DEVELOPMENT OF EFAVIRENZ LOADED PRONIOSOME FORMULATION FOR ENHANCED ORAL BIOAVAILABILITY: AN INVITRO AND IN-VIVO STUDY

Abstract

In the present investigation, proniosome of Efavirenz were formulated, optimized and evaluated for effective oral
delivery in order to overcome the bioavailability issues of orally administered Efavirenz. The proniosome were
prepared using a blend of Span-60, cholesterol and maltodextrin and were evaluated for in-vitro parameters, ex-vivo
permeation and in-vivo performance. Results indicated that the vesicles were spherical in shape, their size ranged from
284.00 nm to 941.40 nm and they had high zeta potential. The entrapment efficiency for spans was higher compared
to tweens. DSC and IR studies confirmed the absence of chemical interactions between the Efavirenz and proniosome
components. In-vitro release study showed that formulations with spans exhibit controlled release profile and followed
the Higuchi model. No significant change in vesicle size and entrapment efficiency was observed when the
proniosomes were stored at 4 ± 1 °C and 25 ± 2 °C for three months. Proniosomes with span 60 showed no signs of
erythema or edema and has highest flux across the rat skin (169.851 ± 2.13 μg cm−2 h−1 ). The relative bioavailability
was 92% after transdermal administration of proniosomes and the tmax was increased to 8 h. So we conclude that the
developed proniosome formulation would be a promising alternative to improve the bioavailability problems of
Efavirenz.