Articles de revues : « Nanoparticles, folic acid, camptothecin, Hela »

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Ancira-Cortez, Alejandra, Enrique Morales-Avila, Blanca E. Ocampo-García, Carlos González-Romero, Luis A. Medina, Gustavo López-Téllez et Erick Cuevas-Yáñez. « Preparation and Characterization of a Tumor-Targeting Dual-Image System Based on Iron Oxide Nanoparticles Functionalized with Folic Acid and Rhodamine ». Journal of Nanomaterials 2017 (2017) : 1–11. http://dx.doi.org/10.1155/2017/5184167.

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Cancer is one of the diseases with most deaths worldwide, around 8.2 million annually. For this reason, several treatments and diagnostic tools have been investigated and developed over the past decades. Among them, a dual-image system has been developed to achieve and enhance the detection of cancer, which has not been done with systems currently available. The present study describes the preparation of a dual-image targeting system composed of magnetic iron oxide nanoparticles functionalized with folic acid and rhodamine; nanoparticles synthesis was achieved by a coprecipitation method; the functionalization was carried out by a carbodiimide with folic acid and/or the rhodamine isothiocyanate; conjugates were characterized by spectrometric techniques; toxicity was measured by cell proliferation assay on HeLa cells using progressive concentrations of functionalized nanoparticles. Cellular uptake assay was carried out by competitive assay on HeLa cells. Iron oxide magnetite nanoparticles, modified with folic acid and rhodamine, were successfully synthetized with a particle size lower than 20 nm (TEM), EDS, HRTEM, and XDR showed highly crystalline Fe3O4 nanoparticles. Folic acid and rhodamine were conjugated with high efficiency. A significant selectivity and uptake, facilitated by surface modification of iron oxide nanoparticles with folic acid, were demonstrated. The multifunctional system showed suitable physicochemical and biological properties for cell targeting through folate receptors.

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Guerrero-Florez, Valentina, Stelia C. Mendez-Sanchez, Olga A. Patrón-Soberano, Vicente Rodríguez-González, Diana Blach et Fernando Martínez O. « Gold nanoparticle-mediated generation of reactive oxygen species during plasmonic photothermal therapy : a comparative study for different particle sizes, shapes, and surface conjugations ». Journal of Materials Chemistry B 8, n^o 14 (2020) : 2862–75. http://dx.doi.org/10.1039/d0tb00240b.

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Xia, Yu, Tiantian Xu, Mingqi Zhao, Liang Hua, Yi Chen, Changbing Wang, Ying Tang et Bing Zhu. « Delivery of Doxorubicin for Human Cervical Carcinoma Targeting Therapy by Folic Acid-Modified Selenium Nanoparticles ». International Journal of Molecular Sciences 19, n^o 11 (13 novembre 2018) : 3582. http://dx.doi.org/10.3390/ijms19113582.

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Cancer-specific drug delivery represents an attractive approach to preventing undesirable side effects and increasing the accumulation of the drug in tumors. The surface modification of selenium nanoparticles (SeNPs) with targeting moieties thus represents an effective strategy for cancer therapy. In this study, SeNPs were modified with folic acid (FA), whose receptors were overexpressed on the surface of cancer cells, including human cervical carcinoma HeLa cells, to fabricate tumor-targeting delivery carrier FA-SeNPs nanoparticles. Then, the anticancer drug doxorubicin (DOX) was loaded onto the surface of the FA-SeNPs for improving the antitumor efficacy of DOX in human cervical carcinoma therapy. The chemical structure characterization of FA-Se@DOX showed that DOX was successfully loaded to the surface of FA-SeNPs to prepare FA-Se@DOX nanoparticles. FA-Se@DOX exhibited significant cellular uptake in human cervical carcinoma HeLa cells (folate receptor overexpressing cells) in comparison with lung cancer A549 cells (folate receptor deficiency cells), and entered HeLa cells mainly by the clathrin-mediated endocytosis pathway. Compared to free DOX or Se@DOX at the equivalent dose of DOX, FA-Se@DOX showed obvious activity to inhibit HeLa cells’ proliferation and induce the apoptosis of HeLa cells. More importantly, FA-Se@DOX could specifically accumulate in the tumor site, which contributed to the significant antitumor efficacy of FA-Se@DOX in vivo. Taken together, FA-Se@DOX may be one novel promising drug candidate for human cervical carcinoma therapy.

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Xuan, Guangshan, Min Zhang, Yang Chen, Shan Huang et Imshik Lee. « Design and Characterization of a Cancer-Targeted Drug Co-Delivery System Composed of Liposomes and Selenium Nanoparticles ». Journal of Nanoscience and Nanotechnology 20, n^o 9 (1 septembre 2020) : 5295–304. http://dx.doi.org/10.1166/jnn.2020.17882.

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A drug co-delivery system composed of selenium nanoparticles (SeNPs) has attracted increasing interest due to its ability to increase the anticancer efficacy against multidrug-resistant cancer cells. In this study, a cancer-targeted drug co-delivery system combining fluorescein-loaded liposomes and SeNPs was designed and evaluated. The system was developed by coating SeNPs and fluorescein-loaded liposomes with folic acid-chitosan conjugates (FA-CS-SeNPs-Lips). Folic acid-chitosan conjugates (FA-CS) were synthesized by coupling folic acid (FA) with chitosan (CS), and the structure was confirmed by performing Fourier transform spectroscopy (FT-IR) and nuclear magnetic resonance (1H-NMR) spectroscopy. Dynamic light scattering (DLS) measurements and transmission electron microscopy (TEM) were used to evaluate the particle size, Zeta potential, and morphology. The cytotoxicity of SeNPs coated with FA-CS conjugates (FA-CS-SeNPs) toward A549 cells and HeLa cells was examined using the MTT assay. The cancer-targeting ability and drug release behaviors were evaluated in vitro by measuring the cellular uptake of fluorescein and dialysis, respectively. The FA-CS-SeNPs were uniform, spherical particles with a ~50 nm diameter and high positive Zeta potential (+57.7 mV). Based on the results of the MTT assay, FA-CS-SeNPs displayed a more significant increase in the anticancer efficacy in HeLa cells than CS-SeNPs. FA-CS-SeNPs-Lips not only slowly released fluorescein but also specifically targeted HeLa cells through selective binding between folate and folate receptors to increase the cellular uptake of fluorescein.

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Zhou, Yu, Yanming Han, Gaiyun Li, Sheng Yang, Fuquan Xiong et Fuxiang Chu. « Preparation of Targeted Lignin–Based Hollow Nanoparticles for the Delivery of Doxorubicin ». Nanomaterials 9, n^o 2 (2 février 2019) : 188. http://dx.doi.org/10.3390/nano9020188.

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Due to their exceptional absorption capacity, biodegradability, and non-toxicity, nanoparticles (NPs) from lignin have emerged as vehicles for inorganic particles and drug molecules. However, the method for preparing targeted lignin particles is still complex and lacks sufficient research. Herein, a succinct strategy was proposed for the preparation of targeted lignin-based drug delivery NPs to load Doxorubicin Hydrochloride (DOX). The lignin hollow NPs (LHNPs) were used as a platform for the preparation of targeted delivery material by incorporating magnetic NPs and folic acid (FA) via layer-by-layer self-assembling. The results showed that the surface of LHNPs was covered uniformly by Fe3O4 NPs and grafted with folic acid. The folic-magnetic-functionalized lignin hollow NPs (FA-MLHNPs) could respond to magnetic field and folic acid receptors. In addition, the targeting performance of the FA-MLHNPs increased the cellular uptake of NPs in the case of HeLa cells. This research not only supported the modified NPs platform as a highly efficient nano-delivery method but also provided a facile approach to utilize renewable lignin biomaterials.

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Zu, Yuangang, Dan Wang, Xiuhua Zhao, Ru Jiang, Qi Zhang, Dongmei Zhao, Yong Li, Baishi Zu et Zhiqiang Sun. « A Novel Preparation Method for Camptothecin (CPT) Loaded Folic Acid Conjugated Dextran Tumor-Targeted Nanoparticles ». International Journal of Molecular Sciences 12, n^o 7 (28 juin 2011) : 4237–49. http://dx.doi.org/10.3390/ijms12074237.

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Erdem, M., S. Yalcin et U. Gunduz. « Folic acid-conjugated polyethylene glycol-coated magnetic nanoparticles for doxorubicin delivery in cancer chemotherapy : Preparation, characterization and cytotoxicity on HeLa cell line ». Human & ; Experimental Toxicology 36, n^o 8 (10 octobre 2016) : 833–45. http://dx.doi.org/10.1177/0960327116672910.

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Conventional chemotherapy is the most valid method to cope with cancer; however, it has serious drawbacks such as decrease in production of blood cells or inflammation of the lining of the digestive tract. These side effects occur since generally the drugs used in chemotherapy are distributed evenly within the body of the patient and cannot distinguish the cancer cells from the healthy ones. In this study, folic acid (FA)-conjugated, polyethylene-coated magnetic nanoparticles (FA-MNPs), and doxorubicin (Dox)-loaded formulation (Dox-FA-MNPs) were prepared. The cytotoxicity of these nanoparticles on HeLa and Dox-resistant HeLa cells was investigated. Magnetic nanoparticles (MNPs), polyethylene glycol (PEG)-coated MNPs (PEG-MNPs), and FA-MNPs were successfully synthesized and characterized by several methods. Dox loading of FA-MNPs and release profile of Dox from the nanoparticles were studied. Cytotoxic effects of FA-MNPs and Dox-FA-MNPs on HeLa cells were analyzed. MNPs, PEG-MNPs, and FA-MNPs all had small sizes and supermagnetic behavior. High amounts of Dox could be loded onto the nanoparticles (290 μgmL−1). In 24 h, 15.7% of Dox was released from the Dox-FA-MNPs. The release was increased in acidic conditions (pH 4.1). Internalization studies showed that FA-MNPs and Dox-FA-MNPs were taken up efficiently by HeLa cells. The investigation of cytotoxicity of the particles indicated that 38–500 μgmL−1 Dox-FA-MNPs significantly decreased the proliferation of HeLa cells compared to FA-MNPs. Due to their size, magnetic properties, internalization, drug release, and cytotoxicity characteristics, the MNPs prepared in this study may have potential application as a drug delivery system in cancer chemotherapy.

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Zheng, Xiawen, Yuejian Chen, Zhiming Wang, Lina Song, Yu Zhang, Ning Gu et Fei Xiong. « Preparation and In Vitro Cellular Uptake Assessment of Multifunctional Rubik-Like Magnetic Nano-Assemblies ». Journal of Nanoscience and Nanotechnology 19, n^o 6 (1 juin 2019) : 3301–9. http://dx.doi.org/10.1166/jnn.2019.16129.

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Through self-assembly of nanoparticles into high-order and stable structures of cubic clusters, high drug-loading rubik-like magnetic nano-assemblies (MNAs), possessing folic acid targeting and strong magnetism-enhanced cellular uptake capabilities, were built. In this study, the core of the cubic drug assemblies consisted of four monodisperse superparamagnetic iron oxide nanoparticles coated with layers of oleic acid (Fe3O4@OA), simultaneously encapsulating fluorescein, and Paclitaxol (Flu-MNAs and PTX-MNAs) for imaging and therapeutic applications. To enable preferential tumor cellular uptake by the nanocarriers, the outermost layer of Fe3O4 was functionalized with the new dual-oleic acid-polyethylene glycol-folic acid polymer (FA-PEG-Lys-OA2) as a “shell.” The drug carriers exhibited excellent stability and biocompatibility, and showed high drug loading and excellent magnetic response In Vitro. Furthermore, preliminary evaluations of the drug carriers with Hela cells showed effective cellular targeting capability. In addition, the cubic assemblies enhanced anticancer efficiency for Hela cells compared to bare drugs. Especially, the applied external magnetic field further improved the uptake of the vectors, and thereby enhanced the inhibitory effect. In brief, all these results suggested that cubic assemblies could serve as potential strategies for targeted anticancer therapies.

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Liu, Min-Chao, Bing Liu, Xian-Li Chen, Hui-Chao Lin, Xiang-Yu Sun, Jia-Zheng Lu, Yan-Yu Li, Si-Qi Yan, Lu-Yong Zhang et Ping Zhao. « Calcium carbonate end-capped, folate-mediated Fe3O4@mSiO2 core-shell nanocarriers as targeted controlled-release drug delivery system ». Journal of Biomaterials Applications 32, n^o 8 (22 janvier 2018) : 1090–104. http://dx.doi.org/10.1177/0885328217752994.

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Magnetic mesoporous silica nanospheres (MMSN) were prepared and the surface was modified with cancer cell-specific ligand folic acid. Calcium carbonate was then employed as acid-activated gatekeepers to cap the mesopores of the MMSN, namely, MMSN-FA-CaCO3. The formation of the MMSN-FA-CaCO3 was proved by several characterization techniques, viz. transmission electron microscopy, zeta potential measurement, Fourier transform infrared spectroscopy, BET surface area measurement, and UV–Vis spectroscopy. Daunomycin was successfully loaded in the MMSN-FA-CaCO3 and the system exhibited sensitive pH stimuli-responsive release characteristics under blood or tumor microenvironment. Cellular uptake by folate receptor (FR)-overexpressing HeLa cells of the MMSN-FA-CaCO3 was higher than that by non-folated-conjugated ones. Intracellular-uptake studies revealed preferential uptake of these nanoparticles into FR-positive [FR(+)] HeLa than FR-negative [FR(-)]A549 cell lines. DAPI stain experiment showed high apoptotic rate of MMSN-FA-DNM-CaCO3 to HeLa cells. The present data suggest that the CaCO3 coating and folic acid modification of MMSN are able to create a targeted, pH-sensitive template for drug delivery system with application in cancer therapy.

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Sun, Lining, Zuwu Wei, Haige Chen, Jinliang Liu, Jianjian Guo, Ming Cao, Tieqiao Wen et Liyi Shi. « Folic acid-functionalized up-conversion nanoparticles : toxicity studies in vivo and in vitro and targeted imaging applications ». Nanoscale 6, n^o 15 (2014) : 8878–83. http://dx.doi.org/10.1039/c4nr02312a.

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Three kinds of folate-targeted up-conversion nanoparticle imaging agents were prepared. These nanoparticles show good biocompatibility and up-conversion luminescence emission in water, and low cytotoxicity in vivo and in vitro. They were successfully applied to the targeted imaging of HeLa cells.

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Lim, Kyungseop, Hwang Kyung Kim, Xuan Thien Le, Nguyen Thi Nguyen, Eun Seong Lee, Kyung Taek Oh, Han-Gon Choi et Yu Seok Youn. « Highly Red Light-Emitting Erbium- and Lutetium-Doped Core-Shell Upconverting Nanoparticles Surface-Modified with PEG-Folic Acid/TCPP for Suppressing Cervical Cancer HeLa Cells ». Pharmaceutics 12, n^o 11 (17 novembre 2020) : 1102. http://dx.doi.org/10.3390/pharmaceutics12111102.

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Photodynamic therapy (PDT) combined with upconverting nanoparticles (UCNPs) are viewed together as an effective method of ablating tumors. After absorbing highly tissue-penetrating near-infrared (NIR) light, UCNPs emit a shorter wavelength light (~660 nm) suitable for PDT. In this study, we designed and prepared highly red fluorescence-emitting silica-coated core-shell upconverting nanoparticles modified with polyethylene glycol (PEG5k)-folic acid and tetrakis(4-carboxyphenyl)porphyrin (TCPP) (UCNPs@SiO2-NH2@FA/PEG/TCPP) as an efficient photodynamic agent for killing tumor cells. The UCNPs consisted of two simple lanthanides, erbium and lutetium, as the core and shell, respectively. The unique core-shell combination enabled the UCNPs to emit red light without green light. TCPP, folic acid, and PEG were conjugated to the outer silica layer of UCNPs as a photosensitizing agent, a ligand for tumor attachment, and a dispersing stabilizer, respectively. The prepared UCNPs of ~50 nm diameter and −34.5 mV surface potential absorbed 808 nm light and emitted ~660 nm red light. Most notably, these UCNPs were physically well dispersed and stable in the aqueous phase due to PEG attachment and were able to generate singlet oxygen (1O2) with a high efficacy. The HeLa cells were treated with each UCNP sample (0, 1, 5, 10, 20, 30 μg/mL as a free TCPP). The results showed that the combination of UCNPs@SiO2-NH2@FA/PEG/TCPP and the 808 nm laser was significantly cytotoxic to HeLa cells, almost to the same degree as naïve TCPP plus the 660 nm laser based on MTT and Live/Dead assays. Furthermore, the UCNPs@SiO2-NH2@FA/PEG/TCPP was well internalized into HeLa cells and three-dimensional HeLa spheroids, presumably due to the surface folic acid and small size in conjunction with endocytosis and the nonspecific uptake. We believe that our UCNPs@SiO2-NH2@FA/PEG/TCPP will serve as a new platform for highly efficient and deep-penetrating photodynamic agents suitable for various tumor treatments.

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Mazarío, Eva, Magdalena Cañete, Fernando Herranz, Jorge Sánchez-Marcos, Jesús M. de la Fuente, Pilar Herrasti et Nieves Menéndez. « Highly Efficient T2 Cobalt Ferrite Nanoparticles Vectorized for Internalization in Cancer Cells ». Pharmaceuticals 14, n^o 2 (5 février 2021) : 124. http://dx.doi.org/10.3390/ph14020124.

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Uniform cobalt ferrite nanoparticles have been synthesized using an electrochemical synthesis method in aqueous media. Their colloidal, magnetic, and relaxometric properties have been analyzed. The novelty of this synthesis relies on the use of iron and cobalt foils as precursors, which assures the reproducibility of the iron and cobalt ratio in the structure. A stable and biocompatible targeting conjugate nanoparticle-folic acid (NP-FA) was developed that was capable of targeting FA receptor positivity in HeLa (human cervical cancer) cancer cells. The biocompatibility of NP-FA was assessed in vitro in HeLa cells using the MTT assay, and morphological analysis of the cytoskeleton was performed. A high level of NP-FA binding to HeLa cells was confirmed through qualitative in vitro targeting studies. A value of 479 Fe+Co mM−1s−1 of transverse relaxivity (r2) was obtained in colloidal suspension. In addition, in vitro analysis in HeLa cells also showed an important effect in negative T2 contrast. Therefore, the results show that NP-FA can be a potential biomaterial for use in bio medical trials, especially as a contrast agent in magnetic resonance imaging (MRI).

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Butzbach, Kathrin, Matthias Konhäuser, Matthias Fach, Denise Bamberger, Benjamin Breitenbach, Bernd Epe et Peter Wich. « Receptor-mediated Uptake of Folic Acid-functionalized Dextran Nanoparticles for Applications in Photodynamic Therapy ». Polymers 11, n^o 5 (16 mai 2019) : 896. http://dx.doi.org/10.3390/polym11050896.

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In photodynamic therapy (PDT), photosensitizers and light are used to cause photochemically induced cell death. The selectivity and the effectiveness of the phototoxicity in cancer can be increased by a specific uptake of the photosensitizer into tumor cells. A promising target for this goal is the folic acid receptor α (FRα), which is overexpressed on the surface of many tumor cells and mediates an endocytotic uptake. Here, we describe a polysaccharide-based nanoparticle system suitable for targeted uptake and its photochemical and photobiological characterization. The photosensitizer 5, 10, 15, 20-tetraphenyl-21H, 23H-porphyrine (TPP) was encapsulated in spermine- and acetal-modified dextran (SpAcDex) nanoparticles and conjugated with folic acid (FA) on the surface [SpAcDex(TPP)-FA]. The particles are successfully taken up by human HeLa-KB cells, and a light-induced cytotoxicity is observable. An excess of free folate as the competitor for the FRα-mediated uptake inhibits the phototoxicity. In conclusion, folate-modified SpAcDex particles are a promising drug delivery system for a tumor cell targeted photodynamic therapy.

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Ortega-Muñoz, Mariano, Simona Plesselova, Angel V. Delgado, Francisco Santoyo-Gonzalez, Rafael Salto-Gonzalez, Maria Dolores Giron-Gonzalez, Guillermo R. Iglesias et Francisco Javier López-Jaramillo. « Poly(ethylene-imine)-Functionalized Magnetite Nanoparticles Derivatized with Folic Acid : Heating and Targeting Properties ». Polymers 13, n^o 10 (15 mai 2021) : 1599. http://dx.doi.org/10.3390/polym13101599.

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Magnetite nanoparticles (MNPs) coated by branched poly (ethylene-imine) (PEI) were synthesized in a one-pot. Three molecular weights of PEI were tested, namely, 1.8 kDa (sample MNP-1), 10 kDa (sample MNP-2), and 25 kDa (sample MNP-3). The MNP-1 particles were further functionalized with folic acid (FA) (sample MNP-4). The four types of particles were found to behave magnetically as superparamagnetic, with MNP-1 showing the highest magnetization saturation. The particles were evaluated as possible hyperthermia agents by subjecting them to magnetic fields of 12 kA/m strength and frequencies ranging between 115 and 175 kHz. MNP-1 released the maximum heating power, reaching 330 W/g at the highest frequency, in the high side of reported values for spherical MNPs. In vitro cell viability assays of MNP-1 and MNP-4 against three cell lines expressing different levels of FA receptors (FR), namely, HEK (low expression), and HeLa (high expression), and HepG2 (high expression), demonstrated that they are not cytotoxic. When the cells were incubated in the presence of a 175 kHz magnetic field, a significant reduction in cell viability and clone formation was obtained for the high expressing FR cells incubated with MNP-4, suggesting that MNP-4 particles are good candidates for magnetic field hyperthermia and active targeting.

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Prieto-Montero, Ruth, Alberto Katsumiti, Miren Pilare Cajaraville, Iñigo López-Arbeloa et Virginia Martínez-Martínez. « Functionalized Fluorescent Silica Nanoparticles for Bioimaging of Cancer Cells ». Sensors 20, n^o 19 (29 septembre 2020) : 5590. http://dx.doi.org/10.3390/s20195590.

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Functionalized fluorescent silica nanoparticles were designed and synthesized to selectively target cancer cells for bioimaging analysis. The synthesis method and characterization of functionalized fluorescent silica nanoparticles (50–60 nm), as well as internalization and subcellular localization in HeLa cells is reported here. The dye, rhodamine 101 (R101) was physically embedded during the sol–gel synthesis. The dye loading was optimized by varying the synthesis conditions (temperature and dye concentration added to the gel) and by the use of different organotriethoxysilanes as a second silica precursor. Additionally, R101, was also covalently bound to the functionalized external surface of the silica nanoparticles. The quantum yields of the dye-doped silica nanoparticles range from 0.25 to 0.50 and demonstrated an enhanced brightness of 230–260 fold respect to the free dye in solution. The shell of the nanoparticles was further decorated with PEG of 2000 Da and folic acid (FA) to ensure good stability in water and to enhance selectivity to cancer cells, respectively. In vitro assays with HeLa cells showed that fluorescent nanoparticles were internalized by cells accumulating exclusively into lysosomes. Quantitative analysis showed a significantly higher accumulation of FA functionalized fluorescent silica nanoparticles compared to nanoparticles without FA, proving that the former may represent good candidates for targeting cancer cells.

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Ghiarasim, Razvan, Natalia Simionescu, Adina Coroaba, Cristina M. Uritu, Narcisa Laura Marangoci, Sorin-Alexandru Ibanescu et Mariana Pinteala. « SI-ATRP Decoration of Magnetic Nanoparticles with PHEMA and Post-Polymerization Modification with Folic Acid for Tumor Cells’ Specific Targeting ». International Journal of Molecular Sciences 23, n^o 1 (23 décembre 2021) : 155. http://dx.doi.org/10.3390/ijms23010155.

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Targeted nanocarriers could reach new levels of drug delivery, bringing new tools for personalized medicine. It is known that cancer cells overexpress folate receptors on the cell surface compared to healthy cells, which could be used to create new nanocarriers with specific targeting moiety. In addition, magnetic nanoparticles can be guided under the influence of an external magnetic field in different areas of the body, allowing their precise localization. The main purpose of this paper was to decorate the surface of magnetic nanoparticles with poly(2-hydroxyethyl methacrylate) (PHEMA) by surface-initiated atomic transfer radical polymerization (SI-ATRP) followed by covalent bonding of folic acid to side groups of the polymer to create a high specificity magnetic nanocarrier with increased internalization capacity in tumor cells. The biocompatibility of the nanocarriers was demonstrated by testing them on the NHDF cell line and folate-dependent internalization capacity was tested on three tumor cell lines: MCF-7, HeLa and HepG2. It has also been shown that a higher concentration of folic acid covalently bound to the polymer leads to a higher internalization in tumor cells compared to healthy cells. Last but not least, magnetic resonance imaging was used to highlight the magnetic properties of the functionalized nanoparticles obtained.

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Xing, Jinjing, Yeqiang Cai, Yikun Wang, Haifu Zheng et Yujia Liu. « Synthesis of Polymer Assembled Mesoporous CaCO3 Nanoparticles for Molecular Targeting and pH-Responsive Controlled Drug Release ». Advances in Polymer Technology 2020 (5 janvier 2020) : 1–8. http://dx.doi.org/10.1155/2020/8749238.

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CaCO3 nanoparticles are very suitable as intelligent carriers because of their ideal biocompatibility and biodegradability, especially their sensitivity to pH. In this paper, we use mesoporous CaCO3 nanoparticles as intelligent carrier, sodium alginate, and chitosan as alternating assembly materials, folic acid as target molecules, and exploit layer-by-layer assembly technology to achieve sensitive molecular targeting and pH response drug release. Mesoporous CaCO3 hybrid nanoparticles have high drug loading on doxorubicin. The effects of different pH values on drug release in vitro were studied by regulating simulated body fluids with different pH values. The cytotoxicity, targeting effect, and drug release of human cervical cancer cell line (HeLa) were studied by cell vitality and imaging experiments. All the evidence suggests that the smart mesoporous CaCO3 nanoparticles may be a potential clinical application platform for cancer therapy.

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Ji, Zhen. « Synthesis and characterization of folic acid-conjugated human serum albumin (HSA) nanoparticles for isoalantolactone cellular uptake in HeLa ». African Journal of Pharmacy and Pharmacology 7, n^o 17 (8 mai 2013) : 1038–45. http://dx.doi.org/10.5897/ajpp12.723.

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Khlebtsov, Boris Nikolayevich, Andrey Mikhailovich Burov, Timofey Evgenevich Pylaev et Nikolai G. Khlebtsov. « Polydopamine-coated Au nanorods for targeted fluorescent cell imaging and photothermal therapy ». Beilstein Journal of Nanotechnology 10 (1 avril 2019) : 794–803. http://dx.doi.org/10.3762/bjnano.10.79.

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Au nanorods (AuNRs) have attracted a great interest as a platform for constructing various composite core/shell nanoparticles for theranostics applications. However, the development of robust methods for coating AuNRs with a biocompatible shell of high loading capacity and with functional groups still remains challenging. Here, we coated AuNRs with a polydopamine (PDA) shell and functionalized AuNR-PDA particles with folic acid and rhodamine 123 (R123) to fabricate AuNR-PDA-R123-folate nanocomposites. To the best of our knowledge, such AuNR-PDA-based composites combining fluorescent imaging and plasmonic phothothermal abilities have not been reported previously. The multifunctional nanoparticles were stable in cell buffer, nontoxic and suitable for targeted fluorescent imaging and photothermal therapy of cancer cells. We demonstrate the enhanced accumulation of folate-functionalized nanoparticles in folate-positive HeLa cells in contrast to the folate-negative HEK 293 cells using fluorescent microscopy. The replacement of folic acid with polyethylene glycol (PEG) leads to a decrease in nanoparticle uptake by both folate-positive and folate-negative cells. We performed NIR light-mediated targeted phototherapy using AuNR-PDA-R123-folate and obtained a remarkable cancer cell killing efficiency in vitro in comparison with only weak-efficient nontargeted PEGylated nanoparticles. Our work illustrates that AuNR-PDA could be a promising nanoplatform for multifunctional tumor theranostics in the future.

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Safdar, Muhammad Hassan, Humna Hasan, Mariam Anees et Zahid Hussain. « FOLIC ACID-CONJUGATED DOXORUBICIN-LOADED PHOTOSENSITIZING MANGANESE FERRITE NANOPARTICLES : SYNTHESIS, CHARACTERIZATION AND ANTICANCER ACTIVITY AGAINST HUMAN CERVICAL CARCINOMA CELL LINE (HELA) ». International Journal of Pharmacy and Pharmaceutical Sciences 9, n^o 5 (1 mai 2017) : 60. http://dx.doi.org/10.22159/ijpps.2017v9i5.17261.

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Objective: On account of several complications and adverse effects associated with the use of conventional chemotherapeutic regimen, the advanced drug-targeted therapies have gained the remarkable attention of the researchers due to their fabulous pharmaceutical and therapeutic advantages. The present study was designed with the aim to synthesize manganese ferrite nanoparticles (MnFe2O4 NPs) and folic acid-conjugated doxorubicin (DOX)-loaded manganese ferrite bovine serum albumin NPs (FA-BSA-DOX-MnFe2O4 NPs) using desolvation cross-linking method.Methods: Having assessed their physicochemical characteristics, the prepared NPs were evaluated for hem compatibility, photo-mediated cytotoxicity, and anti-cancer potential against human cervical carcinoma cell line (HeLa) using a range of in vitro assays which include hemolysis assay, sulforhodamine B (SRB) and MTT assays.Results: Spectroscopic characterization revealed that MnFe2O4 NPs were spherical with an average size diameter of approx. 15 nm and a band gap of 1.4 eV. Another remarkable feature of FA-BSA-DOX conjugated MnFe2O4 NPs was high entrapment efficiency (approx. 95%). MTT assay demonstrated that MnFe2O4 NPs revealed potential photosensitizing ability upon exposure to sunlight. FA-BSA-DOX conjugated MnFe2O4 NPs showed promising cytotoxicity against human cervical epithelial malignant carcinoma cell line (HeLa). Interestingly, the cytotoxicity of these NPs was gradually increased with time of exposure to sunlight.Conclusion: These findings suggested that FA-BSA-DOX conjugated MnFe2O4NPs exhibit promising photosensitizing and anticancer potential against human cervical carcinoma and thus can be considered as an alternative targeted therapy against human cervical cancer.

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Ranji-Burachaloo, Hadi, Qiang Fu, Paul A. Gurr, Dave E. Dunstan et Greg G. Qiao. « Improved Fenton Therapy Using Cancer Cell Hydrogen Peroxide ». Australian Journal of Chemistry 71, n^o 10 (2018) : 826. http://dx.doi.org/10.1071/ch18281.

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Fenton cancer therapy as a new methodology for the treatment of tumour cells is largely restricted owing to the low stability, high aggregation, and poor selectivity of reported nanoparticles. In this study, an improved approach for the selective destruction of cancer cells is reported. Metal–organic framework (MOF) nanoparticles were synthesized and reduced via a hydrothermal method, and then PEGylated through the surface-initiated atom transfer radical polymerization (SI-ATRP) reaction to produce a PEGylated reduced MOF (P@rMOF). The ratio of PEG to nanoparticles was used to optimize the size and aggregation of the nanoparticles, with 2P@rMOF (2 : 1 mass ratio) having the smallest hydrodynamic diameter. The nanoparticles were further conjugated with folic acid for cell targeting. In vitro cell uptake experiments demonstrated that the internalization of 2P@rMOF-FA nanoparticles into cancer cells (HeLa) was almost 3-fold that of normal cells (NIH-3T3). In the presence of 2P@rMOF-FA, the HeLa cell viability decreased dramatically to 22 %, whereas the NIH-3T3 cell viability remained higher than 80 % after 24 h incubation. The selectivity index for 2P@rMOF-FA is 4.48, which is significantly higher than those reported in the literature for similar strategies. This work thus demonstrates the most stable and selective nanoparticle system for the treatment of cancer cells using the cell’s own H2O2.

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Mazzotta, Elisabetta, Selene De Benedittis, Antonio Qualtieri et Rita Muzzalupo. « Actively Targeted and Redox Responsive Delivery of Anticancer Drug by Chitosan Nanoparticles ». Pharmaceutics 12, n^o 1 (26 décembre 2019) : 26. http://dx.doi.org/10.3390/pharmaceutics12010026.

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The clinical efficacy of methotrexate (MTX) is limited by its poor water solubility, its low bioavailability, and the development of resistance in cancer cells. Herein, we developed novel folate redox-responsive chitosan (FTC) nanoparticles for intracellular MTX delivery. l-Cysteine and folic acid molecules were selected to be covalently linked to chitosan in order to confer it redox responsiveness and active targeting of folate receptors (FRs). NPs based on these novel polymers could possess tumor specificity and a controlled drug release due to the overexpression of FRs and high concentration of reductive agents in the microenvironment of cancer cells. Nanoparticles (NPs) were prepared using an ionotropic gelation technique and characterized in terms of size, morphology, and loading capacity. In vitro drug release profiles exhibited a glutathione (GSH) dependence. In the normal physiological environment, NPs maintained good stability, whereas, in a reducing environment similar to tumor cells, the encapsulated MTX was promptly released. The anticancer activity of MTX-loaded FTC-NPs was also studied by incubating HeLa cells with formulations for various time and concentration intervals. A significant reduction in viability was observed in a dose- and time-dependent manner. In particular, FTC-NPs showed a better inhibition effect on HeLa cancer cell proliferation compared to non-target chitosan-based NPs used as control. The selective cellular uptake of FTC-NPs via FRs was evaluated and confirmed by fluorescence microscopy. Overall, the designed NPs provide an attractive strategy and potential platform for efficient intracellular anticancer drug delivery.

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Pichardo-Molina, Juan Luis, Ana Pamela Alejandra Andrade-Pérez, Jacqueline Torres-Ramírez, Juan Carlos Martínez-Espinosa, Julio Cesar Villagómez-Castro, José Pedro Castruita-Domínguez, Iván Salgado Tránsito et Lérida Liss Flores-Villavicencio. « Biological Impact of the Interaction of Functionalized and Bioconjugated Gold Nanoparticles of Different Sizes on HeLa and SH-SY5Y Human Cell Lines ». Journal of Nanomaterials 2022 (1 juin 2022) : 1–18. http://dx.doi.org/10.1155/2022/9711723.

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Nanotechnology opens new perspectives in many science and technology fields through new materials, such as metal nanoparticles. The biomedical field is one of these areas where nanoparticles offer promising application in the diagnosis and therapy of disease, generating biosensors for disease detection, bioimaging, and drug delivery. However, the controversy about whether nanoparticles are inert or exhibit different degrees of toxicity related to their physicochemical properties remains a subject of study and debate. This work shows how gold nanoparticles and nanorods were simultaneously functionalized with 4-aminothiophenol (4-ATP) and methoxypolyethylene glycol thiol (mPEG-SH). Then, folic acid (FA) gold nanoparticle bioconjugates caused diverse biological effects on HeLa and SH-SY5Y cell cultures after 24 h of incubation, when they were evaluated in the range of gold concentrations from 0.17 to 350 μM. We found notable changes in cell metabolic activity, viability, and biomass. 16 nm nanoparticles produced the most enhanced damage for functionalized (AuNPs) and bioconjugated (AuNPs-FA) nanoparticles, which we expected to be more biocompatible when coated with FA. Besides, epifluorescence images showed damage to F-actin microfilaments, adhesion and cell attachment loss, morphology changes (cells became round and detached), presence of blebs, and rupture of cell membrane. These results suggested that both AuNPs and AuNPs-FA have significant biological impact on HeLa and SH-SY5Y cell cultures, whereas gold nanorods showed significant changes only in the metabolic activity of SH-SY5Y cells when they were exposed to gold nanorods of 23 and 27 nm in length with a diameter of 5 nm, and crystal violet did not show evidence of toxicity.

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Razjouyan, Javad, Hamidreza Zolata, Omid Khayat, Fereidoun Nowshiravan, Nami Shadanpour et Meisam Mohammadnia. « Synthesis and evaluation of radiolabeled, folic acid-PEG conjugated, amino silane coated magnetic nanoparticles in tumor bearing Balb/C mice ». Nukleonika 60, n^o 3 (1 juillet 2015) : 497–502. http://dx.doi.org/10.1515/nuka-2015-0066.

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Abstract To design a potent agent for positron emission tomography/magnetic resonance imaging (PET/MRI) imaging and targeted magnetic hyperthermia-radioisotope cancer therapy radiolabeled surface modified superparamagnetic iron oxide nanoparticles (SPIONs) were used as nanocarriers. Folic acid was conjugated for increasing selective cellular binding and internalization through receptor-mediated endocytosis. SPIONs were synthesized by the thermal decomposition of tris (acetylacetonato) iron (III) to achieve narrow and uniform nanoparticles. To increase the biocompatibility of SPIONs, they were coated with (3-aminopropyl) triethoxysilane (APTES), and then conjugated with synthesized folic acid-polyethylene glycol (FA-PEG) through amine group of (3-aminopropyl) triethoxysilane. Finally, the particles were labeled with 64Cu (t1/2 = 12.7 h) using 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid mono (N-hydroxy succinimide ester) DOTA-NHS chelator. After the characterization of SPIONs, their cellular internalization was evaluated in folate receptor (FR) overexpressing KB (established from a HeLa cell contamination) and mouse fibroblast cell (MFB) lines. Eventually, active and passive targeting effects of complex were assessed in KB tumor-bearing Balb/C mice through biodistribution studies. Synthesized bare SPIONs had low toxicity effect on healthy cells, but surface modification increased their biocompatibility. Moreover, KB cells viability was reduced when using folate conjugated SPIONs due to FR-mediated endocytosis, while having little effect on healthy cells (MFB). Moreover, this radiotracer had tolerable in vivo characteristics and tumor uptake. In the receptor blocked case, tumor uptake was decreased, indicating FR-specific uptake in tumor tissue while enhanced permeability and retention effect was major mechanism for tumor uptake.

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Mbatha, Londiwe Simphiwe, Fiona Chepkoech Maiyo et Moganavelli Singh. « Dendrimer functionalized folate-targeted gold nanoparticles for luciferase gene silencing in vitro : A proof of principle study ». Acta Pharmaceutica 69, n^o 1 (1 mars 2019) : 49–61. http://dx.doi.org/10.2478/acph-2019-0008.

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Abstract Use of exogenous small interfering RNA (siRNA) has shown potential in gene silencing. The need for target-specific siRNA delivery vehicles is crucial to successful gene silencing. This study is aimed at developing and evaluating the safety and efficiency of siRNA delivery using unmodified and folic acid (FA) modified poly(amidoamine) generation 5 (PAMAM G5D) functionalized gold nanoparticles (Au:G5D/Au:G5D:FA) in vitro. All formulations were physico--chemically characterized and nanocomplexes were evaluated using the band shift, dye displacement, nuclease protection, MTT cell viability, and luciferase reporter gene assays. Nanocomplexes bound and protected siRNA against degrading RNases, and were well tolerated by the cells. The Au:G5D:FA nanocomplexes elicited excellent gene silencing in folate receptor expressing HeLa-Tat-Luc cells, decreasing significantly in the presence of excess FA ligand, indicating nanocomplex uptake by the mechanism of receptor mediation. These results highlight the synergistic role played by Au and the dendrimer in enhancement of transgene silencing.

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Prieto-Montero, Ruth, Alejandro Prieto-Castañeda, Alberto Katsumiti, Miren P. Cajaraville, Antonia R. Agarrabeitia, María J. Ortiz et Virginia Martínez-Martínez. « Functionalization of Photosensitized Silica Nanoparticles for Advanced Photodynamic Therapy of Cancer ». International Journal of Molecular Sciences 22, n^o 12 (21 juin 2021) : 6618. http://dx.doi.org/10.3390/ijms22126618.

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BODIPY dyes have recently attracted attention as potential photosensitizers. In this work, commercial and novel photosensitizers (PSs) based on BODIPY chromophores (haloBODIPYs and orthogonal dimers strategically designed with intense bands in the blue, green or red region of the visible spectra and high singlet oxygen production) were covalently linked to mesoporous silica nanoparticles (MSNs) further functionalized with PEG and folic acid (FA). MSNs approximately 50 nm in size with different functional groups were synthesized to allow multiple alternatives of PS-PEG-FA decoration of their external surface. Different combinations varying the type of PS (commercial Rose Bengal, Thionine and Chlorine e6 or custom-made BODIPY-based), the linkage design, and the length of PEG are detailed. All the nanosystems were physicochemically characterized (morphology, diameter, size distribution and PS loaded amount) and photophysically studied (absorption capacity, fluorescence efficiency, and singlet oxygen production) in suspension. For the most promising PS-PEG-FA silica nanoplatforms, the biocompatibility in dark conditions and the phototoxicity under suitable irradiation wavelengths (blue, green, or red) at regulated light doses (10–15 J/cm2) were compared with PSs free in solution in HeLa cells in vitro.

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Lodhi, Madeeha Shahzad, Fatima Khalid, Muhammad Tahir Khan, Zahoor Qadir Samra, Shabbir Muhammad, Yu-Juan Zhang et Kejie Mou. « A Novel Method of Magnetic Nanoparticles Functionalized with Anti-Folate Receptor Antibody and Methotrexate for Antibody Mediated Targeted Drug Delivery ». Molecules 27, n^o 1 (1 janvier 2022) : 261. http://dx.doi.org/10.3390/molecules27010261.

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Therapeutic effects of anticancer medicines can be improved by targeting the specific receptors on cancer cells. Folate receptor (FR) targeting with antibody (Ab) is an effective tool to deliver anticancer drugs to the cancer cell. In this research project, a novel formulation of targeting drug delivery was designed, and its anticancer effects were analyzed. Folic acid-conjugated magnetic nanoparticles (MNPs) were used for the purification of folate receptors through a novel magnetic affinity purification method. Antibodies against the folate receptors and methotrexate (MTX) were developed and characterized with enzyme-linked immunosorbent assay and Western blot. Targeting nanomedicines (MNP-MTX-FR Ab) were synthesized by engineering the MNP with methotrexate and anti-folate receptor antibody (anti-FR Ab). The cytotoxicity of nanomedicines on HeLa cells was analyzed by calculating the % age cell viability. A fluorescent study was performed with HeLa cells and tumor tissue sections to analyze the binding efficacy and intracellular tracking of synthesized nanomedicines. MNP-MTX-FR Ab demonstrated good cytotoxicity along all the nanocomposites, which confirms that the antibody-coated medicine possesses the potential affinity to destroy cancer cells in the targeted drug delivery process. Immunohistochemical approaches and fluorescent study further confirmed their uptake by FRs on the tumor cells’ surface in antibody-mediated endocytosis. The current approach is a useful addition to targeted drug delivery for better management of cancer therapy along with immunotherapy in the future.

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Chavez, Dalia Holanda, Karla Juarez-Moreno et Gustavo Alonso Hirata. « Aminosilane Functionalization and Cytotoxicity Effects of Upconversion Nanoparticles Y2O3 and Gd2O3 Co-Doped with Yb3+and Er3+ ». Nanobiomedicine 3 (1 janvier 2016) : 1. http://dx.doi.org/10.5772/62252.

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In this study, luminescent upconversion nanoparticles (UCNPs) Y2O3 and Gd2O3 co-doped with Yb3+ and Er3+ were prepared by the sol-gel method (SG). These NPs are able to absorb near infrared photons and upconvert them into visible radiation with a direct application in bioimaging, as an important tool to diagnose and visualize cancer cells. The UCNPs were coated with a thin silica shell and functionalized with amino groups for further folic acid conjugation to allow their interaction with folate ligands on the cell surface. Their physical properties were analysed by Transmission Electron Microscopy (TEM), Fourier transform infrared spectroscopy (FTIR) and photoluminescence (PL) measurements. The PL results revealed excellent luminescence properties on all core-shell UCNPs. Cytotoxicity experiments with concentrations of bare and aminosilane coated/functionalized UCNPs between 0.001 μg/mL to 1 μg/mL were tested on two different cell lines from human cervix carcinoma (HeLa) and human colorectal adenocarcinoma (DLD-1) with a colorimetric assay based on the reduction of MTT reagent (methy-134-thiazolyltetrazolium). The assays show that some concentrations of bare UCNPs were cytotoxic for cervical adenocarcinoma cells (HeLa); however, for human colorectal adenocarcinoma all UCNPs are non-cytotoxic. After UCNPs functionalization with silica-aminosilane (APTES/TEOS), all of the nanoparticles tested were found to be non-cytotoxic for both cell lines. The UCNPs functionalized in this work can be further conjugated with specific ligands and used as biolabels for detection of cancer cells.

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Pillay, Nikita Simone, Aliscia Daniels et Moganavelli Singh. « Folate-Targeted Transgenic Activity of Dendrimer Functionalized Selenium Nanoparticles In Vitro ». International Journal of Molecular Sciences 21, n^o 19 (29 septembre 2020) : 7177. http://dx.doi.org/10.3390/ijms21197177.

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Current chemotherapeutic drugs, although effective, lack cell-specific targeting, instigate adverse side effects in healthy tissue, exhibit unfavourable bio-circulation and can generate drug-resistant cancers. The synergistic use of nanotechnology and gene therapy, using nanoparticles (NPs) for therapeutic gene delivery to cancer cells is hereby proposed. This includes the benefit of cell-specific targeting and exploitation of receptors overexpressed in specific cancer types. The aim of this study was to formulate dendrimer-functionalized selenium nanoparticles (PAMAM-SeNPs) containing the targeting moiety, folic acid (FA), for delivery of pCMV-Luc-DNA (pDNA) in vitro. These NPs and their gene-loaded nanocomplexes were physicochemically and morphologically characterized. Nucleic acid-binding, compaction and pDNA protection were assessed, followed by cell-based in vitro cytotoxicity, transgene expression and apoptotic assays. Nanocomplexes possessed favourable sizes (<150 nm) and ζ-potentials (>25 mV), crucial for cellular interaction, and protected the pDNA from degradation in an in vivo simulation. PAMAM-SeNP nanocomplexes exhibited higher cell viability (>85%) compared to selenium-free nanocomplexes (approximately 75%), confirming the important role of selenium in these nanocomplexes. FA-conjugated PAMAM-SeNPs displayed higher overall transgene expression (HeLa cells) compared to their non-targeting counterparts, suggesting enhanced receptor-mediated cellular uptake. Overall, our results bode well for the use of these nano-delivery vehicles in future in vivo studies.

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Lebret, Valérie, Laurence Raehm, Jean-Olivier Durand, Monique Smaïhi, Martinus H. V. Werts, Mireille Blanchard-Desce, Delphine Méthy-Gonnod et Catherine Dubernet. « Surface functionalization of two-photon dye-doped mesoporous silica nanoparticles with folic acid : cytotoxicity studies with HeLa and MCF-7 cancer cells ». Journal of Sol-Gel Science and Technology 48, n^o 1-2 (19 mars 2008) : 32–39. http://dx.doi.org/10.1007/s10971-008-1724-1.

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Huang, Ming, Lijun Wang, Xiaojuan Zhang, Jin Zhou, Lihua Liu, Yuefang Pan, Bin Yu et Zhangsen Yu. « Synthesis and Characterization of Folic Acid Labeled Upconversion Fluorescent Nanoprobes for in vitro Cancer Cells Targeted Imaging ». Nano 12, n^o 05 (15 mars 2017) : 1750057. http://dx.doi.org/10.1142/s1793292017500576.

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Upconversion nanoparticles (UCNPs) are widely used in the field of biomedicine, such as biosensing, cell labeling and medical multimodal imaging because of their unique optical properties. In this paper, we demonstrated the synthesis of polyethylenimine-modified NaLuF4:Yb,Er ([Formula: see text], Yb[Formula: see text], Er[Formula: see text] UCNPs in three different solvents, such as water, ethylene glycol and diethylene glycol. The as-prepared UCNPs were characterized and the experimental results showed that the UCNPs synthesized in ethylene glycol had excellent properties. The obtained UCNPs in ethylene glycol had the smallest particle size and uniform size distribution, and the pure cubic phase of crystallization and Dynamic light scattering and particle dispersion index (DLS/Pdi) were the smallest. What’s more, the upconversion fluorescence intensity was 7 and 52 times greater than that of UCNPs synthesized in diethylene glycol and water, respectively. In addition, the factors of reaction solvent that had an impact on the particle size, morphology, crystalline phase, DLS and upconversion fluorescence intensity of the synthesized UCNPs were discussed. Moreover, in order to obtain the targeted nanoprobe, we used an EDC/NHS covalent coupling method to modify folic acid to the NaLuF4:Yb,Er/PEI UCNP surface. The NaLuF4:Yb,Er/PEI–FA upconversion fluorescent nanoprobes had low cytotoxicity and were suitable for the application in HeLa cells targeted fluorescent imaging.

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Maiyo, Fiona, et Moganavelli Singh. « Polymerized Selenium Nanoparticles for Folate-Receptor-Targeted Delivery of Anti-Luc-siRNA : Potential for Gene Silencing ». Biomedicines 8, n^o 4 (5 avril 2020) : 76. http://dx.doi.org/10.3390/biomedicines8040076.

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The development of a biocompatible and nontoxic gene delivery vehicle remains a challenging task. Selenium nanoparticles (SeNPs) have the potential to increase delivery efficiency, to reduce side effects, and to improve therapeutic outcomes. In this study, chitosan (Ch) functionalized folate (FA)-targeted SeNPs were synthesized, characterized, and evaluated for their potential to bind, protect, and safely deliver Fluc-siRNA in vitro. SeNPs of less than 100 nm were successfully synthesised and further confirmed using UV-vis and Fourier transform infrared spectroscopy, transmission electron microscopy, and nanoparticle tracking analysis. Cell viability studies were conducted in vitro in selected cancer and non-cancer cell lines. Folate receptor (FOLR1) targeted and nontargeted luciferase gene silencing studies were assessed in the transformed Hela-tat-Luc cell line expressing the luciferase gene. Targeted and nontargeted SeNP nanocomplexes showed minimal toxicity in all cell lines at selected w/w ratios. Maximum gene silencing was achieved at optimum w/w ratios for both nanocomplexes, with Selenium-chitosan-folic acid (SeChFA) nanocomplexes showing slightly better transgene silencing, as supported by results from docking studies showing that SeChFA nanocomplexes interacted strongly with the folate receptor (FOLR1) with high binding energy of −4.4 kcal mol−1.

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Fatima, Mehreen, Anadil Noel, Zeeshan Abdullah, Kainat Bibi, Shumaila Yousaf, Muhammad Nouman Aziz, Muhammad Farhan Zafar Chaudhry et al. « Therapeutic and Diagnostic Analysis of Cadmium Sulfide Quantum Dots Conjugated with Cysteine, Anticancer Drug and Folate ». Pakistan Journal of Medical and Health Sciences 16, n^o 9 (30 septembre 2022) : 408–12. http://dx.doi.org/10.53350/pjmhs22169408.

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Background: Nanotechnology is evolving in the field of cancer drug design and cancer therapy. The ultrafine nanoparticles that have a size range of 1-10nm are called Quantum Dots. The ability to fluorescence has deemed quantum dots as suitable candidate for diagnostic imaging. Upon proper structural arrangement these quantum dots can be engineered to detect specifically cancer cells and deliver anticancer agents to the targeted site for cancer cell apoptosis. Aim: Cadmium sulfide (CdS) nanoparticles conjugated with cysteine were prepared by wet method under high temperature and pressure Methods: Folic acid receptor has shown overexpression in multiple types of cancers therefore the binding of folate to the composite ensures that only the cancer cells are targeted and normal cells remain unaffected. HeLa cells were opted to check the composite activity. Results: Composite showed 23% cell death in the first 2 hours of delivery. FTIR analysis confirmed conjugation of CdS with cysteine and further conjugation of dacarbazine and folate to cysteine. The molecules of folic acid attached to cysteine could be measured to be 2.545× 1018 molecules which were attached to 0.996× 〖10〗^22 molecules of cysteine that were attached 1.66 x〖 10〗^(20 ) molecules of CdS. Similarly, 2.3103 × 1019 of doxorubicin were attached to 0.996× 〖10〗^22 molecules of of cysteine attached to 1.66 x〖 10〗^(20 ) molecules of CdS. Furthermore, the cytotoxic nature of Cadmium Sulfide also gives an advantage two way cancer cell death. Conclusion: Quantum dots attached to specific ligands that bind to cancer antigens, antibodies, proteins, Receptors etc. can be used for effective diagnosis of cancer. They can act as probe and detect thousands of molecules simultaneously by using only a small quantity of nanoComposite. Keywords: Cadmium sulfide, Cancer, Quantum dots, Dacarbazine

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Martínez-Relimpio, Ana María, Marta Benito, Elena Pérez-Izquierdo, César Teijón, Rosa María Olmo et María Dolores Blanco. « Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization ». Polymers 13, n^o 13 (24 juin 2021) : 2083. http://dx.doi.org/10.3390/polym13132083.

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Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform of the folate receptor (FR) is overexpressed on a significant number of human cancers; therefore, folate-targeted crosslinked nanoparticles based on BSA and alginate mixtures and loaded with paclitaxel (PTX) have been prepared to maximize the proven antineoplastic activity of the drug against solid tumors. Nanometric-range-sized particles (169 ± 28 nm–296 ± 57 nm), with negative Z-potential values (between −0.12 ± 0.04 and −94.1± 0.4), were synthesized, and the loaded PTX (2.63 ± 0.19–3.56 ±0.13 µg PTX/mg Np) was sustainably released for 23 and 27 h. Three cell lines (MCF-7, MDA-MB-231 and HeLa) were selected to test the efficacy of the folate-targeted PTX-loaded BSA/ALG nanocarriers. The presence of FR on the cell membrane led to a significantly larger uptake of BSA/ALG–Fol nanoparticles compared with the equivalent nanoparticles without folic acid on their surface. The cell viability results demonstrated a cytocompatibility of unloaded nanoparticle–Fol and a gradual decrease in cell viability after treatment with PTX-loaded nanoparticle–Fol due to the sustainable PTX release.

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Chávez-García, D., K. Juárez-Moreno et G. A. Hirata. « Upconversion Nanoparticles Y2O3 and Gd2O3 Co-Doped with Er3+ and Yb3+ with Aminosilane-Folic Acid Functionalization for Breast and Cervix Cancer Cells Detection ». MRS Advances 2, n^o 52 (2017) : 2983–88. http://dx.doi.org/10.1557/adv.2017.447.

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ABSTRACTThe upconversion nanoparticles (UCNPs) possess the ability to absorb near infrared energy (980 nm) and upconvert it to emit in the visible spectra. In this research, the UNCPs emit in red (660 nm) due to the electronic transitions between two rare earth ions: Er3+ and Yb3+, this process is called energy transfer upconversion (ETU). The UCNPs were functionalized with aminosilanes and folic acid receptors (UCNP-FR) and analyzed by transmission electron microscopy, Fourier transform infrared spectroscopy and luminescence measurements. UCNPs-FR of Y2O3 have a particle size of 70 ± 10 nm and the Gd2O3 have a 50 ± 10 nm particle size. Both showed a good luminescence spectrum in comparison with the bare ones. Cytotoxicity of different amounts between 0.001 µg/ml to 1 µg/ml of bare and functionalized UCNPs was measured with the colorimetric assay MTT in three cancer cell lines: human cervical adenocarcinoma (HeLa), human breast cancer cells MB-MDA-231. Some concentrations of bare UCNPs were cytotoxic for cancer cells; however after their functionalization they resulted to be non-cytotoxic. The functionalized UCNPs were able to bind to folate receptors which are overexpressed in cervical and breast cancers cells. It was demonstrated by confocal microscopy, that the functionalized UCNPs were internalized into the cancer cells, confirming that they can be used as biolabels for breast and cervical cancer cells.

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Bertel Garay, Linda, Fernando Martínez Ortega et Stelia Carolina Méndez-Sanchez. « Use in vitro of Gold Nanoparticles Functionalized with Folic Acid as a Photothermal Agent on Treatment of HeLa Cells ». Journal of the Mexican Chemical Society 62, n^o 1 (21 mai 2018). http://dx.doi.org/10.29356/jmcs.v62i1.385.

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<p>Folic acid (FA) is used as a recognition molecule to achieve selective internalization in cancer cells. Here functionalized gold nanoparticles with folic acid (AuNP-FA) are proposed as suitable therapeutic agents for cervix cancer cells by photothermal damage. The functionalized gold nanoparticles with folic acid were synthesized by mixing hydrogen tetrachloroaurate with folic acid in a molar ratio of 0.56/1 under radiation of mercury lamp (λ<sub>max</sub>=254 nm). HeLa cells were incubated with AuNP-FA during 48 h, then were irradiated and the cytotoxicity was analyzed 12 h after irradiation. The AuNP-FA were dose-dependent cytotoxic under irradiation and not cytotoxic in the absence of radiation. The viability of cancer cells treated with functionalized and non-functionalized gold nanoparticles (AuNPs), with and without near infrared light at 808 nm, was measured by MTT assays. This work provides useful guidance toward the synthesis of biocompatible nanomaterials for biological applications.</p>

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PUTRI, DARA A., SUTRIYO SUTRIYO et FADLINA C. SAPUTRI. « CELLULAR UPTAKE STUDY AND CYTOTOXICITY STUDY OF RESVERATROL-GOLD-PEG-FOLATE (RSV-AU-PEG-FA) NANOPARTICLES ON HELA HUMAN CERVICAL CANCER CELL LINE ». International Journal of Applied Pharmaceutics, 14 mai 2020, 113–18. http://dx.doi.org/10.22159/ijap.2020v12i4.37307.

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Objective: This study aimed to evaluate the effectivity of resveratrol-gold-PEG-folate (RSV-Au-PEG-FA) nanoparticles formulation in resveratrol (RSV) targeted delivery and cytotoxicity effect on HeLa human cervical cancer cell line. Methods: Gold nanoparticles (AuNP) were used as carriers and folic acid (FA) was used as active targeting moiety, using polyethylene glycol-bis-amine (PEG-bis-amine) as linker. RSV-Au-PEG-FA nanoparticles were characterized by UV-Vis spectrophotometry, infrared spectroscopy, particle size analyzer (PSA), and transmission electron microscopy (TEM). Cellular uptake study was conducted by using fluorescence microscope. Cytotoxicity study was conducted by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results: Cellular uptake study has shown that RSV-Au-PEG-FA nanoparticles are potential to be accumulated intracellularly in HeLa cells more than in Vero cells. Cytotoxicity study has shown RSV-Au-PEG-FA nanoparticles IC50 67.06±2.14 mM and RSV IC50 9.66±1.44 mM on HeLa cells Conclusion: RSV-Au-PEG-FA nanoparticles are potential to enhance RSV uptake by HeLa cells selectively.

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Singh, Harjit, Bharat Khurana, Daisy Arora et Sukhbir Kaur. « Formulation, Optimization and in vitro / in vivo characterization of Spray Dried Doxorubicin Loaded Folic Acid Conjugated Gelatin Nanoparticles ». Current Molecular Pharmacology 13 (5 mai 2020). http://dx.doi.org/10.2174/1874467213666200505095143.

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Purpose: Formulation, optimization and anticancer activity of spray-dried Doxorubicin loaded folic acid conjugated Gelatin nanoparticles (DOX-FA-GN). Method: Doxorubicin loaded gelatin nanoparticles (DOX-GN) were prepared by the Coacervation phase separation method, optimized using DoE and then conjugated with folic acid by covalent coupling to formulate Doxorubicin loaded folic acid conjugated nanoparticles (DOX-FA-GN). The formulated nanoparticles were characterized to evaluate its physicochemical properties. Cellular uptake and cell viability studies were carried out using MTT assay and biodistribution studies were carried out in Wistar rats. Result: Particle size, PDI and entrapment efficiency for optimized DOX-GN was found to be 152.3 ± 9.3 nm 0.294 ± 0.1 and 86.9± 3.4 % while for DOX-FA-GN, 193.9 ± 12.3 nm 0.247 ± 0.2 and 84 ± 3.6 %. The cytotoxic studies showed a cell viability of 75.1% for DOX-GN and 29.5 % DOX-FA-GN. Biodistribution studies found to be statistically insignificant for conjugated nanoparticles with excellent flow properties. Significantly higher DOX distribution in the lungs was observed in the case of DOX-FA-GN. Conclusions: There was a higher uptake of DOX on HeLa cells with DOX-FA-GN compared to DOX-GN. Also, the biodistribution of Dox in the lungs of Wistar rats was higher in conjugated nanoparticles as compared to unconjugated nanoparticles.

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Veerappan, Radhini, Aliscia Daniels et Moganavelli Singh. « Polymeric Silver Nanoparticles : Potential for Folate-Targeted Delivery of Cisplatin In Vitro ». International Journal of Nanoscience 20, n^o 05 (octobre 2021). http://dx.doi.org/10.1142/s0219581x21500411.

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Nanotechnology is a favorable avenue for improving therapeutic strategies, especially in cancer therapy. The harmful side effects of traditional cancer therapy impact dramatically on the patient’s quality of life. Cisplatin, a commonly used anticancer drug, is implicated in side effects such as neurotoxicity, nephrotoxicity and reduced blood cell count. Silver nanoparticles (AgNPs) have been investigated for their antibacterial effects and their anticancer activities to a lesser extent. Their capability as drug delivery vehicles has not been fully exploited, primarily due to their inconclusive cytotoxicity observed in healthy tissues. This study aimed to synthesize and characterize nanoparticles (NPs), consisting of Ag, chitosan (Cs) and folic acid (FA) (CsAg and FACsAg), loading them with cisplatin (C) (C-CsAg and C-FACsAg) and comparing their anticancer activities in the human embryonic kidney (HEK293), breast adenocarcinoma (MCF-7) and cervical carcinoma (HeLa) cells. All NPs and drug nanocomplexes were morphologically and physicochemically characterized, revealing NPs and nanocomplexes of favorable sizes ([Formula: see text][Formula: see text]nm), polydispersity and stability. The drug encapsulation efficiencies for C-CsAg and C-FACsAg were 50% and 72%, respectively, while drug release studies indicated that cisplatin release was pH dependent. The C-FACsAg nanocomplexes produced greater anticancer activity than C-CsAg. Folate receptor-mediated uptake was confirmed for the C-FACsAg nanocomplexes in the receptor-rich HeLa cells boding well for future in vivo research.

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Zhao, Shuai, Shan Sun, Kai Jiang, Yuhui Wang, Yu Liu, Song Wu, Zhongjun Li, Qinghai Shu et Hengwei Lin. « In Situ Synthesis of Fluorescent Mesoporous Silica–Carbon Dot Nanohybrids Featuring Folate Receptor-Overexpressing Cancer Cell Targeting and Drug Delivery ». Nano-Micro Letters 11, n^o 1 (5 avril 2019). http://dx.doi.org/10.1007/s40820-019-0263-3.

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Abstract Multifunctional nanocarrier-based theranostics is supposed to overcome some key problems in cancer treatment. In this work, a novel method for the preparation of a fluorescent mesoporous silica–carbon dot nanohybrid was developed. Carbon dots (CDs), from folic acid as the raw material, were prepared in situ and anchored on the surface of amino-modified mesoporous silica nanoparticles (MSNs–NH2) via a microwave-assisted solvothermal reaction. The as-prepared nanohybrid (designated MSNs–CDs) not only exhibited strong and stable yellow emission but also preserved the unique features of MSNs (e.g., mesoporous structure, large specific surface area, and good biocompatibility), demonstrating a potential capability for fluorescence imaging-guided drug delivery. More interestingly, the MSNs–CDs nanohybrid was able to selectively target folate receptor-overexpressing cancer cells (e.g., HeLa), indicating that folic acid still retained its function even after undergoing the solvothermal reaction. Benefited by these excellent properties, the fluorescent MSNs–CDs nanohybrid can be employed as a fluorescence-guided nanocarrier for the targeted delivery of anticancer drugs (e.g., doxorubicin), thereby enhancing chemotherapeutic efficacy and reducing side effects. Our studies may provide a facile strategy for the fabrication of multifunctional MSN-based theranostic platforms, which is beneficial in the diagnosis and therapy of cancers in future.

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Chávez, D., K. Juárez-Moreno et G. A. Hirata. « Silica coated, aminosilane functionalization, upconversion emission and cytotoxicity in cancer cell lines of the nanoparticles Y2O3 and Gd2O3 co-doped with Yb3+ and Er3+ ». MRS Proceedings 1817 (2016). http://dx.doi.org/10.1557/opl.2016.44.

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ABSTRACTY2O3 and Gd2O3 upconversion nanoparticles (UCN) co-doped with Yb3+ and Er3+ can absorb and upconvert near infrared (NIR) radiation into visible light. These UCN find application in bioimaging, as an important tool to diagnose and visualize cancer cells. The UCN can be used as biolabels to identify the cells; the nanoparticles can be coated and functionalized with ligands that bind to receptors on the surface of the cell. In this project, the UCN were synthesized by sol-gel method and subsequently coated with a thin silica shell by using the Stöber method. The core-shell UCN were functionalized with amine group to enable folic acid conjugation. The functionalized core-shell nanoparticles were analyzed by transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), and luminescence measurements. Concentrations of bare and coated/functionalized UCN between 0.001 µg/mL and 1 µg/mL were tested on two different cell lines from human cervix carcinoma (HeLa) and human colorectal adenocarcinoma (DLD-)1 with colorimetric assay based on the MTT reagent (methy-134 thiazolyltetrazolium). The results show good luminescence spectra on all core-shell UCN. The MTT assays show that some concentrations of bare UCN of Y2O3: Er, Yb (1%, 1% mol) and Gd2O3 were cytotoxic for cervical adenocarcinoma cells (HeLa). For human colorectal adenocarcinoma all UCN are non-cytotoxic. The UCN with silica-aminosilane functionalization (APTS/TEOS) were non-cytotoxic on both cell lines.

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Pinilla, Ana María, Diana Blach, Stelia Carolina Mendez et Fernando Martínez Ortega. « AOT direct and reverse micelles as a reaction media for anisotropic silver nanoparticles functionalized with folic acid as a photothermal agent on HeLa cells ». SN Applied Sciences 1, n^o 8 (15 juillet 2019). http://dx.doi.org/10.1007/s42452-019-0894-5.

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Luo, Wenli, Zhaojian Li, Ling Zhang et Xingyi Xie. « Polyethylenimine-CO2 adduct templated CaCO3 nanoparticles as anticancer drug carrier ». Cancer Nanotechnology 14, n^o 1 (4 février 2023). http://dx.doi.org/10.1186/s12645-023-00156-z.

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Abstract Background Due to their porous structure and capability to degrade under acidic conditions, CaCO3 nanoparticles in vaterite form can be used as carriers to effectively deliver drugs to low-pH sites such as tumors. The usually used intravenous administration requires long-term vaterite phase and colloidal stability for storage and blood circulation. While passive accumulation in tumors can be achieved via the enhanced permeation and retention effect, active accumulation requires reactive groups on vaterite nanoparticles to conjugate targeting molecules. Both requirements are hard to achieve in one simple and economical vaterite formulation. Herein, we used polyethylenimine (PEI)-based CO2 adduct as both a CO2 source and a template for vaterite mineralization to generate PEI-CO2@CaCO3 colloidal particles, with reactive amino groups from the PEI template. Results The obtained nanoparticles with a hydrodynamic diameter of 200–300 nm have a vaterite phase and colloidal stability in an aqueous solution for over 8 months. These nanoparticles could effectively load anticancer drug doxorubicin via coprecipitation and be surface-modified with polyethylene glycol (PEG) and folic acid for long-term blood circulation and tumor targeting purposes, respectively. After being endocytosed, the PEI-CO2 adduct accelerates the dissolution of drug-loaded nanoparticles to generate CO2 bubbles to break the lysosomes, leading to rapid doxorubicin delivery inside tumor cells. The degradation of PEI-CO2 in the CaCO3 nanoparticles could also release PEI and CO2 and may contribute to the disruption of normal cellular functions. As a result, the drug-loaded PEI-CO2@CaCO3 nanoparticles strongly suppressed tumor growth in mice with HeLa tumor xenografts. Conclusions A new and effective vaterite drug carrier for anticancer therapy has been developed using PEI-CO2 adduct as both a CO2 source and vaterite template for CaCO3 mineralization. This delivery system illustrates an application of CO2 generation materials in drug delivery and has the potential for further development.

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