Design and Development of Simvastatin-Loaded Pharmacosomes to Enhance Transdermal Permeation

Abstract

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.

Central Composite Face-Centered Design-Based Optimisation, Development and Characterisation of Favipiravir-Loaded Plga Nanoparticles

“…The low magnitude of relative error, less than±2%, confers the robustness and predictability of software in preparing the stable Favipiravir-loaded PLGA nanoparticles [38,44]. This result indicated that there was no interaction between favipiravir and polymers during the preparation of favipiravirloaded PLGA nanoparticles [22,24].…”

“…The morphological characteristics of the favipiravir-loaded PLGA nanoparticles were determined by performing analysis using scanning electron microscopy (FEI Quanta 250 FEG, USA). For SEM analysis, favipiravir-loaded PLGA nanoparticles were positioned onto a brass stub and sputtered with gold using gold coating-Quorum, later fixed into a sample holder, then examined under low vacuum (1023 mm HG) and photographed randomly [24].…”

“…Korsmeyer peppas model of optimised formulation FNP021 showed good linearity with a regression coefficient (R 2 ) of 0.995 and a diffusional exponent "n" value of 0.690, indicating an anomalous non-fickian diffusion mechanism, in which favipiravir is released by diffusion and relaxation of polymer occurs simultaneously. The favipiravir release from nanoparticles follows first-order kinetics with non-fickian diffusion [24].…”