Preparation and characterization of raloxifene proniosomes using sorbitan esters

Abstract

A 2nd-generation selective oestrogen receptor modulator, raloxifene HCl (RLX-HCl) is a non- steroidal benzothiophene that binds to oestrogen receptors. While administer orally due to its extensive first pass metabolism in gut, it possess only 2% absolute bioavailability. In this present work, RLX-HCL was formulated as proniosomes by slurry method, where different ratios of surfactant and cholesterol were used for preparation and evaluating study. The shape of prepared RLX-HCl loaded proniosomes were spherical with an average particle size of 690nm with a high encapsulation efficiency of 83.64%. The study revealed that in 24h, formulation RS606 had the highest cumulative drug release (99.42%). From the stability study, 5°C was identified as the suitable temperature for the optimized proniosomes. In conclusion, an improved bioavailability and prolonged drug release profile of the proniosome formulation seems to be a promising delivery system for RLX-HCl.