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Development and Characterization of Clobetasol Propionate Loaded Squarticles as a Lipid Nanocarrier for Treatment of Plaque Psoriasis.

JOURNAL OF MICROENCAPSULATION(2020)

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摘要
Aim: The aim of this project is to improve the therapeutic effectiveness, permeation and retention of clobetasol propionate in sebaceous glands by reporting the use of Squarticles as lipidic nanosystem. Methods: Homogenisation method is used for the formulation of Squarticles (nanoemulgel) which was characterised on the basis of size, polydispersity index (PDI), viscosity, spreadability, DSC, % in vitro release, in vitro skin permeation deposition studies, and in vivo studies, scanning electron microscopic (SEM) and physical storage stability studies were done at different temperature conditions, i.e. 4 +/- 2 degrees C, 25 +/- 2 degrees C and 45 +/- 2 degrees C for a period of 6 months for drug and formulation. Result: The morphological characterisation of prepared nanoemulsion shows small spherical shape and uniform size distribution as observed in the Scanning electron microscopic (SEM), having mean size (240.5 +/- 9.2) and mean size distribution (0.282 +/- 0.03) and zeta potential (-51.21). The drug release from optimised nanoemulsion (F2) in PBS (pH 5.5) was approximately 84.24 +/- 1.35%, nanoemulgel formulations showed the release of 66.83 +/- 2.05% while marketed gel showed the release of 57.67 +/- 1.63% after 24 h. The cumulative percentage retention of clobetasol propionate loaded nanoemulgel was 63 +/- 1.28% which was more than the marketed formulation (23.12% +/- 0.54). Physical stability studies show that formulation is more stable in cold condition. Further, the stability of active ingredient in gel formulation was determined using HPLC which shows around 15 +/- 0.84% of loss in its activity. Conclusion: The present work has demonstrated the use of Squarticles as a novel carrier for treatment of plaque psoriasis by enhancing the better permeation, increasing skin retention, and enhances the effect of drug. The study also shows that the formulation is more stable in cold condition
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关键词
Nanoemulgel,nanoemulsion,sebaceous gland,Squarticles,permeation,deposition
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