Development Optimization and Characterization of Ethosomes and Transfersomes of Curcumin for Skin Cancer Treatment via the Transdermal Route

Abstract

newlineBackground newlineABSTRACT newlineCurcumin (Cur) is a hydrophobic polyphenol that exhibits diverse pharmacological newlineactivities, including anti-cancer effects. However, the oral bioavailability of curcumin newlineis severely limited due to its poor aqueous solubility, extensive first pass metabolism newlineand stability problems. newlineObjectives newlineThe main objective of the present study is to develop, statistically optimize and newlineevaluate ethosomes and transferosomes of curcumin and compare their therapeutic newlineusefulness in treating melanoma via the transdermal route. newlineMethodology newlineThe curcumin loaded ethosomes and transfersomes were prepared by cold method and newlinethin film hydration method respectively. A 3 newlinexviii newline newline2 newline factorial design was used for the newlineoptimization of the nanovesicular formulations (ethosomes and transfersomes) using newlineDesign-Expert® software. The prepared formulations were characterized for vesicle newlinesize, size distribution, shape, zeta potential, entrapment efficiency, and in vitro skin newlinepermeation and deposition studies. The optimized ethosomal and transferosomal newlineformulations were subjected to in vitro skin penetration and in vitro cell culture newlinestudies. Finally, the optimized nanovesicular formulations were incorporated into newlinecarbopol® 980NF and characterized for pH, viscosity, spreadability, drug content, in newlinevitro skin permeation and deposition, histopathological examination and stability newlinestudies. newlineResults newlineThe optimized ethosomes and transfersomes were found to be spherical and newlineunilamellar in structures having nanometric size range with narrow size distribution, newlineand high entrapment efficiency. The optimized formulations of curcumin loaded newlineethosomes and transfersomes showed significant skin permeation and deposition in newlinethe skin layers when compared to drug loaded traditional liposomes and ethanolic newlinephosphate buffer saline. The fluorescence microscopy study using rhodamine 6G newlineconfirmed the enhanced penetration of the ethosomes and transfersomes in the deeper newlinelayers of skin. The results of differenti