Preparation, Characterization and Optimization of Maltodextrin based Efavirenz loaded Proniosomes using Box Behnken Design: In vitro and ex-vivo permeation study

Abstract

This research work focuses on development of proniosomal efavirenz (EFV) formulation using maltodextrin as a carrier. Thus an effort is made to increase the effectiveness of oral drug delivery of EFV by blending them in proniosomal powders (maltodextrin-based). The slurry method was employed for the preparation of proniosomes. A mix of Span-60, cholesterol and maltodextrin were used for its preparation..Box Behnken Design used to study the effect of independent variables X1, X2, and X3 (maltodextrin, Span-60 and cholesterol) on response variables Y1, Y2 and Y3 (Entrapment efficiency ,Vesicle size and Cumulative Drug Release percentage). Scanning Optical electron microscopy was used for studying surface-morphology of proniosome (optimized) and proniosome formation. To study any drug interaction or its conversion to the molecular and amorphous state from crystalline state, various tests like differential scanning calorimetry and FT-IR were performed. Compared to EFV in pure form, the proniosomalmaltodextrinbaseddrug showed better dissolution 98.41% in vitro-dissolution study. The optimized Efavirenz loaded proniosomal formulation showed maximum permeation (2614±215µg) in rat intestine as compared to pure drug(1500±114µg). The effectiveness of this drug (oral delivery) is obvious from the fact that rat intestine drug permeation is better. This shows maltodextrin-based EVF proniosomal formulation is suitable for oral delivery of efavirenz.