Objective: The objective of the selected study was to design and formulate simvastatin-loaded pharmacosomes and then incorporate into a transdermal patch by solvent evaporation technique to enhance the solubility, bioavailability, and half-life of simvastatin. Methods: Simvastatin comes under the BCS-II class, which has low solubility and high permeability. Simvastain loaded pharmacosomes of six different formulations were prepared by taking simvastatin and soya lecithin in varying ratios and dissolved in a high polarity solvent dichloromethane and then subjected to the solvent evaporation method. Results: Formulated simvastatin-loaded pharmacosomes (SLP) were subjected to evaluation; out of six formulations, optimized formulation (F3) shown in vitro drug release of 86.88%; particle size of 151.6 nm with zeta potential of-16.5mV, which indicates good stability. SEM studies confirmed their smooth, porous structure with a number of nano-channels. The FT-IR spectra and DSC showed a stable character of simvastatin in a mixture of lipid and solvent shows compatible and revealed the absence of drug polymer interactions. The SLP was loaded into a transdermal patch by solvent evaporation method and evaluated for physical characteristics and results were found to be patch surface pH 6.15±0.08, thickness 0.146±0.0096 mm, weight uniformity 1.12±1.73, % swell-ability 13.50±0.028 for best patch formulation (F3). Conclusion: This research paper gives an outline on the significance of simvastatin-loaded Pharmacosomes as a transdermal patch for enhancing trans-permeation through the skin and its characterization and results. Through obtained results, it is concluded that pharmacosomes is a promising carrier to enhance the permeation of the selected drug through skin.
Objective: The objective of the selected study was to develop and statistically optimize fluconazole (drug) loaded pharmacosomes (carrier) to enhance transdermal permeation by incorporating into gel base and to treat fungal infections by selecting the Box-Behnken model. Methods: Fluconazole is an antifungal drug which belongs to BCS class-II with high permeability and choice for topical drug delivery. In the study, the levels of the lecithin (lipid), dichloromethane and DMSO are selected as independent variables were varied to study the influence on particle size, % entrapment efficiency and in vitro drug release as dependent variables. Factorial designs through software Design expert version 13 (Box-Behnken design) is applied for this study and the optimization process was carried out using the desirability plots and point prediction techniques. Results: Results of the study with the application of a design expert shows that the optimized drug-loaded pharmacosomes with vesicle size of 158.87±0.56 nm as predicted and zeta potential of-30.6mV indicating good stability of the formulation, entrapment efficiency of 90.6±1.12% and in vitro drug release of 97.59±1.84% respectively. The optimized formulation loaded into gel base and compared with the marketed gel formulation. All the evaluation parameters confirmed that the physical mixture of drug and excipients was compatible without any interactions. Conclusion: Through obtained results, it’s concluded that; the independent variable plays a crucial role in optimizing formulation. Study data provided strong evidence that the optimized vesicular formulation through Box-Behnken factorial design can be potentially useful as a drug carrier for loading drug of selected category for enhancing transdermal delivery.
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