Design and Development of Chitosan Based Etravirine Nanosuspension

Objective(s): The objective of this study was to design, develop, optimize, and evaluate Chitosan based Etravirine Nanosuspension to enhance their solubility and extent of release.
Methods: The Chitosan based Etravirine Nanosuspension was formulated by the modified solvent evaporation combined ionic cross-linking method and it was optimized through design of experiments (Box-Behnken Design). The impact of Drug, Chitosan and Sodium Tripolyphosphate concentration on the drug release, particle size and drug entrapment efficiency were evaluated. The optimized Nano formulation were characterized using, Zetasizer, Transmission electron microscopy, X-ray diffractogram and saturation solubility study.
Results: The three level, three factor response surface design was applied in design of experiments which yields regression equations for individual responses against composition variables to arrive a design space to produce nanosuspension constantly with desired attributes. Among the trials conducted, the Batch # F6 exhibits optimal results in various parameters like particles size (226 nm), poly dispersity index (0.2), zeta potential (+30 mV), 92 % of drug release and 80 % entrapment efficiency. The saturation solubility of Batch # F6 was enhanced to about 22 times (89.19±2.56 μg/ml) of pure crystalline drug moiety (4.02±0.03 μg/ ml).
Conclusions: Etravirine, an antiretroviral drug with poor bioavailability has several constraints like lipophilicity, low permeability, crystallinity and first pass metabolism. Hence, Etravirine loaded chitosan based nanosuspension was formulated and considerably improved the solubility and drug release profile. This Nanosuspension could ease the oral administration and facilitate the absorption of Etravirine to attain enhanced bioavailability.