Pharmacokinetic and Pharmacodynamic Evaluation of Novel Drug Delivery Systems for Enhanced Bioavailability of Anticancer Agents

Abstract

Cancer remains a leading cause of death worldwide, with conventional chemotherapy often limited by poor bioavailability, rapid clearance, and systemic toxicity. This study evaluated the pharmacokinetic (PK) and pharmacodynamic (PD) performance of three novel drug delivery systems — liposomes, polymeric nanoparticles, and polymeric micelles — for selected hydrophobic anticancer agents. Formulations were prepared using thin-film hydration, emulsion-solvent evaporation, and self-assembly methods, respectively. In vitro release, encapsulation efficiency, in vivo pharmacokinetics, tumor accumulation, and therapeutic efficacy were systematically assessed in tumor-bearing animal models.
Results showed that all novel delivery systems significantly improved encapsulation efficiency, sustained release, systemic exposure (AUC and half-life), tumor targeting, and tumor growth inhibition while reducing toxicity compared to free drug. Liposomes demonstrated the most favorable overall profile with superior tumor accumulation and therapeutic efficacy, followed closely by polymeric nanoparticles. Polymeric micelles provided good solubility enhancement but showed faster release and lower toxicity reduction.
These findings highlight the potential of advanced drug delivery systems to overcome bioavailability limitations of anticancer agents and support their further development for safer and more effective chemotherapy.