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Leaist, DG. "Concentration Oscillations During Diffusion With Slow First-Order Chemical Reaction in Aqueous Solutions of trans-Dichloro-bis(ethane-1,2-diamine)cobalt(III) Chloride, trans-[Co(en)2Cl2]Cl". Australian Journal of Chemistry 41, nr 4 (1988): 469. http://dx.doi.org/10.1071/ch9880469.
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The rate equations for diffusion and chemical reaction have been solved for isothermal diffusion with the first-order reactionA → Bin stirred diaphragm cells. Provided pseudo-steady-state conditions are established in the diaphragms, the concentration differences across the diaphragm for the reactant and product are predicted to show damped oscillations in time for certain values of the solute diffusivities. Diffusion coefficients have been determined for aqueous solutions of trans-dichlorobis (ethane-1,2-diamine)cobalt(III) chloride in which the 1 : 1 salt slowly converts into a 1:2 salt through the reaction [Co(en)2Cl2]+ + Cl - → [Co(en)2Cl]2+ +2Cl- with k = 3.6×10-5 s-1 at 25°C. Supplementary ternary diffusion coefficients have been determined for aqueous solutions of potassium acetate + potassium sulfate, a ternary mixed electrolyte with ionic mobilities similar to those of the aqueous cobalt salts.
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Esakkiraja, Neelamegan, Keerti Pandey, Anuj Dash i Aloke Paul. "Pseudo-binary and pseudo-ternary diffusion couple methods for estimation of the diffusion coefficients in multicomponent systems and high entropy alloys". Philosophical Magazine 99, nr 18 (25.05.2019): 2236–64. http://dx.doi.org/10.1080/14786435.2019.1619027.
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Esakkiraja, Neelamegan, i Aloke Paul. "A novel concept of pseudo ternary diffusion couple for the estimation of diffusion coefficients in multicomponent systems". Scripta Materialia 147 (kwiecień 2018): 79–82. http://dx.doi.org/10.1016/j.scriptamat.2018.01.002.
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Leaist, Derek G., i Robert A. Noulty. "An eigenvalue method for determination of multicomponent diffusion coefficients. Application to NaOH + NaCl + H2O mixtures". Canadian Journal of Chemistry 63, nr 2 (1.02.1985): 476–82. http://dx.doi.org/10.1139/v85-077.
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A general method for the determination of multicomponent diffusion coefficients is developed using the algebraic technique of matrix diagonalization. When linear combinations of measurements from several multicomponent diffusion experiments performed with different initial concentration gradients (but with the same final composition) are analyzed as simple binary data, particular combinations may be found that transform the multicomponent diffusion coefficient matrix D to diagonal form and thus yield time-invariant, pseudo-binary diffusion coefficients: the eigenvalues of D. Since the matrix that diagonalizes D is given by the coefficients used to form the linear combinations, D is easily recovered by the inverse transformation. The advantages of the eigenvalue method are briefly discussed. For testing purposes, ternary diffusion coefficients are determined from conductance measurements for dilute aqueous NaOH + NaCl mixtures. Diffusion of NaOH in aqueous NaCl is significantly more rapid than in pure water, and large coupled flows of NaCl are observed. The results are in close agreement with behavior predicted by Onsager–Fuoss theory.
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Barros, Marisa C. F., Ana C. F. Ribeiro, Luís M. P. Verissimo, Derek G. Leaist i Miguel A. Esteso. "Diffusion in ternary aqueous {L-dopa + (NaSO3) -β-cyclodextrin} solutions using the pseudo-binary approximation". Journal of Chemical Thermodynamics 123 (sierpień 2018): 17–21. http://dx.doi.org/10.1016/j.jct.2018.03.014.
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Al Saqr, Ahmed, Manjusha Annaji, Ishwor Poudel, Mohammed F. Aldawsari, Hamad Alrbyawi, Nur Mita, Muralikrishnan Dhanasekaran i in. "Topical Delivery of Diacetyl Boldine in a Microemulsion Formulation for Chemoprotection against Melanoma". Pharmaceutics 15, nr 3 (10.03.2023): 901. http://dx.doi.org/10.3390/pharmaceutics15030901.
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This study aimed to develop a microemulsion formulation for topical delivery of Diacetyl Boldine (DAB) and to evaluate its cytotoxicity against melanoma cell line (B16BL6) in vitro. Using a pseudo-ternary phase diagram, the optimal microemulsion formulation region was identified, and its particle size, viscosity, pH, and in vitro release characteristics were determined. Permeation studies were performed on excised human skin using Franz diffusion cell assembly. The cytotoxicity of the formulations on B16BL6 melanoma cell lines was evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) assay. Two formulation compositions were selected based on the higher microemulsion area of the pseudo-ternary phase diagrams. The formulations showed a mean globule size of around 50 nm and a polydispersity index of <0.2. The ex vivo skin permeation study demonstrated that the microemulsion formulation exhibited significantly higher skin retention levels than the DAB solution in MCT oil (Control, DAB-MCT). Furthermore, the formulations showed substantially higher cytotoxicity toward B16BL6 cell lines than the control formulation (p < 0.001). The half-maximal inhibitory concentrations (IC50) of F1, F2, and DAB-MCT formulations against B16BL6 cells were calculated to be 1 µg/mL, 10 µg/mL, and 50 µg/mL, respectively. By comparison, the IC50 of F1 was 50-fold lower than that of the DAB-MCT formulation. The results of the present study suggest that microemulsion could be a promising formulation for the topical administration of DAB.
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Patel, Swati, Prabhat Jain i Geeta Parkhe. "FORMULATION AND EVALUATION OF ACYCLOVIR LOADED NOVEL NANO-EMULSION GEL FOR TOPICAL TREATMENT OF HERPES SIMPLEX VIRAL INFECTIONS". Journal of Drug Delivery and Therapeutics 8, nr 5-s (1.10.2018): 265–70. http://dx.doi.org/10.22270/jddt.v8i5-s.1968.
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Acyclovir has low bioavailability mainly due to low solubility. This study aimed to formulate an optimized acyclovir (ACV) nanoemulsion gel for the slow, variable and incomplete oral drug absorption in patient suffering from herpes simplex viral infection. The dispersion solubility of acyclovir was studied in various oils, surfactants and co-surfactants and by constructing pseudo phase ternary diagram nanoemulsion area was identified. The optimized formulations of nanoemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in nanoemulsion, Zeta Potential and Vesicle size measurement and than nanoemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Span 40 was selected as surfactant, PEG 400 as co surfactant and castor oil as oil component based on solubility study. The in vitro drug release from acyclovir nanoemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of nanoemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of acyclovir can be increased by formulating into nanoemulsion gel.
Keywords: Acyclovir, Nanoemulsion, In-vitro diffusion, Zeta potential, Stability
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Siddiqui, Ayesha, Pooja Jain, Thompson Santosh Alex, Mohammed Asgar Ali, Nazia Hassan, Jamshed Haneef, Punnoth Poonkuzhi Naseef, Mohamed Saheer Kuruniyan, Mohd Aamir Mirza i Zeenat Iqbal. "Investigation of a Minocycline-Loaded Nanoemulgel for the Treatment of Acne Rosacea". Pharmaceutics 14, nr 11 (28.10.2022): 2322. http://dx.doi.org/10.3390/pharmaceutics14112322.
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In the present investigation, a nanoemulgel of minocycline was formulated and optimized for an improved drug delivery and longer retention time in the targeted area. Combining eucalyptus oil, Tween 20, and Transcutol HP, different o/w nanoemulsions were formulated by the oil phase titration method and optimized by pseudo-ternary phase diagrams. The morphology, droplet size, viscosity, and refractive index of the thermodynamically stable nanoemulsion were determined. Furthermore, optimized nanoemulsion was suspended in 1.0% w/v of Carbopol 940 gel to formulate the nanoemulgel, and for this, pH, viscosity, and spreadability were determined and texture analysis was performed. To compare the extent of drug penetration between nanoemulsion and nanoemulgel, ex vivo skin permeation studies were conducted with Franz diffusion cell using rat skin as the permeation membrane, and the nanoemulgel exhibited sustained-release behavior. It can be concluded that the suggested minocycline-containing naoemulgel is expected to treat acne rosacea more effectively.
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Tole, Karishma, i Ganesh Deshmukh. "DESIGN AND CHARACTERIZATION OF MICROEMULSION GEL FOR TRANSDERMAL DRUG DELIVERY SYSTEM OF DULOXETINE HYDROCHLORIDE". Asian Journal of Pharmaceutical and Clinical Research 11, nr 11 (7.11.2018): 157. http://dx.doi.org/10.22159/ajpcr.2018.v11i11.27552.
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Objective: The objective was to improve the bioavailability, stability of formulation, and skin permeability of Duloxetine HCl.Method: Microemulsion was prepared with oleic acid as oil, water, and Smix ratio of tween 20 to propylene glycol (1:3). Pseudo-ternary phase diagrams were constructed to determine the region of existence of microemulsions prepared using oil titration method. Optimization of formulations was done based on the in vitro diffusion studies. The microemulsion was gelled using carbopol 934p and HPMCK 100 as the gelling agent.Result: After the analysis of different evaluation parameter and drug release, the F3 batch was selected as a promising formulation for delivery of duloxetine HCl as a microemulsion gel for transdermal drug delivery with 79.607% drug release in 10 h.Conclusion: It was observed that transdermal microemulsion gel can be formulated successfully for duloxetine HCl with improved bioavailability. Among the other batches, the F3 batch was selected as an optimized batch because all the evaluation parameters results are satisfactory. From stability data, the formulation was found to be stable as no phase separation or turbidity was observed in the formulation after 3 months.
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Ghazwani, Mohammed, Rajalakshimi Vasudevan, Geetha Kandasamy, Naredla Manusri, Praveen Devanandan, Ranadheer Chowdary Puvvada, Vinoth Prabhu Veeramani i in. "Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug". Gels 9, nr 6 (2.06.2023): 457. http://dx.doi.org/10.3390/gels9060457.
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The purpose of the present work was to develop nanoemulsion-based formulations of mirtazapine for intranasal delivery using a spray actuator to target the brain for treating depression. Research on the solubility of medications in different oils, surfactants, co-surfactants, and solvents has been done. Using pseudo-ternary phase diagrams, the various ratios of the surfactant and co-surfactant mix were computed. Thermotriggered nanoemulsion was formulated using different concentrations of poloxamer 407 (i.e., 15%, 15.5%, 16%, 16.5% up to 22%). Similarly, mucoadhesive nanoemulsion using 0.1% Carbopol and water-based plain nanoemulsions were also prepared for comparative assessment. The developed nanoemulsions were analyzed for physicochemical properties, i.e., physical appearance, pH, viscosity, and drug content. Drug-excipient incompatibility was determined by Fourier transform infrared spectral (FTIR) analysis and differential scanning calorimetry (DSC). In vitro drug diffusion studies were conducted for optimized formulations. Among the three formulations, RD1 showed the highest percentage of drug release. Ex vivo drug diffusion studies were conducted on freshly excised sheep nasal mucosa with Franz diffusion cell simulated nasal fluid (SNF) for all three formulations up to 6 h, and the thermotriggered nanoemulsion (RD1) showed 71.42% drug release with 42.64 nm particle size and a poly dispersity index of 0.354. The zeta potential was found to be −6.58. Based on the above data, it was concluded that thermotriggered nanoemulsion (RD1) has great potential to be used as an intranasal gel for treating depression in patients. It can offer great benefits by reducing dosing frequency and improving bioavailability of mirtazapine by direct nose-to-brain delivery.
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Dash, Anuj, Saswata Bhattacharyya i Aloke Paul. "Concepts for estimating all types of diffusion coefficients of NiCoFeCr multi-principal element alloys using two dissimilar or a combination of ideal and non-ideal pseudo-ternary diffusion couples". Scripta Materialia 237 (grudzień 2023): 115719. http://dx.doi.org/10.1016/j.scriptamat.2023.115719.
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Bindhani, Sabitri, Snehamayee Mohapatra i Rajat Kumar Kar. "Vegetable Oil-Based Self-Microemulsifying Drug Delivery System of Eprosartan Mesylate: in vitro and ex vivo Evaluation". Asian Journal of Chemistry 33, nr 9 (2021): 2182–90. http://dx.doi.org/10.14233/ajchem.2021.23288.
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This study was planned to increase the intestinal permeability and thereby bioavailability of eprosartan mesylate (EPM) by designing a self-microemulsifying drug delivery system (SMEDDS) by the use of vegetable oils. Various SMEDDS-based formulations were prepared with oleic acid and peppermint oil. Tween 80 was used as surfactant and PEG 400 as co-surfactant. Pseudo ternary phase diagrams were constructed for identifying emulsification region between 1:1, 1:2, 2:1, 3:1 ratio of SCOS mix. Eight batches of SMEDDS were found to be thermodynamically stable and from which SMEDDSOF9 and PF5 were best formulations due to their highest drug content, minimum particle size. They have shown highest release of drug in vitro and higher in vitro drug diffusion and ex vivo permeation analysis than pure drug. FTIR study ascertained no incompatibility between drug and excipients present in formulation. From the accelerated stability study, slight effect on particle size and zeta potential, assay content along with cumulative % of drug release was found. The results demonstrated the SMEDDS of EPM are potent drug delivery system to increase dissolution rate and bioavailability of drug via increased intestinal permeability and consequently improving the therapeutic efficacy of eprosartan mesylate.
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Zhao, Zhi-Juan, Xiao-Dong Cui, Xiao-Li Ma i Zhuan-Hua Wang. "Formulation of a Self-Nanoemulsifying Drug Delivery System of Buckwheat Flavonoids and Evaluation of Its Antimicrobial Activity". Journal of Nanoscience and Nanotechnology 21, nr 5 (1.05.2021): 3050–58. http://dx.doi.org/10.1166/jnn.2021.19080.
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This study was aimed at constructing a self-nanoemulsifying drug delivery system of buckwheat flavonoids and evaluating its antimicrobial activity. The construction of the nanoemulsion followed a pseudo-ternary phase diagram, and its particle properties (particle size, zeta potential, and surface morphology) and physicochemical parameters (turbidity, surface tension, pH value, conductivity, encapsulation efficiency, and stability) were evaluated. The antimicrobial potential of buckwheat flavonoids nanoemulsion was determined against Staphylococcus aureus, Escherichia coli, and Candida albicans and compared to the buckwheat flavonoids suspension. The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) exhibited that the antimicrobial activity of the nanoemulsions and suspension increased while enhancing the drug concentration, and the antimicrobial activity of nanoemulsion was significantly higher than that of the suspension against those three bacteria. Agar disc diffusion test demonstrated that the inhibition zone diameter of the suspension was about 50% of the nanoemulsion against three bacteria. The time killing assay indicated that the IC50 of the nanoemulsion was significantly lower than that of the suspension. These results indicate that nanoemulsion is a promising drug delivery system, which can improve the antimicrobial activity of buckwheat flavonoids.
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Bhattacharya, Sankha, i Bhupendra G. Prajapati. "FORMULATION AND OPTIMIZATION OF CELECOXIB NANOEMULGEL". Asian Journal of Pharmaceutical and Clinical Research 10, nr 8 (1.08.2017): 353. http://dx.doi.org/10.22159/ajpcr.2017.v10i8.19510.
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Objective: The main objective of this experiment was to prepare and optimized celecoxib nanoemulgel. This formulation can be used for acuterheumatoid arthritis patients.Methods: Celecoxib is a poorly water soluble drug. We prepared celecoxib nanoemulgel to improve intrinsic solubility of celecoxib and enhancedeeper permeation throughout the skin. After several screening, the combination of acetonitrile, triacetin, campul 908P was considered for oil phase;acconon MC8-2EP as surfactant, and capmul MCM C-10 as a co-surfactant accordingly. As per Box-Behnken surface design model, optimization wasdone for all the 13 formulations.Results: Based on pseudo ternary plot, it was found that 4:1 Smix ratio was optimum and possessed maximum drug solubility. Further, screeningshown, 0.25-0.75% carbopol-940 can be a stable candidate for hydrogel preparation. Prepared nanoemulsions and hydrogels were admixed to preparenanoemulgel. Based on overlay plot, EG14* formulation was consider as optimum one, and various evaluation parameters were performed along withother formulations. Using Franz diffusion cell, in-vitro diffusion studies was performed. Almost all the formulations produces good qualitative drugrelease profile. The EG14* shown 95.50% drug release after 12th hrs with standard Higuchi plot (R2 value 0.9989). The optimum viscosity was foundto be 521±0.81 mPas at 100 rpm. The appearance of the formulations was milky, yellowish white with expectable pH ranged from 5.8 to 6.7. Theoptimized formulation has good spreadability coefficient, good ex-vivo diffusion enhancement factor (3.03) as compare to marketed gel. Mostly, ourformulations have less skin irritation and higher anti-inflammatory activity (92.56% of inhibition of paw edema for EG14*).Conclusion: From the thermodynamic studies, it was confirmed that EG14* maintained excellent stability profile in various heating-cooling cycle,centrifugation, and freeze-thaw cycle condition. Hence, it can be conclude that, our formulation, can be consider for pilot scale up.
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Shen, Jia-Chao, Hong-Yan Zeng, Bi Foua Claude Alain Gohi i Chao-Rong Chen. "Adsorption Behaviour of Cr(VI) from Ternary Mesoporous Mg/Fe/Al Oxide Using Glucose as a Soft Template". Journal of Nanoscience and Nanotechnology 20, nr 9 (1.09.2020): 5555–62. http://dx.doi.org/10.1166/jnn.2020.17875.
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The ternary mesoporous MgFeAl oxide (MgFeAlO) material was designed and prepared using glucose as a soft template by calcination of its MgFeAl hydrotalcite precursor. The MgFeAlO showed significantly better Cr(VI) adsorption performance than binary MgAlO. The effect of Fe3+ on Cr(VI) removal in simulated wastewater was studied by researching the microstructure, adsorption properties and mechanism of the material. The results showed that the addition of Fe3+ affected the microstructure of MgAlO, where the partial substitution of Al3+ by Fe3+ into the host layers resulted in an increase in the interlayer region and specific area (SBET) as well as an enlargement in mesoporous feature into the MgFeAlO. The Cr(VI) adsorption process, taking place by the reconstruction of the MgFeAlO oxide with water (memory effect) companying with the intercalation of CrO2−4 anions, was much more efficient than that occurring in the binary MgAlO. MgFeAlO’s adsorption of Cr(VI) follows the pseudo-second-order model and it is controlled by intra particle diffusion. The adsorption isotherm was better fitted by the Langmuir model, suggesting that the Cr(VI) adsorption was a monolayer adsorption onto the homogeneous support surface. All thermodynamic and kinetic calculations suggested that the Cr(VI) adsorption process on the MgFeAlO was of chemisorption nature, in which activation energy (Ea) and enthalpy change (ΔH) were 30.01 and 193.58 kJ·mol−1, respectively.
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H M, Raghu Kumar, i Parthiban S. "DEVELOPMENT OF LEVOFLOXACIN LOADED MICROEMULSION FORMULATED WITH MUSTARD OIL". Journal of Pharmaceutical and Scientific Innovation 10, nr 3 (31.05.2021): 87–93. http://dx.doi.org/10.7897/2277-4572.103210.
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The aim of the current study is to develop Levofloxacin loaded microemulsion formulated with mustard oil for better skin penetration effect and to obtain combined effect of both the oil and the drug to improve the efficacy with a reduced dose. Primarily we developed a pseudo ternary phase diagrams to find out the region of microemulsion formation zone by using oil (mustard oil), surfactant (Tween 20 and Tween 80), and co-surfactant (propylene glycol) by water titration method. We formulated six different formulations (MM1-MM6) by varying the concentrations of the oil water and surfactant and cosurfactant ratio. The developed microemulsion formulation was characterized for various parameters % Transmittance, viscosity, pH, drug content, surface morphology, zeta potential, and in-vitro drug release study. The selected microemulsion formulation is further converted in to microemulgel by dispersing the ME into 2%w/W Carbopol gel (MM-G) and various parameters are evaluated for the gel. The antimicrobial efficacy was carried out for ME and Microemulgel by well diffusion method against Staphylococcus aureus (MTCC: 737) compared with the standard streptomycin which showed that MM3 and MM-G have a better antimicrobial effect than standard proved that the drug levofloxacin and the mustard oil shows the synergistic effect in the Microemulsion formulation with better skin penetration effect.
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K M, Pavankumar, i Parthiban S. "DESIGN AND CHARACTERIZATION OF FLUCONAZOLE MICROEMULSION FORMULATED WITH LEMONGRASS OIL". Journal of Pharmaceutical and Scientific Innovation 10, nr 3 (31.05.2021): 80–86. http://dx.doi.org/10.7897/2277-4572.103209.
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The goal of the current investigation is to formulate Fluconazole loaded microemulsion (ME) with Lemongrass oil for deeper skin penetration and to obtain the dual benefit of drug and oil combination to improve antifungal efficacy of a drug with a reduced dose. We developed a Pseudo ternary phase diagram to identify the microemulsion zone by using the oil (clove oil), surfactant (Tween 20 and Tween 80), and co-surfactant (Propylene glycol) by water titration method. We formulated six different formulations (LM1 – LM6) by changing the oil/surfactant and cosurfactant ratio. The developed microemulsion formulation was characterized for various parameters % Transmittance, viscosity, pH, drug content, surface morphology, zeta potential, and in-vitro drug release study. The optimized microemulsion emulsion formulation is further converted into Microemulgel by dispersing the ME into 2% w/v Carbapol gel (LM-G) and further evaluated for various parameters. The antifungal efficacy was carried out for ME and Microemulgel by diffusion method against Candida albicans (MTCC no: 227) and compared with marketed gel which showed LM and LM-G have a better antifungal effect than marketed product, proved that the synergistic effect could be achieved by both clove oil and fluconazole drug by microemulsion formulation with deeper skin penetration effect.
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Yang, Ting-Lun, Chien-Ming Hsieh, Ling-Jei Meng, Tsuimin Tsai i Chin-Tin Chen. "Oleic Acid-Based Self Micro-Emulsifying Delivery System for Enhancing Antifungal Activities of Clotrimazole". Pharmaceutics 14, nr 3 (22.02.2022): 478. http://dx.doi.org/10.3390/pharmaceutics14030478.
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Due to the increasing rate of drug resistance in Candida spp., higher doses of antifungal agents are being used resulting in toxicity. Drug delivery systems have been shown to provide an effective approach to enhance the efficacy and reduce the toxicity of antifungal agents. Oleic acid was revealed to effectively inhibit biofilm formation, hence reducing the virulence of Candida albicans. In this study, oleic acid-based self micro-emulsifying delivery systems (OA-SMEDDS) were developed for delivering clotrimazole (CLT). Based on the pseudo-ternary phase diagram and loading capacity test, the optimal ratio of OA-SMEDDS with CLT was selected. CLT-loaded OA-SMEDDS not only bears a higher drug loading capacity but also maintains good storage stability. The minimum inhibitory concentration (MIC50) of CLT-loaded OA-SMEDDS (0.01 μg/mL) in Candida albicans was significantly lower than that of CLT dissolved in DMSO (0.04 μg/mL). Moreover, we showed CLT-loaded OA-SMEDDS could effectively prevent biofilm formation and destroy the intact biofilm structure of Candida albicans. Furthermore, a CLT-loaded OA-SMEDDS gel was developed and evaluated for its antifungal properties. Disk diffusion assay indicated that both CLT-loaded OA-SMEDDS and CLT-loaded OA-SMEDDS gels were more effective than commercially available products in inhibiting the wild-type and drug-resistant species of Candida.
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Harwansh, Ranjit Kumar, Kartik Chandra Patra, Surendra Kumar Pareta, Jagadish Singh i Mohammed Akhlaquer Rahman. "Nanoemulsions as vehicles for transdermal delivery of glycyrrhizin". Brazilian Journal of Pharmaceutical Sciences 47, nr 4 (grudzień 2011): 769–78. http://dx.doi.org/10.1590/s1984-82502011000400014.
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The present investigation aims to evaluate an isotropic and thermodynamically stable nanoemulsion formulation for transdermal delivery of glycyrrhizin (GZ), with minimum surfactant and cosurfactant (Smix) concentrations that could improve its solubility, permeation enhancement, and stability. Pseudo-ternary phase diagrams were developed and various nanoemulsion formulations were prepared using soyabean oil as oil, Span 80, Brij 35 as a surfactant and isopropyl alcohol as a cosurfactant. Nanoemulsion formulations that passed the thermodynamic stability tests were characterized for pH, viscosity and droplet size using a transmission electron microscopy. The transdermal ability of glycyrrhizin through human cadaver skin was determined using Franz diffusion cells. The in vitro skin permeation profile of the optimized nanoemulsion formulation (NE2) was compared to that of conventional gel. A significant increase in permeability parameters such as steady-state flux (Jss) and permeability coefficient (Kp) was observed in the optimized nanoemulsion formulation (NE2), which consisted of 1% wt/wt of mono ammonium glycyrrhizinate (MAG), 32.4% Span 80, 3.7% Brij 35, 10% isopropyl alcohol, 46.5% soyabean oil and 6.4% distilled water. No obvious skin irritation was observed for the studied nanoemulsion formulation (NE2) or the gel. The results indicated that nanoemulsions are promising vehicles for transdermal delivery of glycyrrhizin through human cadaver skin, without the use of additional permeation enhancers, because excipients of nanoemulsions act as permeation enhancers themselves.
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Bedse, Anjali, Ajinath Nikam, Aditi Kulkarni, Vaishali Potnis i Suchita Dhamane. "Development and Characterization of topical microemulsion as novel drug delivery system for Dapsone". International Journal of Pharmaceutical Sciences and Nanotechnology 15, nr 1 (28.02.2022): 5805–12. http://dx.doi.org/10.37285/ijpsn.2022.15.1.8.
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Dapsone is a Biopharmaceutical Classification System class II drug with anti inflammatory, immunosuppressive, antibacterial, and antibiotic properties and is used as an antileprotic. The purpose of the present study was to investigate the potential of a microemulsion formulation for topical delivery of dapsone to enhance permeation and to avoid systemic side effects. When administered orally, dapsone undergoes hepatic metabolism. Its hepatic metabolite, dapsone hydroxylamine, shows systemic side effects such as hemolytic anaemia peripheral neuropathy, nausea, and headache. A novel drug delivery system in the form of a microemulsion was developed for dapsone. This is the first attempt that dapsone has been combined with chaulmoogra oil in a topical microemulsion. The primary drugs used for the treatment of leprosy are found in chaulmoogra seeds. Considering its good solubilizing capacity and its use in the treatment of leprosy, chaulmoogra oil was chosen as the oil phase. Based on emulsification ability, Cremophor RH40 and PEG 400 were selected as surfactant and co-surfactant, respectively. A pseudo-ternary phase diagram was constructed to identify the microemulsion region. Smix (Cremophor RH40: PEG-400 in the ratio of 1:2) was most effective in imparting stability to the formulation. The selected formulation exhibited appropriate diffusion behavior (in vitro). The developed dapsone containing microemulsion formulation exhibited the optimal homogeneity, clarity, pH, type of microemulsion, viscosity, percent drug content, and percent transmittance to qualify as a topical drug delivery system for local treatment of leprosy.
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Sabitri Bindhani, Snehamayee Mohapatra, Rajat Ku. Kar i Utkalika Mahapatra. "Preparation of self micro emulsifying drug delivery system(smedds) of poorly soluble drug eprosartan mesylate and its in vitro evaluation". International Journal of Research in Pharmaceutical Sciences 10, nr 4 (16.10.2019): 3304–14. http://dx.doi.org/10.26452/ijrps.v10i4.1636.
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Eprosartan Mesylate (EM), an angiotensin II receptor blocker used in the treatment of high blood pressure. But poor solubility and bioavailability (13%) of eprosartan mesylate is a major challenging factor for improving its drug release rate. The main objective of the present work to develop and characterize self micro emulsifying drug delivery system of eprosartan mesylate by using compatible oil, surfactant and co-surfactant. For the selection of oil, surfactant and cosurfactant, solubility screening studies has been carried out. The nine formulations are prepared using peppermint oil, tween 80 and PEG 400. A pseudo ternary phase diagram was prepared to determine the self emulsion region. Four optimized formulations were prepared at 1:1 ratio(a mixture of surfactant and cosurfactant). These four formulations were evaluated for self-emulsification time, droplet size measurement, drug content analysis robustness to dilution test, viscosity analysis, f.t.i.r. The study and in-vitro diffusion studies. The ratio of scosmix (a mixture of surfactant and cosurfactant) of optimized formulation (pf5) was varied to pfa1 (2:1), pf2 (3:1), pfa3 (1:2) and compared with pure drug. The formulation having pfa1 (2:1) shown drug release of 93.13 % in 330 minutes where as pure drug showed a drug release of 54.51% in 330 minutes. So the prepared SMEDDS formulations were efficient and better than the pure drug, and it followed Korsmeyer pappes due to highest r2 value followed by Hixon crowel. It was concluded that incorporation of eprosartan mesylate in selfmicroemulsifying system is a great potential for improving the solubility and dissolution rate of eprosartan mesylate.
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Jantrawut, Pensak, Kasidech Boonsermsukcharoen, Kanyanut Thipnan, Tanpong Chaiwarit, Kyu-Mok Hwang i Eun-Seok Park. "Enhancement of Antibacterial Activity of Orange Oil in Pectin Thin Film by Microemulsion". Nanomaterials 8, nr 7 (19.07.2018): 545. http://dx.doi.org/10.3390/nano8070545.
Pełny tekst źródłaStreszczenie:
The purpose of this study was to prepare orange oil microemulsion (ME) and to investigate the antimicrobial activity of film containing orange oil ME. First, surfactants and co-surfactants were screened on their efficiency to form ME using pseudo-ternary phase diagrams. The influences of surfactant and co-surfactant mass ratios were studied and optimized ME-loaded-films were prepared. Then, films containing orange oil ME were characterized by SEM and texture analyzer, and then evaluated for antimicrobial activity against Staphylococcus aureus and Propionibacterium acnes using an agar disc diffusion method. The results showed that Tween 80 as surfactant and propylene glycol as co-surfactant at a 1:1 ratio possessed the maximum ME area. Three ME formulations of ME 20, ME 25, and ME 30, which consisted of 20, 25, and 30% w/v of orange oil were prepared, respectively. All ME formulations showed particle sizes of about 60.26–80.00 nm, with broad a polydispersity index of 0.42. The orange oil ME films exhibited higher elastic values than the control. The diameters of inhibition zones for FME 20, FME 25, and FME 30 against P. acnes were 13.64, 15.18, and 16.10 mm, respectively. Only the FME 30 had an antimicrobial activity against S. aureus with 8.32 mm of inhibition zone. Contrarily, the control film had no antimicrobial activity against both bacteria. In conclusion, the present study found that the antibacterial activity of orange oil in pectin thin film could be enhanced by preparing orange oil as an ME before loading into pectin thin film.
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Bindhani, Sabitri, Utkalika Mohapatra, Snehamayee Mohapatra i Rajat K. Kar. "Enhancement of Solubility and Dissolution Rate of Poorly Soluble Drug Nifedipine by Solid Sedds". International Journal of Drug Delivery Technology 10, nr 01 (25.03.2020): 9–15. http://dx.doi.org/10.25258/ijddt.10.1.3.
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Nifedipine is a dihydropyridine calci channel blocking agent belongs to biopharmaceutical classification system (BCS) class-II mainly applied in the treatment of hypertension and angina-pectoris. The objective of this work is to improve the solubility and dissolution rate of nifedipine by formulating into a solid-self micro emulsifying drug delivery system (solid smedds). Methods: Oil, Surfactant, and cosurfactant were selected by solubility screening study. For the determination of the best emulsion region, a pseudo ternary diagram was prepared. Based on solubility castor oil, tween 80 and polyethylene glycol (PEG) 400 was selected in which SCOSmix (a mixture of surfactant and cosurfactant) was 1:1. Thermodynamic stability study was performed for the determination of stable smedds formulation. These formulations were evaluated for self emulsification time, drug content analysis, robustness to dilution test, particle size analysis, and in vitro diffusion study. The optimized formulation was selected for formulating into solid-smedds by using aerosil 200 at a different ratio. SCF9L (0.65:1) was selected due to its good flow property. Then it was evaluated for particle size analysis, drug content study, differential scanning calorimetry (DSC), X-Ray Diffraction study (XRD), fourier transform infrared spectroscopy (FTIR) Scanning Electron Microscopy study (SEM) analysis, and in vitro dissolution study. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM analysis, the texture of powder showed a uniform granular structure, and there was no incompatibility between drugs. Excipients was observed from ftir study. From the in vitro dissolution study, it improved the dissolution rate of nifedipine, which was 98.68% of drug release, where pure drug release only 6.75%.
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Venkatachalam, Abhirami, Harini Chowdary Vadlamudi i Sneha Bharti. "Factorial Design Executed Development of Miconazole Nitrate Microemulsion Based Bioadhesive Gel and Its Evaluation". International Journal of Research and Review 9, nr 1 (29.01.2022): 574–87. http://dx.doi.org/10.52403/ijrr.20220167.
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Miconazole nitrate (MN) is a poorly aqueous soluble antifungal drug. The microemulsion (ME) based bioadhesive antifungal gel of MN was designed to improve the antifungal activity by increasing the bioadhesion potential. Based on the solubility results, components of ME were selected viz. rice bran oil: tween 80: propylene glycol and proceeded with pseudo-ternary phase diagram studies. 23 factorial design was employed for the formulation of MEs employing water titration technique. The MEs was examined for further studies and was optimized using DESIGN EXPERT 12 software considering the responses like globule size, zeta potential and in vitro drug release. Tamarind seed polysaccharide (TSP) and carbopol 934 were used as gel bases for the formulation of microemulsion-based bioadhesive gels. The gels were examined for drug content, pH, spreadability, viscosity, bioadhesive strength, ex vivo drug permeation and in vivo skin irritation potential. The antifungal activity against Candida albicans and Cryptococcus neoformans of four formulations (MN-ME, MN- ME based TSP gel, MN- ME based carbopol gel and marketed miconazole gel (2% Miconazole gel) was evaluated using modified agar diffusion method. The results revealed that microemulsion based bioadhesive gel (MBG) of TSP and CP exhibited drug content of about 87.29% and 83.34% and ex vivo skin permeation of 84.21% and 73.94% at the end of 10 h. MBG of TSP showed better antifungal activity and no skin irritation potential in comparison to the carbopol gel. Therefore, MBG of TSP has the ability to enhance the contact time owing to greater bioadhesion thereby providing a better therapeutic activity. Keywords: Miconazole nitrate, Tamarind Gum, Topical delivery, Microemulsion based bioadhesive gel, fungal infection.
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Ashara, Kalpesh C., i Ketan V. Shah. "Emulsion of Chloramphenicol: an Overwhelming Approach for Ocular Delivery". Folia Medica 59, nr 1 (1.03.2017): 23–30. http://dx.doi.org/10.1515/folmed-2017-0007.
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Abstract Background: Ophthalmic formulations of chloramphenicol have poor bioavailability of chloramphenicol in the ocular cavity. Aim: The present study aimed at exploring the impact of different oil mixtures in the form of emulsion on the permeability of chloramphenicol after ocular application. Materials and methods: Selection of oil mixture and ratio of the components was made by an equilibrium solubility method. An emulsifier was chosen according to its emulsification properties. A constrained simplex centroid design was used for the assessment of the emulsion development. Emulsions were evaluated for physicochemical properties; zone of inhibition, in-vitro diffusion and ex-vivo local accumulation of chloramphenicol. Validation of the design using check-point batch and reduced polynomial equations were also developed. Optimization of the emulsion was developed by software Design® expert 6.0.8. Assessment of the osmolarity, ocular irritation, sterility testing and isotonicity of optimized batch were also made. Results: Parker Neem®, olive and peppermint oils were selected as an oil phase in the ratio 63.64:20.2:16.16. PEG-400 was selected as an emulsifier according to a pseudo-ternary phase diagram. Constrained simplex-centroid design was applied in the range of 25-39% water, 55-69% PEG-400, 5-19% optimized oil mixture, and 1% chloramphenicol. Unpaired Student’s t-test showed for in-vitro and ex-vivo studies that there was a significant difference between the optimized batch of emulsion and Chloramphenicol eye caps (a commercial product) according to both were equally safe. Conclusion: The optimized batch of an emulsion of chloramphenicol was found to be as safe as and more effective than Chloramphenicol eye caps.
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Mehreen Sattar, Somia Sarfraz, Uzma Liaquat, Iqra Shoukat, Bilal Ahmad i Talib Hussain. "Formulation and evaluation of topical piroxicam microemulgel for arthritis". Journal of Contemporary Pharmacy 7, nr 1 (30.06.2023): 16–23. http://dx.doi.org/10.56770/jcp2023713.
Pełny tekst źródłaStreszczenie:
Background: Piroxicam is an anti-inflammatory, analgesic, and antipyretic drug. Piroxicam is widely used in the management of chronic pain. The objective of this work was to develop and analyze topical Piroxicam microemulgel to improve drug solubility, enhance permeation, reduce GIT side effects reduce the frequency of the drug. Method: The Piroxicam microemulgel was prepared by drawing the pseudo ternary phase picture and water titration procedure. Formulation was prepared by using isopropyl myristate as an oil, Tween 80 as an surfactant, n-butanol as Co-surfactant and water. It was converted to gel by using 1% Carbopol 940 and few drops of ethanolamine. The prepared formulation was characterized for thermodynamic stability, pH, droplet size, viscosity, FTIR,DSC, electrical conductivity, dye solubility drug content, and in-vitro release using a Franz diffusion cell. Result: Microemulgel formulation was thermodynamically stable on visual inspection after being treated with a freeze-thaw cycle and centrifugation. pH of formulation was 6.5. The mean droplet size for ME gel was 100±0.472nm. The viscosity of the microemulgel was 90.4±0.01 cps which showed Newtonian flow. FTIR and DSC studies showed that microemulgel was compatible with its excipients. Electrical conductivity and dye solubility testing confirmed that the microemulgel was O/W. Piroxicam microemulsion gel showed 89.89% drug content and the release rate of piroxicam was 98±8.63% after 48h. It followed the Korsmeyer Pappas model which means it was a hydrogel-based system. Conclusion: Microemulsion gel formulation obtained remarkably inflated skin retention for piroxicam over the piroxicam gel. It might act as a promising vehicle for the topical delivery of poor water-soluble drugs.
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Sattar, Mehreen, Somia Sarfraz, Uzma Liaquat, Iqra Shoukat, Bilal Ahmad i Talib Hussain. "Formulation and evaluation of topical piroxicam microemulgel for arthritis". Journal of Contemporary Pharmacy 7, nr 1 (30.06.2023): 16–23. http://dx.doi.org/10.56770/jcp.2023713.
Pełny tekst źródłaStreszczenie:
Background: Piroxicam is an anti-inflammatory, analgesic, and antipyretic drug. Piroxicam is widely used in the management of chronic pain. The objective of this work was to develop and analyze topical Piroxicam microemulgel to improve drug solubility, enhance permeation, reduce GIT side effects reduce the frequency of the drug. Method: The Piroxicam microemulgel was prepared by drawing the pseudo ternary phase picture and water titration procedure. Formulation was prepared by using isopropyl myristate as an oil, Tween 80 as an surfactant, n-butanol as Co-surfactant and water. It was converted to gel by using 1% Carbopol 940 and few drops of ethanolamine. The prepared formulation was characterized for thermodynamic stability, pH, droplet size, viscosity, FTIR,DSC, electrical conductivity, dye solubility drug content, and in-vitro release using a Franz diffusion cell. Result: Microemulgel formulation was thermodynamically stable on visual inspection after being treated with a freeze-thaw cycle and centrifugation. pH of formulation was 6.5. The mean droplet size for ME gel was 100±0.472nm. The viscosity of the microemulgel was 90.4±0.01 cps which showed Newtonian flow. FTIR and DSC studies showed that microemulgel was compatible with its excipients. Electrical conductivity and dye solubility testing confirmed that the microemulgel was O/W. Piroxicam microemulsion gel showed 89.89% drug content and the release rate of piroxicam was 98±8.63% after 48h. It followed the Korsmeyer Pappas model which means it was a hydrogel-based system. Conclusion: Microemulsion gel formulation obtained remarkably inflated skin retention for piroxicam over the piroxicam gel. It might act as a promising vehicle for the topical delivery of poor water-soluble drugs.
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Nagaraja, Sreeharsha, Girish Meravanige Basavarajappa, Mahesh Attimarad i Swati Pund. "Topical Nanoemulgel for the Treatment of Skin Cancer: Proof-of-Technology". Pharmaceutics 13, nr 6 (18.06.2021): 902. http://dx.doi.org/10.3390/pharmaceutics13060902.
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The present study is a mechanistic validation of ‘proof-of-technology’ for the effective topical delivery of chrysin nanoemulgel for localized, efficient treatment of melanoma-affected skin. Background: Currently available treatments for skin cancer are inefficient due to systemic side effects and poor transcutaneous permeation, thereby presenting a formidable challenge for the development of novel nanocarriers. Methods: We opted for a novel approach and formulated a nanocomplex system composed of hydrophobic chrysin dissolved in a lipid mix, which was further nanoemulsified in Pluronic® F-127 gel to enhance physicochemical and biopharmaceutic characteristics. Chrysin, a flavone extracted from passion flowers, exhibits potential anti-cancer activities; however, it has limited applicability due to its poor solubility. Pseudo-ternary phase diagrams were constructed to identify the best self-nanoemulsifying region by varying the compositions of oil, Caproyl® 90 surfactant, Tween® 80, and co-solvent Transcutol® HP. Chrysin-loaded nanoemulsifying compositions were characterized for various physicochemical properties. Results: This thermodynamically stable, self-emulsifying drug delivery system showed a mean droplet size of 156.9 nm, polydispersity index of 0.26, and viscosity of 9100 cps after dispersion in gel. Mechanical characterization using Texture Analyzer exhibited that the gel had a hardness of 487 g and adhesiveness of 500 g. Ex vivo permeation through rat abdominal skin revealed significant improvement in percutaneous absorption measured as flux, the apparent permeability coefficient, the steady-state diffusion coefficient, and drug deposition. In vitro cytotoxicity on A375 and SK-MEL-2 cell lines showed a significantly improved therapeutic effect, thus ensuring reduction in dose. The safety of the product was established through biocompatibility testing on the L929 cell line. Conclusion: Aqueous, gel-based, topical, nanoemulsified chrysin is a promising technology approach for effective localized transcutaneous delivery that will help reduce the frequency and overall dose usage and ultimately improve the therapeutic index.
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Gohel, Mukesh, Ankita Purohit, Asha Patel i Lal Hingorani. "OPTIMIZATION OF BACOSIDE A LOADED SNEDDS USING D-OPTIMAL MIXTURE DESIGN FOR ENHANCEMENT INSOLUBILITY AND BIOAVAILABILITY". International Journal of Pharmacy and Pharmaceutical Sciences 8, nr 12 (1.12.2016): 213. http://dx.doi.org/10.22159/ijpps.2016v8i12.13488.
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<p><strong>Objective</strong>:<strong> </strong>The objective of present study is to enhance solubility and bioavailability of poorly soluble <em>bacoside A</em> present in <em>Bacopa monnieri</em> extract using self nano emulsifying drug delivery system (SNEDDS) for the treatment of Alzheimer's disease.</p><p><strong>Methods: </strong>Solubility of the drug was assessed in various oils (edible as well as synthetic oil), surfactant and co-surfactant by saturation solubility study. Pseudo-ternary phase diagram was used to obtain appropriate concentration ranges of components include oil, surfactant and co-surfactant.</p><p><strong>Results: </strong>From the result of saturated solubility study and phase diagram, oleic acid, tween 20 and ethanol was selected as oil, surfactant and co-surfactant. The D-Optimal mixture design was used to optimize the formulation on the basis of solubility of drug and dilution potential. <em>In vitro</em> dissolution, study showed 89% of drug release from optimized SNEDDS formulation compared to untreated drug<em> </em>extract with 24% of drug release in 60 min. Ex vivo diffusion study showed more than 90% of drug diffused from optimized SNEDDS formulation compared to pure extract.</p><p><strong>Conclusion: </strong>In a nutshell, the developed SNEDDS formulation using the design of experimentation approach held great potential as a possible alternative to traditional oral formulations of poorly soluble <em>Bacoside A </em>to improve solubility and bioavailability.</p>
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Jiang, Kui, Jie Zhang, Zhengxing Peng, Francis Lin, Shengfan Wu, Zhen Li, Yuzhong Chen i in. "Pseudo-bilayer architecture enables high-performance organic solar cells with enhanced exciton diffusion length". Nature Communications 12, nr 1 (20.01.2021). http://dx.doi.org/10.1038/s41467-020-20791-z.
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AbstractSolution-processed organic solar cells (OSCs) are a promising candidate for next-generation photovoltaic technologies. However, the short exciton diffusion length of the bulk heterojunction active layer in OSCs strongly hampers the full potential to be realized in these bulk heterojunction OSCs. Herein, we report high-performance OSCs with a pseudo-bilayer architecture, which possesses longer exciton diffusion length benefited from higher film crystallinity. This feature ensures the synergistic advantages of efficient exciton dissociation and charge transport in OSCs with pseudo-bilayer architecture, enabling a higher power conversion efficiency (17.42%) to be achieved compared to those with bulk heterojunction architecture (16.44%) due to higher short-circuit current density and fill factor. A certified efficiency of 16.31% is also achieved for the ternary OSC with a pseudo-bilayer active layer. Our results demonstrate the excellent potential for pseudo-bilayer architecture to be used for future OSC applications.
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Chaturvedi, Priyanka, i Praveen Sharma. "Evaluation of the in-vitro antifungal activity of Holoptelea Integrifolia ethanolic extract loaded in microemulsion". EJPPS EUROPEAN JOURNAL OF PARENTERAL AND PHARMACEUTICAL SCIENCES, 28.07.2023. http://dx.doi.org/10.37521/ejpps.28202.
Pełny tekst źródłaStreszczenie:
Microemulsions improve the transdermal delivery of several drugs over conventional topical preparations such as emulsions and gels: enhanced drug solubilization, increased skin flux, and decreased diffusion coefficient. Microemulsion-based systems find significant improvement in the topical delivery of antifungals. We believe that drug-loaded microemulsion will show better antifungal activity by better penetration into the skin and fungal cells. Antifungal agents are mostly lipophilic and easily formulated in topical vehicles. Microemulsions were prepared by the phase titration method. Formulations of the same drug and Excipient ratio and different concentrations were optimized with selected parameters like pseudo ternary phase diagram, particle analysis size, zeta potential validation, entrapment efficiency, and drug release studies performed by dialysis bag diffusion techniques at a temperature (37ºC). The study continued for 24 hours. The maximum amount of drug Holoptelea integrifolia release is 90% within 8hr. The study was monitored at 37ºC. Successfully done preparation, characterization, and drug release study of Microemulsion drug loaded.
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Kamar, Firas Hashim, Aurelia Cristina Nechifor, Gheorghe Nechifor, Tariq J. Al-Musawi i Asem Hassan Mohammed. "Aqueous Phase Biosorption of Pb(II), Cu(II), and Cd(II) onto Cabbage Leaves Powder". International Journal of Chemical Reactor Engineering 15, nr 2 (1.04.2017). http://dx.doi.org/10.1515/ijcre-2015-0178.
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Abstract In this study, the biosorption of lead (Pb(II)), copper (Cu(II)), and cadmium (Cd(II)) ions from aqueous solution using waste of cabbage leaves powder (CLP) was investigated as a function of pH, shaking time, initial metal concentration, and biosorbent dose. The maximum removal efficiency at optimum condition in single biosorption system was 95.67, 92.42, and 88.92 % for Pb(II), Cu(II), and Cd(II) ions, respectively. These values reduced in ternary systems in the same sequence. Langmuir and extended Langmuir isotherm models were found to be the best fit of the isotherm data for single and ternary biosorption systems, respectively. The kinetic data of the three metals were better fit by the pseudo-second-order model with higher coefficient of determination and more closely predicted uptake. In addition, the results showed that the intraparticle diffusion was the dominating mechanism. Thermodynamic study showed that the biosorption of Pb(II), Cu(II), and Cd(II) onto CLP was a chemical reaction which was exothermic in nature. Finally, SEM image shows that CLP has a number of heterogeneous small pores while the Fourier transform infrared (FTIR) spectroscopic analysis showed that the carboxyl, amine, and hydroxyl groups are the major groups that are responsible for the biosorption process.
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Patel, Neelam, Sunita Chaudhary i Ankit Chaudhary. "Formulation Development and Evaluation of Apremilast Nanoemulsion". Research Journal of Pharmacy and Technology, 26.06.2023, 2859–66. http://dx.doi.org/10.52711/0974-360x.2023.00471.
Pełny tekst źródłaStreszczenie:
Apremilast is a selective phosphodiesterase 4 inhibitor administered orally in the treatment of moderate-to-severe plaque psoriasis and active psoriatic arthritis. It is classified as class IV drug as per BCS classification so it indicates low solubility and lower permeability through the skin. Therefore the objective of the research is to improve permeability of Apremilast through the skin and improve solubility by using oil and surfactant by formulating Nanoemulsion. Nanoemulsion was prepared by selecting Captex 355, Cremophore RH 40, Labrafil and Propylene glycol as the oil, surfactant,co-surfactant and co-solvent respectively after solubility study. Pseudo-ternary phase diagrams were constructed to find out the optimum ratio of oil: Smix (surfactant: co-Surfactant). Simple lattice design was applied to the optimization of the prepared nanoemulsion. The nanoemulsion was evaluated for Physical parameter, pH, Droplet size, zeta potential, in-vitro diffusion study etc. Results of Droplet size measurements, zeta potential and % drug diffusion indicated A5 batch optimized batch than other formulation of the nanoemulsion. So, optimized formulation further tested for Skin irritation study and stability study.The Apremilast loaded stable Nanoemulsion system was prepared and various process variables were evaluated. Batch A5 was selected as an optimized batch containing 10 % Captex 355, 40 % Smix (Cremophore RH 40 and Labrafil) and 50% water. Optimized batch was found to be stable after three month at ambient condition of temperature and humidity, giving reproducible results when evaluated.
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Grifoni, Lucia, Giulia Vanti, Maria Giuliana vannucchi, Maria Camilla Bergonzi i Anna Rita BILIA. "Development and evaluation of khellin-loaded microemulgel for dermatological applications". Planta Medica, 4.03.2022. http://dx.doi.org/10.1055/a-1789-3112.
Pełny tekst źródłaStreszczenie:
Microemulsions are optically nanosized emulsions, isotropic and thermodynamically stable. They represent versatile drug delivery systems with high potential because can be administered through all routes. In the present study, we report on the formulation of a microemulsion made with glycerol (2.25%), Labrasol (20.25%) vitamin E acetate (2.50%), and water (75.00%), which was developed using the pseudo-ternary phase diagram. Globules of the microemulsion had PdI less than 0.25 and size of about 17 nm, evaluated by DLS analysis. These values did not change after loading khellin, a natural lipophilic molecules with interesting biological activities, used as a model of lipophilic drug. Carboxymethyl cellulose was selected as gelling polymer to obtain a microemulgel. Viscosity was 22,100.0±1555.6 mPas·s at 21±2°C, while it was 8,916.5±118.1 mPas·s at 35±2°C, remaining stable over time. Khellin recovery was 93.16±4.39% and it was unchanged after 4 weeks of storage (93.23±2.14%). The pH was 6.59±0.19 and it was found 6.42±0.34 at the end of the storage lifetime. The diffusion of khellin from the developed formulation was prolonged over an extended period. Based on overall results and due to the dermatological properties of the ingredients of the formulation, the developed microemulgel loaded with khellin is very promising and suitable for skin care applications.
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DAS, SAHELI, SHARADHA M., M. P. VENKATESH, SUBHASHREE SAHOO, JOGABRATA TRIPATHY i D. V. GOWDA. "FORMULATION AND EVALUATION OF TOPICAL NANOEMULGEL OF METHOTREXATE FOR RHEUMATOID ARTHRITIS". International Journal of Applied Pharmaceutics, 7.09.2021, 351–57. http://dx.doi.org/10.22159/ijap.2021v13i5.41026.
Pełny tekst źródłaStreszczenie:
Objective: The purpose of this study was to develop and evaluate methotrexate-loaded nanoemulgel for topical delivery in the management of rheumatoid arthritis.
Methods: Based on nanoemulsion composition, the pseudo ternary phase diagram was fabricated by using peanut oil, Tween 20 as the surfactant, and PEG 400 being used as a co-surfactant. The methotrexate-loaded nanoemulsion was formulated by using the spontaneous emulsification method. Badam gum was used as a gel matrix in the prepared nanoemulsion to form nanoemulgel. The methotrexate loaded nanoemulgel was characterized and evaluated for pH, particle size, physical appearance, viscosity, spreadability, TEM, drug content, diffusion study, release kinetics, and stability studies.
Results: The nanoemulgel constituting 8.6% peanut oil, 34.4% of Tween 20 and PEG 400 as Smix (surfactant and co-surfactant mixture), 43% water, and 12.5% w/w badam gum was concluded as optimized formulation. The prepared nanoemulgel was translucent in nature having a particle size of 195.1nm and zeta potential of -0.278mV. Drug content and drug release for the optimized formulation were found to be 98.11±0.34% and 95.11±0.02% respectively. pH, viscosity, and spreadability were found to be optimum. Stability study data showed that the prepared nanoemulgel was stable at different temperatures varying from -25 to +45ºC.
Conclusion: Methotrexate loaded nanoemulgel has been formulated for topical drug delivery for the management of rheumatoid arthritis.
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Bisht, Alpna, Chetna Hemrajani, Charul Rathore, Tania Dhiman, Rajan Rolta, Navneet Upadhyay, Prakriti Nidhi i in. "Hydrogel composite containing azelaic acid and tea tree essential oil as a therapeutic strategy for Propionibacterium and testosterone-induced acne". Drug Delivery and Translational Research, 15.11.2021. http://dx.doi.org/10.1007/s13346-021-01092-4.
Pełny tekst źródłaStreszczenie:
AbstractAzelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (−1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris. Graphical abstract
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OZA, NISHANT, SWATI SAGAR i AKRUTI KHODAKIYA. "USE OF SIMPLEX LATTICE DESIGN IN DEVELOPMENT OF ORAL SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ROSUVASTATIN CALCIUM". International Journal of Applied Pharmaceutics, 6.03.2020, 40–47. http://dx.doi.org/10.22159/ijap.2020v12i3.34358.
Pełny tekst źródłaStreszczenie:
Objective: The aim of the present work was to enhance the solubility of rosuvastatin calcium by self-nano emulsifying drug delivery system (SNEDDS) using mixtures of oil, cosolvent, surfactant and cosurfactant.
Methods: Based on solubility study and emulsification efficiency, Preliminary investigations of various oils, surfactants and cosurfactants were carried out for the selection of the proper SNEDDS ingredients. Pseudo-ternary phase diagrams were constructed to identify the efficient self-emulsification region. A series of SNEDDS formulations were prepared using labrasol: cremophor EL with a combination of peceol: ethyl oleate by using the simplex lattice design. Prepared formulation evaluated for refractive index, turbidimetric, droplet size, zeta potential and polydispersity index, self-emulsification, stability tests, viscosity and in vitro diffusion studies.
Results: The best formula for SNEDDS in the current study were: 15% oil (peceol: ethyloleatein 1:1 ratio), 50% Labrasol and 35% Cremophor EL. All the SNEDDS batches globule size was found to be varied from 22.90±1.50 nm to 43.90±1.40 nm. and no significant variations in globule size were observed after 3 mo stability studies. All the batches % transparency was found to be varied from 95.40±1.40% to 99.50±1.10% and drug diffused in 10 min varied from 63.65±1.51% to 93.72±1.46 %.
Conclusion: The data suggest the use of rosuvastatin calcium SNEDDS to offer the potential for delivery and it increases the aqueous solubility and bioavailability of the drug.
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Vaghela, Sohansinh, Sunita Chaudhary i Ankit Chaudhary. "Formulation Development and Optimization of Blonanserin Liquid SMEDDS using D-Optimal Mixture Design". Current Drug Therapy 17 (21.04.2022). http://dx.doi.org/10.2174/1574885517666220421125528.
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Background: Blonanserin is an atypical antipsychotic potent antagonist of dopamine-D2 and D3 receptors with low aqueous solubility BCS class II drugs. Objective: The present research aims to develop and optimize Blonanserin loaded liquid self-micro emulsifying drug delivery system (SMEDDS) for improvement of its in vitro drug release by D-optimal mixture design. Methods: Saturation solubility of Blonanserin was checked in various oils, surfactants, and cosurfactants. The pseudo-ternary phase diagram was developed to identify the region of micro emulsion. Trial batch designed to determine dependent and independent variables in the formulation. D-Optimal Mixture design applies for optimization and minimized trials. The amount of oil(X1), surfactant(X2), and co-surfactant(X3) were selected as independent variables, and solubility(Y1) and in vitro percentage cumulative drug release(Y2) and size of globule(Y3) after 250 times dilution were selected as the dependant variable. The level of the independent variables in the design will be selected based on the phase diagram, trial batches, and solubility of the drug. The developed SMEDDS was then evaluated for globule size, transparency, self-emulsification time, in vitro dissolution, and relative dissolution of the final formulation with marketed products and pure drug. Results: BLN shows highest solubility in (1:1) Captex 200P: Capmul MCM (oil), Tween 20 (surfactant) and Ethanol (cosurfactant). Trial batches were shows 1:9, 2:8 and 3:7 oil to surfactant and cosurfactant ratio suitable for optimization. Optimization using D-optimal mixture design gives 11 run batches and the result surface and contour plot suggest the best design space. The optimized formula given by mixture design of the target formulation had maximum drug solubility, maximum drug release, and minimum globule size. Optimized formula containing Blonanserin, Captex 200P: Capmul MCM (1:1) Mixture (23% v/v), Tween 80 (57% v/v), and Ethanol (20% v/v) having 94.72% in vitro diffusion within 30 min with 21 nm globule size. Optimized liquid SMEDDS have a higher invitro diffusion rate than marketed products and pure drug. Conclusion: Blonanserin liquid SMEDDS was successfully developed with high solubility, nano-globule size, and improvement in in vitro diffusion rate vice versa for improvement in bioavailability of the drug.
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Xin, Yang, Shi Yun, Lu Yuhe, Mao Yinxue, Niu Shurui, Zhou Yue, Qin Kunming i Li Weidong. "Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization". Frontiers in Nanotechnology 3 (18.11.2021). http://dx.doi.org/10.3389/fnano.2021.748791.
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In this research, we sought to surmount the poor dissolvability and transdermal absorption rate of licorice flavonoids (LFs) by fabricating a LFs microemulsion. LFs content was determined using high performance liquid chromatography. Initial studies such as dissolution testing, emulsification testing, and pseudo ternary phase diagram generation were implemented for screening components and optimized adopting the central composite design. While the tested responses were solubility, droplet size and PDI, thirteen trials were performed using two different variables, oil percentage and optimized emulsifier and co-emulsifier ratio. Microemulsions were then characterized for droplet size, PDI, transmission electron microscopy, viscosity, electrical conductivity, pH, entrapment efficiency, drug content and stability. Additionally, skin release profile, percutaneous absorption and retention were investigated adopting Franz diffusion cell. The optimal formulation was found to compose of laureth-9 (emulsifier, 6.72 g), propylene glycol (co-emulsifier, 1.80 g), isopropyl myristate (IPM, oil, 1.48 g), LFs (1.50 g) and at least more than 85% deionized water. The optimized and storage for 3 months of microemulsion was found to clear, light yellow color without phase separation or precipitation indicated the stability of the preparation to long-term placement. The mean droplet size, PDI, entrapment efficiency and drug content were discovered as 12.68 ± 0.12 nm, 0.049 ± 0.005, 97.28 ± 0.13% and 122.67 ± 0.40 mg·g−1, respectively. Furthermore, the optimal formulation sustained release LFs, remarkably deliver more LFs through the skin layer (644.95 ± 6.73 μg cm−2) and significantly retained LFs in the skin layer (9.98 μg cm−2). The study concluded that optimized microemulsion has potential and enhanced the dissolvability and cumulative penetration amount of LFs.
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Saab, May, Karim Raafat i Hoda El-Maradny. "Transdermal Delivery of Capsaicin Nanoemulgel: Optimization, Skin Permeation and in Vivo Activity Against Diabetic Neuropathy". Advanced Pharmaceutical Bulletin, 9.10.2021. http://dx.doi.org/10.34172/apb.2022.080.
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Purpose: Diabetic somatic neuropathy is one of the most prevalent complications in type 1 diabetes mellitus. Many treatments were investigated to alleviate the pain associated with this condition. Capsaicin is a naturally occurring lipophilic alkaloid that proved to be an effective and safe treatment of chronic painful disorders. Despite the known therapeutic benefits of capsaicin, the conventional topical formulations have limited bioavailability. Therefore, the current study aims to develop capsaicin nanoemulgel to increase skin permeation and enhance its activity against neuropathic pain. Methods: Low-energy emulsification method was used to prepare nanoemulsions, using eucalyptus oil as the oily phase, tween 80 as a surfactant, propylene glycol, ethanol and isopropyl alcohol as co-surfactants. Pseudo-ternary phase diagrams were constructed to investigate and optimize the formulation. Subsequently, the optimum formulation was formulated as a nanoemulgel and investigated for, skin permeation using Franz diffusion cell, and diabetic neuropathy management using alloxan-induced diabetic mice. Results: The selected nanoemulsion containing 0.05% capsaicin is composed of 8 % oil, 24 % Smix (Tween 80: isopropyl alcohol 2:1 w/w) and 68 % water. It is characterized by nanosized globules (28.15±0.24 nm) with a relatively low polydispersity index (0.27±0.05). The nanoemulgel revealed circa 4-fold increase in capsaicin cumulative permeation when compared to the conventional gel, and an improvement in its antinociceptive properties was observed in the treated diabetic mice (p<0.05). Conclusion: The selected capsaicin nanoemulgel would be a promising transdermal formulation that may alleviate diabetic neuropathy in type 1 diabetes mellitus patients.
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BINDHANI, SABITRI, SNEHAMAYEE MOHAPATRA i RAJAT KUMAR KAR. "PREPARATION, CHARACTERIZATION AND STABILITY STUDIES OF SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM OF NIFEDIPINE". International Journal of Applied Pharmaceutics, 18.02.2020, 94–102. http://dx.doi.org/10.22159/ijap.2020v12i2.36406.
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Objective: The objective of this work was to improve the solubility and dissolution rate of Nifedipine by preparing a solid-self micro emulsifying drug delivery system (Solid-smedds).
Methods: Liquid-self-emulsifying drug delivery system formulations were prepared by using linseed oil as oil, tween 80 as a surfactant and PEG 400 as cosurfactant. Components were selected by solubility screening studies and the self-emulsifying region was identified by the pseudo-ternary phase diagram. Thermodynamic stability study was performed for the determination of stable liquid-smedds formulation. These formulations were evaluated for self-emulsification time, drug content analysis, robustness to dilution test, particle size analysis, in vitro diffusion study, and Stability study. Solid self-micro emulsifying formulations were prepared by using aerosil-200 at a different ratio. Lf9S (0.65:1) was selected due to its highest drug entrapment efficiency and a decrease in particle size. It was selected for further studies into DSC, SEM, FTIR, and XRD analysis.
Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM study, it was observed that the drug has been uniformly distributed and having a smooth surface. From the in vitro dissolution study, it improved the dissolution rate of nifedipine which was 98.70% of drug release where pure drug release only 6.72%.
Conclusion: In conclusion, a solid self-micro emulsifying drug delivery system is improved the solubility and drug release rate but also improved the stability of the formulation.
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Prajapati, Bhupendra, Uma Patel, Chetna Modi i Prakash Kendre. "Nanoemulsion based In-situ Gel for ocular delivery of Brimonidine Tartrate". Current Drug Therapy 18 (26.06.2023). http://dx.doi.org/10.2174/1574885518666230626164030.
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Background: Brimonidine tartrate is currently used to treat glaucoma; however, conventional ocular formulations have some disadvantages in terms of treating disorders like glaucoma, as less than 5% of the drug reaches a posterior segment of the eye; hence, there is a need for sustained treatment. Objective: The objective of this study was to develop a self-nanoemulsion (SNEDDS) in-situ gel of brimonidine tartrate to investigate the sustained-release effect to improve ocular bioavailability. Method: Oil, surfactant, and co-surfactant were screened using the pseudo-ternary phase diagram (TPD) by aqueous-titration method based on the drug solubility. Nanoemulsions were evaluated for the pH, viscosity, % drug content, % transmittance, dispersibility, particle size, zeta-potential, TEM, and conductivity test. Nanoemulsion was incorporated into in-situ gel and evaluated for gelling capacity, pourability, gel strength, in vitro drug release study, and drug release kinetics. Result: Castor oil (10%) as oil phase, Acrysol K-140 (10%) as surfactant, and PEG 400 (20%) as co-surfactant were selected in preparation of SNEDDS from TPD. Evaluation parameters of SNEDDS were found in an acceptable range. % Drug release showed the controlled release up to 8 hrs. Optimum % drug content and % CDR were 100.25% and 92.46% after 12hrs, respectively. Optimized SNEDDS in-situ gel followed the Higuchi model via diffusion mechanism having 0.99 R² value and exhibiting sustained release up to 12 hr. Stability study proved no significant changes during storage. In vitro, the ocular irritancy test proved suitable for ocular delivery. Conclusion: A sustained-release formulation was obtained by developing brimonidine tartrate SNEDDS in-situ gel as a stable formulation without irritancy during ocular administration.