Abstract
In the current study, surface-modified poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) of brigatinib (BRB) were prepared by studying the variables PLGA (polymer), PVA (stabilizer) and chitosan (coater) against experimentally obtained responses. The optimized NPs (F2) were evaluated in vitro for differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), particle size, polydispersity index (PDI) and drug entrapment (EE), in vitro release, hematocompatibility and in vitro anticancer studies. The optimized NPs' (F2) composition, PLGA (75 mg), PVA (035% w/v), chitosan (0.75% w/v) and 30 mg of BRB was found to be optimum with particle size (406.3 +/- 5.1 nm), PDI (0.277), zeta potential (30.4 +/- 3.3 mV) and %EE (82.32%). The in vitro release profile showed a sustained release pattern of the F2 nanoparticles of BRB. The 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay revealed a significant anticancer activity for F2 NPs against A549 cell lines in comparison to free BRB. The result obtained in this work indicated the immense potential of nanoparticles to effectively deliver the BRB to the cancer site for the treatment of non-small cell lung cancer.