In-vitro and Ex-vivo evaluation of Raloxifene hydrochloride delivery using nano-transfersome based formulations

Abstract

Osteoporosis has remained a leading cause of reduced bone mineral density in post-menopausal women. Raloxifene hydrochloride is a selective oestrogen receptor modulator (SERM) drug which shows beneficial effects in the treatment of osteoporosis. Limited bioavailability of RLX prevents its application as an anti-osteoporotic. The aim of this study was to develop and evaluate Raloxifene hydrochloride (RLX) loaded transfersomes, a modified liposome based delivery for transdermal application. RLX loaded transfersomes were prepared by thin film hydration technique and characterized using different techniques like optical microscopy, dynamic light scattering, zeta potential and entrapment efficiency. Transdermal formulations of transfersomes like Cream, Patch and Gel were compared for permeation characteristics. Ex vivo skin permeation studies were performed using male Wistar rat skin and release profiles were modelled using different mathematical models for drug release. The results indicate that the composition of transfersomes play an important role in affecting the efficiency of transdermal RLX delivery. Incorporation of anionic surfactants such as sodium deoxycholate (SDC) and sodium cholate (SC) in the liposomes gave flexibility to bilayer of carriers making them permeable to pass through the skin. Release of RLX was prolonged for 48 h following Higuchi kinetics from transferosome formulations. Transferosome suspension was found to have a better permeation profile from skin obtained from rats to an extent of 77.9% at the end of 48 h. Patch and Gel formulations released the drug with a lag time in comparison to RLX transfersomes. RLX loaded transfersomes prove to be interesting avenues for transdermal delivery to provide controlled release for drugs with poor bioavailability. © 2018 Elsevier B.V.