with calcium carbonate (CaCO3) ingredients were prepared and analyzed. The composites were analyzed for mechanical, thermomechanical, and morphological properties. The reinforcements were chemically functionalized using 5% w/v NaOH to enhance their interactions with the epoxy resins. The chemical functionalization created perforation on the fiber surface, improving the interlocking of fibres with the resin material and strengthening the mechanical performance of the composite. The composites developed using modified reinforcement treatment resulted in increased tensile strength (64.8%) and flexural strength (70%). The reinforcement treatment influenced the hydrophilicity, and the water absorption of treated composites was reduced more than five times compared to the unmodified composites. Scanning electron microscopy revealed morphological changes due to fiber modification, the underlaying mechanism of fiber contraction, and enhanced fiber matrix interface interlocking and adhesion strengthening. Thermal analysis confirmed that alkali treatment improves the crystallinity of the fiber and thereto the degradation temperature of treated fiber composites (both bagasse and coconut husk), which is 375.27 °C, the highest amongst the developed hybrid composites.
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De Pasquale, Ilaria, Michela Verni, Vito Verardo, Ana María Gómez-Caravaca, and Carlo Giuseppe Rizzello. "Nutritional and Functional Advantages of the Use of Fermented Black Chickpea Flour for Semolina-Pasta Fortification." Foods 10, no. 1 (January 18, 2021): 182. http://dx.doi.org/10.3390/foods10010182.
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Pasta represents a dominant portion of the diet worldwide and its functionalization with high nutritional value ingredients, such as legumes, is the most ideal solution to shape consumers behavior towards healthier food choices. Aiming at improving the nutritional quality of semolina pasta, semi-liquid dough of a Mediterranean black chickpea flour, fermented with Lactiplantibacillus plantarum T0A10, was used at a substitution level of 15% to manufacture fortified pasta. Fermentation with the selected starter enabled the release of 20% of bound phenolic compounds, and the conversion of free compounds into more active forms (dihydrocaffeic and phloretic acid) in the dough. Fermented dough also had higher resistant starch (up to 60% compared to the control) and total free amino acids (almost 3 g/kg) contents, whereas antinutritional factors (raffinose, condensed tannins, trypsin inhibitors and saponins) significantly decreased. The impact of black chickpea addition on pasta nutritional, technological and sensory features, was also assessed. Compared to traditional (semolina) pasta, fortified pasta had lower starch hydrolysis rate (ca. 18%) and higher in vitro protein digestibility (up to 38%). Moreover, fortified cooked pasta, showing scavenging activity against DPPH and ABTS radicals and intense inhibition of linoleic acid peroxidation, was appreciated for its peculiar organoleptic profile. Therefore, fermentation technology appears to be a promising tool to enhance the quality of pasta and promote the use of local chickpea cultivars while preventing their genetic erosion.
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Taherzade, Seyed Dariush, Sara Rojas, Janet Soleimannejad, and Patricia Horcajada. "Combined Cutaneous Therapy Using Biocompatible Metal-Organic Frameworks." Nanomaterials 10, no. 12 (November 25, 2020): 2296. http://dx.doi.org/10.3390/nano10122296.
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Combined therapies emerge as an interesting tool to overcome limitations of traditional pharmacological treatments (efficiency, side effects). Among other materials, metal-organic frameworks (MOFs) offer versatilities for the accommodation of multiple and complementary active pharmaceutical ingredients (APIs): accessible large porosity, availability of functionalization sites, and biocompatibility. Here, we propose topical patches based on water-stable and biosafe Fe carboxylate MOFs (MIL-100 and MIL-127), the biopolymer polyvinyl alcohol (PVA) and two co-encapsulated drugs used in skin disorders (azelaic acid (AzA) as antibiotic, and nicotinamide (Nic) as anti-inflammatory), in order to develop an advanced cutaneous combined therapy. Exceptional MOF drug contents were reached (total amount 77.4 and 48.1 wt.% for MIL-100 and MIL-127, respectively), while an almost complete release of both drugs was achieved after 24 h, adapted to cutaneous delivery. The prepared cutaneous PVA-MOF formulations are safe and maintain the high drug-loading capacity (total drug content of 38.8 and 24.2 wt.% for MIL-100 and MIL-127, respectively), while allowing a controlled delivery of their cargoes, permeating through the skin to the active target sites. The total amount of drug retained or diffused through the skin is within the range (Nic), or even better (AzA) than commercial formulations. The presented results make these drug combined formulations promising candidates for new cutaneous devices for skin treatment.
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Porcello, Alexandre, Michèle Chemali, Cíntia Marques, Corinne Scaletta, Kelly Lourenço, Philippe Abdel-Sayed, Wassim Raffoul, Nathalie Hirt-Burri, Lee Ann Applegate, and Alexis Laurent. "Dual Functionalization of Hyaluronan Dermal Fillers with Vitamin B3: Efficient Combination of Bio-Stimulation Properties with Hydrogel System Resilience Enhancement." Gels 10, no. 6 (May 24, 2024): 361. http://dx.doi.org/10.3390/gels10060361.
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Hyaluronic acid (HA) hydrogels are commonly used for facial dermal filling and for alternative medical aesthetic purposes. High diversity exists in commercial formulations, notably for the optimization of finished product stability, functionality, and performance. Polyvalent ingredients such as calcium hydroxylapatite (CaHA) or vitamin B3 (niacinamide) are notably used as bio-stimulants to improve skin quality attributes at the administration site. The aim of the present study was to perform multi-parametric characterization of two novel cross-linked dermal filler formulas (HAR-1 “Instant Refine” and HAR-3 “Maxi Lift”) for elucidation of the various functional impacts of vitamin B3 incorporation. Therefore, the HAR products were firstly comparatively characterized in terms of in vitro rheology, cohesivity, injectability, and resistance to chemical or enzymatic degradation (exposition to H2O2, AAPH, hyaluronidases, or xanthine oxidase). Then, the HAR products were assessed for cytocompatibility and in vitro bio-stimulation attributes in a primary dermal fibroblast model. The results showed enhanced resilience of the cohesive HAR hydrogels as compared to JUVÉDERM® VOLBELLA® and VOLUMA® reference products in a controlled degradation assay panel. Furthermore, significant induction of total collagen synthesis in primary dermal fibroblast cultures was recorded for HAR-1 and HAR-3, denoting intrinsic bio-stimulatory effects comparable or superior to those of the Radiesse® and Sculptra™ reference products. Original results of high translational relevance were generated herein using robust and orthogonal experimental methodologies (hydrogel degradation, functional benchmarking) and study designs. Overall, the reported results confirmed the dual functionalization role of vitamin B3 in cross-linked HA dermal fillers, with a significant enhancement of hydrogel system stability attributes and the deployment of potent bio-stimulatory capacities.
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Phonesouk, Erick, Séverine Lechevallier, Audrey Ferrand, Marie-Pierre Rols, Christine Bezombes, Marc Verelst, and Muriel Golzio. "Increasing Uptake of Silica Nanoparticles with Electroporation: From Cellular Characterization to Potential Applications." Materials 12, no. 1 (January 7, 2019): 179. http://dx.doi.org/10.3390/ma12010179.
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In the fields of biology and medicine, nanoproducts such as nanoparticles (NPs) are specifically interesting as theranostic tools, since they offer the double capacity to locally deliver active drugs and to image exactly where the product is delivered. Among the many described possibilities, silica nanoparticles (SiNPs) represent a good choice because of their ease of synthesis, the possibility of their vast functionalization, and their good biocompatibility. However, SiNPs’ passive cell internalization by endocytosis only distributes NPs into the cell cytoplasm and is unable to target the nucleus if SiNPs are larger than a few nanometers. In this study, we demonstrate that the cell penetration of SiNPs of 28–30 nm in diameter can be strongly enhanced using a physical method, called electroporation or electropermeabilization (EP). The uptake of fluorescently labelled silica nanoparticles was improved in two different cancer cell lines, namely, HCT-116 (human colon cancer) cells and RL (B-lymphoma) cells. First, we studied cells’ capability for the regular passive uptake of SiNPs in vitro. Then, we set EP parameters in order to induce a more efficient and rapid cell loading, also comprising the nuclear compartment, while preserving the cell viability. In the final approach, we performed in vivo experiments, and evidenced that the labeling was long-lasting, as confirmed by fluorescence imaging of labeled tumors, which enabled a 30-day follow-up. This kind of SiNPs delivery, achieved by EP, could be employed to load extensive amounts of active ingredients into the cell nucleus, and concomitantly allow the monitoring of the long-term fate of nanoparticles.
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Wang, Guanyu, Qiaoge Fu, Ruili Guo, and Zhong Wei. "Selective adsorption and separation of stevioside and rebaudioside A by a metal-organic framework with boronic acid." Canadian Journal of Chemistry 98, no. 11 (November 2020): 708–16. http://dx.doi.org/10.1139/cjc-2020-0175.
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The boronic acid functionalization metal-organic frameworks (MOFs), as unique boronate affinity adsorbents, have desired specific molecular affinity for the separation and enrichment of cis-diol-compounds. Herein, the boronic acid functionalized Zn-based MOF adsorbent (MOF-BA) was synthesized through a simple one-step microwave method and used for the recognition and isolation of steviol glycosides (SGs). This MOF-BA exhibits the same spherical structure and isostructure with the parent framework composed only of the primitive ligand as verified by SEM and XRD characterization. It was confirmed that changing the ratio of ligands could achieve the adjustability of the boron content in the framework. At the same time, the MOF-BA-1.0 showed a suitable pore size (4.69 nm), and the presence of boric acid functional groups showed favorable selectivity for stevioside (STV). The static adsorption results showed that adsorption performances of rebaudioside A (RA) and STV from crude sugar solution (5.0 mg mL−1, pH 8) on MOF-BA-1.0 were investigated at 303 K for 15 h. The adsorption capacities for STV and RA were 42.93 mg g−1 and 22.96 mg g−1, respectively, and the adsorption selectivity (αSTV/RA) reached 4.35. The adsorption isotherm and kinetic data of MOF-BA-1.0 for RA and STV obeyed the Langmuir isotherm model and pseudo second order kinetic model, respectively. The study demonstrated that MOF-BA-1.0 adsorbent could be used as a potential adsorbent to purify the active ingredients of stevia and obtain a high concentration of RA products.
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Ambrogi, Valeria. "A New Challenge for the Old Excipient Calcium Carbonate: To Improve the Dissolution Rate of Poorly Soluble Drugs." Pharmaceutics 15, no. 1 (January 16, 2023): 300. http://dx.doi.org/10.3390/pharmaceutics15010300.
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Calcium carbonate is an excipient traditionally used in solid dosage forms with several functions such as a diluent, a quick dissolution agent, a buffer and an opacifier. Recently, many other challenges have arisen for calcium carbonate and, among them, the possibility of using it as an excipient for improving the dissolution rate of poorly soluble drugs. As a consequence of their poor solubility in biological fluids, many active ingredients suffer from low and erratic bioavailability when administered by the oral route and thus, many formulation strategies and excipients have been proposed to overcome this problem. Among them, calcium carbonate has been proposed as an excipient for improving dissolution rates. Calcium carbonate has many interesting characteristics, in fact it dissolves quickly in gastric fluid, is inexpensive and is safe. It exists in different polymorphic forms and in porous morphology and recently a porous functionalized calcium carbonate has been proposed as a new excipient. This review is the first overview on the use of calcium carbonate as an excipient for improving drug dissolution rates. The drug loading procedure, the physical characterization of the drug/CaCO3 samples and their dissolution profiles will be described. Moreover, the possible mechanisms of dissolution improvement, such as the presence of the drug in amorphous or polymorphic forms, in small crystals, and the effects of CaCO3 dissolution in acidic medium will be discussed. Different polymorphic forms of calcium carbonate and the presence of porosity and functionalization will be analyzed as well and their effects on dissolution rates will be discussed.
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da Silva, Geisiane Rosa, Amanda Luizetto dos Santos, Andrey Coatrini Soares, Marinalva Cardoso dos Santos, Sandra Cruz dos Santos, Ştefan Ţălu, Vânia Rodrigues de Lima, Vanderlei Salvador Bagnato, Edgar Aparecido Sanches, and Natalia Mayumi Inada. "PLGA-PVA-PEG Single Emulsion Method as a Candidate for Aminolevulinic Acid (5-ALA) Encapsulation: Laboratory Scaling up and Stability Evaluation." Molecules 27, no. 18 (September 15, 2022): 6029. http://dx.doi.org/10.3390/molecules27186029.
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One of the most widely used molecules used for photodynamic therapy (PDT) is 5-aminolevulinic acid (5-ALA), a precursor in the synthesis of tetrapyrroles such as chlorophyll and heme. The 5-ALA skin permeation is considerably reduced due to its hydrophilic characteristics, decreasing its local bioavailability and therapeutic effect. For this reason, five different systems containing polymeric particles of poly [D, L–lactic–co–glycolic acid (PLGA)] were developed to encapsulate 5-ALA based on single and double emulsions methodology. All systems were standardized (according to the volume of reagents and mass of pharmaceutical ingredients) and compared in terms of laboratory scaling up, particle formation and stability over time. UV-VIS spectroscopy revealed that particle absorption/adsorption of 5-ALA was dependent on the method of synthesis. Different size distribution was observed by DLS and NTA techniques, revealing that 5-ALA increased the particle size. The contact angle evaluation showed that the system hydrophobicity was dependent on the surfactant and the 5-ALA contribution. The FTIR results indicated that the type of emulsion influenced the particle formation, as well as allowing PEG functionalization and interaction with 5-ALA. According to the 1H-NMR results, the 5-ALA reduced the T1 values of polyvinyl alcohol (PVA) and PLGA in the double emulsion systems due to the decrease in molecular packing in the hydrophobic region. The results indicated that the system formed by single emulsion containing the combination PVA–PEG presented greater stability with less influence from 5-ALA. This system is a promising candidate to successfully encapsulate 5–ALA and achieve good performance and specificity for in vitro skin cancer treatment.
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Mahendra, Brillian Ardy, Satrio Herbirowo, Iman Saefuloh, and Murni Handayani. "Pengembangan Material Maju Superkonduktor Mg-B dengan Penambahan Graphene Oxide melalui Proses Powder in Sealed Tube." Jurnal Mesin Nusantara 5, no. 1 (June 30, 2022): 96–107. http://dx.doi.org/10.29407/jmn.v5i1.17894.
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MgB2 is a high possible superconducting material that can be applied quite practically with the functionalization of Mg-B materials. Material development is carried out by adding carbon, namely Graphene Oxide (GO), which is a single atom layered material. The Powder in Sealed Tube (PIST) method is practically used to reduce oxidation. This study aims to analyze the effect of GO material doped with the PIST method made from MgB2 with a sintering temperature of 800℃ for 2 hours on its superconductivity, compound formation, and microstructure. The manufacturing process is carried out in a 1:2 ratio where 98% purity Mg is mixed with Boron, which is then added with 0, 0.3 and 3% wt GO doping, all ingredients are mixed stoichiometrically. The material that has been put in a tube and compacted sufficiently into SS316L which has been closed on one side to enter the powder, is then compacted with high pressure up to 1000 MPa. The material is sintered at a temperature of 800℃ for 2 hours which is then carried out by cooling in the furnace and taking bulk samples. The XRD results showed the formation of the dominant MgB2 phase and the formation of an impurity phase in the form of MgO and obtained a decent crystal size of 295 which was owned by the 3%wt GO PIST MgB2 sample. The SEM test shows the forms of formation (agglomeration) in each sample, with the presence of several axes. Cryogenic testing shows that with doping there is a movement of critical temperature to a lower direction where MgB2 0%wt GO has a TcOnset value of 39.4 K and a TcZero of 38.7 K, while MgB2 3%wt GO has a TcOnset value of 39.6 K and TcZero of 38 K.
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Sencanski, Jelena, Milica Vujkovic, Ivana Stojkovic, Divna Majstorovic, Danica Bajuk-Bogdanovic, Ferenc Pastor, and Slavko Mentus. "Recycling of LiCo0.59Mn0.26Ni0.15O2 cathodic material from spent Li-ion batteries by the method of the citrate gel combustion." Chemical Industry 71, no. 3 (2017): 211–20. http://dx.doi.org/10.2298/hemind160418031s.
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The Li-ion batteries are the main power source for the high technology devices, such as mobile phones and electric vehicles. Because of that, the number of spent Li-ion batteries significantly increases. Today, the number of active mobile phones crossed 7.19 billion. It is estimated that the mass of the spent lithium ion batteries in China will exceed 500,000 t by 2020. The trouble is in the ingredients of these batteries. They contain Li, Co, Mn, Ni, Cu, Al and toxic and flammable electrolytes which have a harmful affection to the environment. Because of that, the recycling procedure attracts raising attention of researches. Several commercial spent Li-ion batteries were recycled by the relatively fast, economic and simple procedure. The three ways of separating the cathode material from Al collector were examined after the manual dismantling of the components of batteries with the Li(Co?Mn?Ni)O2 as cathode material. These were: 1. dissolution of the Al collector in the alkali medium, 2. peeling off with N-methylpyrrolidone and 3. thermal decomposition of the adhesive at 700?C. The procedure with the highest yield was the one with the dissolution in alkali medium. The chemical analysis of the single batteries'' components (the crust, Al/Cu collector, cathode material) were done by the atomic absorption spectrometry. The components, before the analysis, were dissolved. The re-synthesis of the cathode material by the method of the citrate gel combustion was done after the separating the cathode material and dissolving it in the nitric acid. The obtained product was, after annealing, characterized by the methods of X-ray diffraction and Raman spectroscopy. The recycled product was LiCo0.59Mn0.26Ni0.15O2 stoichiometry, with the hexagonal layered structure ?-NaFeO2 type. The functionalization of the resynthesized material was examined in the 1 M solution LiClO4 in the propylene carbonate, by galvanostatic charging, with the current density of 0.7C. The recycled material showed relatively good capacities of charging and discharging which are 94.9 i 64.8 mA h g?1, respectively.
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Hole, Ratnakar, Achut Munde, and Sandesh Jaybhaye. "Functionalization of multiwalled carbon nanotubes with active pharmaceutical ingredient via carboxylation." Materials Today: Proceedings, July 2020. http://dx.doi.org/10.1016/j.matpr.2020.06.089.
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R.Leivas, Fernanda, and Marcia C. Barbosa. "Functionalized carbon nanocones performance in water harvesting." Journal of Chemical Physics 158, no. 19 (May 15, 2023). http://dx.doi.org/10.1063/5.0142718.
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In this work, we investigate the water capture process for functionalized carbon nanocones (CNCs) through molecular dynamic simulations in the following three scenarios: a single CNC in contact with a reservoir containing liquid water, a single CNC in contact with a water vapor reservoir, and a combination of more than one CNC in contact with vapor. We found that water flows through the nanocones when in contact with the liquid reservoir if the nanocone tip presents hydrophilic functionalization. In contact with steam, we observed the formation of droplets at the base of the nanocone only when hydrophilic functionalization is present. Then, water flows through in a linear manner, a process that is more efficient than that in the liquid reservoir regime. The scalability of the process is tested by analyzing the water flow through more than one nanocone. The results suggest that the distance between the nanocones is a fundamental ingredient for the efficiency of water harvesting.
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Lutter, Ferdinand H., Lucie Grokenberger, Luca Alessandro Perego, Diego Broggini, Sébastien Lemaire, Simon Wagschal, and Paul Knochel. "Regioselective functionalization of aryl azoles as powerful tool for the synthesis of pharmaceutically relevant targets." Nature Communications 11, no. 1 (September 7, 2020). http://dx.doi.org/10.1038/s41467-020-18188-z.
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Abstract Aryl azole scaffolds are present in a wide range of pharmaceutically relevant molecules. Their ortho-selective metalation at the aryl ring is challenging, due to the competitive metalation of the more acidic heterocycle. Seeking a practical access to a key Active Pharmaceutical Ingredient (API) intermediate currently in development, we investigated the metalation of 1-aryl-1H-1,2,3-triazoles and other related heterocycles with sterically hindered metal-amide bases. We report here a room temperature and highly regioselective ortho-magnesiation of several aryl azoles using a tailored magnesium amide, TMPMgBu (TMP = 2,2,6,6-tetramethylpiperidyl) in hydrocarbon solvents followed by an efficient Pd-catalyzed arylation. This scalable and selective reaction allows variation of the initial substitution pattern of the aryl ring, the nature of the azole moiety, as well as the nature of the electrophile. This versatile method can be applied to the synthesis of bioactive azole derivatives and complements existing metal-mediated ortho-functionalizations.
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Kumar, Sanjeev, and Ajay K. Singh. "Micro-photo-flow reactor system for fused N-heteroaryl scaffold synthesis and late-stage functionalization of pyrazolopyridines." Chemical Communications, 2022. http://dx.doi.org/10.1039/d2cc03713k.
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Late-stage functionalization (LSF) of active pharmaceutical ingredients can provide a straightforward approach to efficient de-novo design and synthesis of the drug molecule for the structural activity relationship studies (SARS). Herein,...
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Ibrahim, Nabil A., Hala A. Amin, Mohamed S. Abdel-Aziz, and Basma M. Eid. "A green approach for modification and functionalization of wool fabric using bio- and nano-technologies." Clean Technologies and Environmental Policy, September 2, 2022. http://dx.doi.org/10.1007/s10098-022-02385-z.
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AbstractIn the present work, we propose a green and sustainable strategy for eco-friendly surface modification of wool structure using biosynthesized kerationlytic proteases, from C4-ITA-EGY, Streptomyces harbinensis S11-ITA-EGY and Streptomyces carpaticus S33-ITA-EGY, followed by subsequent environmentally sound functionalization of the bio-treated substrates using ZnONPs, ZrO2NPs, ascorbic acid and vanillin, individually, to provide durable antibacterial as well as UV-protection properties. Both surface modification changes and the extent of functionalization of the final products were characterized by SEM, EDX, antibacterial efficacy, UV-blocking ability, loss in weight, nitrogen content and durability to washing analysis. The obtained data reveal that the developed green wool fabrics exhibit outstanding durable antibacterial activity and UV-blocking ability for fabricating multi-functional textile products that can be utilized in a wide range of sustainable protective textiles, irrespective of the used post-finishing formulation ingredients. The results also show that both modification and functionalization processes are governed by the type of enzyme and kind of active material respectively. Moreover, the biosynthesized kerationlytic proteases could be accessibly used to remove protein-based stains like blood and egg. Graphical abstract
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Li, Ruifeng, Marcel Schmidt, Tong Zhu, Xinyu Yang, Jing Feng, Yu’e Tian, Yinglu Cui, Timo Nuijens, and Bian Wu. "Traceless enzymatic protein synthesis without ligation sites constraint." National Science Review, August 24, 2021. http://dx.doi.org/10.1093/nsr/nwab158.
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Abstract Protein synthesis and semisynthesis offer immense promise for life science and have impacted pharmaceutical innovation. Nevertheless, the absence of a generally applicable method for traceless peptide conjugation with a flexible choice of junction sites remains a bottleneck for accessing many important synthetic targets. Here we introduce the protein activation and ligation with multiple enzymes (PALME) platform designed for the sequence-unconstrained synthesis and modification of biomacromolecules. The upstream activating modules accept and process easily accessible synthetic peptides and recombinant proteins, avoiding the challenges associated with the preparation and manipulation of activated peptide substrates. Cooperatively, the downstream coupling module provides comprehensive solutions for sequential peptide condensation, cyclization, and protein N/C-terminal or internal functionalization. This methodology's practical utility was demonstrated by synthesizing a series of bioactive targets ranging from pharmaceutical ingredients to synthetically challenging proteins. Together, the modular PALME platform exhibits unprecedented broad accessibility for the traceless protein synthesis and functionalization and holds enormous potential to extend the scope of protein chemistry and synthetic biology.
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Simon, Hendrik, Agnese Zangarelli, Tristan Bauch, and Lutz Ackermann. "Ruthenium(II)‐Catalyzed Late‐Stage Incorporation of N‐Aryl Triazoles and Tetrazoles with Sulfonium Salts via C–H Activation." Angewandte Chemie, April 15, 2024. http://dx.doi.org/10.1002/ange.202402060.
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The late‐stage functionalization of active pharmaceutical ingredients is a key challenge in medicinal chemistry. Furthermore, N‐aryl triazoles and tetrazoles are important structural motifs with the potential to boost the activity of diverse drug molecules. Using easily accessible dibenzothiophenium salts for the ruthenium‐catalyzed C–H arylation, these scaffolds were introduced into a variety of bioactive compounds. Our methodology uses cost‐efficient ruthenium, KOAc as a mild base and gives access to a plethora of highly decorated triazole and tetrazole containing drug derivatives.