Optimized Transethosomal Carrier of Psoralen for Enhanced Topical Psoriasis Treatment: In-vitro, In-vivo, and Stability Evaluation

Abstract

Background: The optimized transethosomal (TE) formulation of the psoralen was developed using statistical design of experiment tool for its effectiveness against psoriasis.
Material and Methods: Psoralen-encapsulated transethosomes were prepared by “cold method.  With due diligence, the selected Critical process parameters were concentration of lipid, surfactant & ethanol; temperature and stirring. The design of experiment was planned using half fraction design with 2 blocks. The targeted critical attributes of quality were vesicle size & deformability, zeta potential, entrapment efficiency. The optimized formulation was evaluated for the in vitro release profile utilizing the Franz’s diffusion cell and further evaluated for antipsoratic activity in vivo Imiquimod induced animal model of psoriasis.
Results: In case of vesicle size the impact of D i.e. temperature and square of C (Ethanol Conc.), D and E (Stirring rate) were significant (<0.05) while overall lack of fit was significant. Whereas, in the case of zeta potential A (PC Conc.) was only significant parameter with insignificant lack of fit. The optimized formulation was characterized with FTIR, Transmission electron microscopy and zeta potential. In vitro drug penetration study expressed that TE-psoralen 68.32 ± 4.87 % release without saturation even after 24 h which was more than psoralen free with saturation. In vivo and ILs expression studies were in parallel with enhanced release results and expressing the efficacy of TE-Psoralen 50 µM equivalent to free psoralen 1 mM concentration.
Conclusion: TE-Psoralen produced were having good stability, higher deformability thus efficacy for skin related indication.