Formulation And Development Of Nanosuspension For Solubility Enhancement Of Gefitinib

Abstract

Gefitinib (GFT) is a BCS class II tyrosine kinase inhibitor with limited solubility and bioavailability. In the present investigation, nanosuspensions (NSPs) were formulated to overcome these pitfalls. The GFT-NSPs nine batches were prepared by nanoprecipitation method using Poloxamer-188 (Polo-188) and Tween-80. The developed formulations were subjected to determine percent drug content, percent drug entrapment, particle size, polydispersity index, zeta potential, x-ray diffraction pattern, formulation morphology, solubility and in vitro drug release. Following the percent drug content and entrapment, NSP-6 was selected as an optimized batch. In the study's outcomes, it was observed that NSP-6 showed 96.71 percent drug content and 96.61 percent drug entrapment. In particle size analysis, NSP-6 explored 357.6.4 nm dimensions, 0.325 polydispersity index and -26.5 zeta potential. X-ray diffractogram of NSP-6 indicated characteristics peak of both GFT and Polo-188. Morphological photomicrographs of NSP-6 explored small spherical structures. In the solubility study, it was observed that NSP-6 showed higher solubility enhancement than pure GFT in purified water, methanol and pH 7.4 phosphate buffer. In vitro dissolution study of pure GFT and NSP-6 exhibited 97.23% and 99.14% drug dissolution. NSP showed a maximum drug dissolution rate; therefore, NSP was considered a suitable approach for the solubility enhancement of GFT. The developed NSP significantly increased the water solubility and bioavailability of GFT, suggesting its potential as a nanocarrier in the delivery of GFT for future clinical application.