Abstract :
The objective of this study was to develop and characterize a Nano formulation of Pazopanib using poly(DL-lactide-co-glycolide) (PLGA) for improved bioavailability and reduced systemic toxicity. Pazopanib, a tyrosine kinase inhibitor used in the treatment of renal cell carcinoma and soft tissue sarcoma, exhibits limited solubility and bioavailability, restricting its clinical efficacy. We employed an oil-in-water (o/w) emulsion solvent evaporation technique to prepare Pazopanib-loaded PLGA nanoparticles. Various formulations were optimized by adjusting the drug-to-polymer ratio, yielding spherical nanoparticles with an average size of 135 nm and a low polydispersity index, as confirmed by dynamic light scattering and transmission electron microscopy. The nanoparticles demonstrated a high entrapment efficiency of 33.9 ± 2.5% and a zeta potential of -20.12 mV, indicating good colloidal stability. Fourier transform infrared spectroscopy confirmed the compatibility of Pazopanib with PLGA and other excipients. The in vitro drug release studies revealed a sustained release profile over 7 days, contrasting with the rapid release from the free drug solution. These findings suggest that the developed PLGA-based nanoparticulate system could potentially enhance the therapeutic efficacy of Pazopanib by increasing its bioavailability and ensuring controlled release, thus offering a promising approach for cancer chemotherapy.
Keyword :
PLGA, DMSO, Transmission electron microscopy (TEM)