FORMULATION AND EVALUATION OF SOFT GELATIN CAPSULES OF NELFINAVIR MESYLATE
Jyothirmayee Devineni ? and Vijaya Ratna
ABSTRACT
The present investigation was undertaken with the objective of enhancing the bioavailability of
nelfinavir mesylate (NLF), a HIV protease inhibitor through the preparation of liquid fill formulations for soft
gels. Liquid fill formulations for NLF (250mg) soft gels were prepared using excipients such as solubility
enhancer (Tween 80), viscosity modifier, polyvinylpyrrolidine (PVP K -30), p-gp efflux inhibitors and
hydrophobic vehicle, poly ethylene glycol 400 (PEG 400),hydrophilic vehicle(9:1 ratio of ethyl alchohol and
water).The prepared formulations were evaluated for appearance, pH, content uniformity, water migration,
viscosity, drug-excipient compatibility and in vitro drug release parameters. Optimized formulation was further
subjected to bioavailability studies in rabbits. Stability of the optimized formulation was evaluated by storing for
six months, at 400 C and 75% RH. Among all the prepared formulations, formulation F2 containing 10% PVP k-30
and 10% Tween 80 showed superior % drug release (99.94% ± 0.64 within 4 min) with appreciable physical and
chemical stability. Comparative bioavailability studies were carried out on formulation F2 and NLF suspension.
Formulation F2 showed better relative bioavailability than that of NLF suspension. The results of this study
provide guidance for developing soft gel capsule of NLF that give greater bioavailability, than existing dosage
forms, and provide protection against p-gp efflux. The proposed techniques are economical, convenient and safe.
Keywords: In vitro dissolution, in vivo bioavailability, P-gp efflux, Soft gels, stability, viscosity.
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