DESIGN, PREPARATION AND OPTIMIZATION OF CABAZITAXEL POLYMERIC NANOPARTICLES

The present study was aimed at the design, preparation, and optimization of Cabazitaxel-loaded PLGA polymeric nanoparticles using the nanoprecipitation method to improve drug encapsulation, provide sustained drug release, and enhance formulation stability. Cabazitaxel-loaded polymeric nanoparticles were prepared using poly(lactic-co-glycolic acid) (PLGA) as the biodegradable polymer and polyvinyl alcohol (PVA) as the stabilizer. Eight formulations (F1–F8) were developed by varying the polymer concentration while maintaining a constant drug concentration. The prepared nanoparticles were evaluated for particle size, zeta potential, entrapment efficiency, surface morphology, in-vitro drug release, release kinetics, and stability. The particle size of the formulations ranged from 226 to 362 nm, while the zeta potential varied between −21 and −31 mV, indicating good colloidal stability. Drug entrapment efficiency ranged from 79.83% to 89.23%. SEM analysis of the optimized formulation confirmed the formation of spherical, smooth, and uniformly distributed nanoparticles with minimal aggregation. In-vitro drug release studies demonstrated a biphasic release pattern consisting of an initial burst release followed by sustained release over 12 hours. Among all formulations, F5 exhibited the most desirable characteristics, with a particle size of 226 nm, entrapment efficiency of 89.23%, and cumulative drug release of 98.05%. Drug release kinetic analysis revealed that the optimized formulation best fitted the Higuchi model (R² = 0.978), indicating diffusion-controlled drug release from the PLGA matrix. Stability studies performed under long-term and accelerated storage conditions for three months showed no significant changes in drug release, confirming the stability of the optimized formulation. The study concludes that PLGA-based polymeric nanoparticles prepared by the nanoprecipitation method are an effective carrier system for Cabazitaxel, providing high drug encapsulation, nanosized particles, sustained drug release, and good physicochemical stability. The optimized formulation has the potential to improve the therapeutic efficacy of Cabazitaxel while reducing dosing frequency and systemic toxicity. Keywords: Cabazitaxel, Polymeric nanoparticles, PLGA, Nanoprecipitation, Controlled drug release, Entrapment efficiency, Anticancer drug delivery.