Formulation, Central Composite Design Optimization and in vitro Evaluation of Folic Acid Conjugated Palbociclib Loaded Polymeric Nanoparticles

Abstract

Background: The efficacy of the anticancer agent palbociclib can be limited by its conventional release profile. Developing nano-formulations presents a viable approach to modulate its delivery for improved therapeutic outcomes. This work aimed to design, optimize, and characterize chitosan-based Polymeric Nanoparticles (PNs) for the oral delivery of palbociclib, with a specific focus on controlling particle size and surface charge.Materials and Methods: Palbociclib-loaded PNs were fabricated using a solvent evaporation technique. A Central Composite Design was employed to optimize the concentrations of chitosan and Polyvinyl Alcohol (PVA). The lead formulation was thoroughly characterized using FT-IR, SEM, and in vitrorelease studies, with its release kinetics modelled.Results: An optimized formulation was identified with a particle size of 337.8 nm and a zeta potential of 32.4 mV, which aligned closely with statistical predictions. The system exhibited high drug entrapment (81.28%) and provided a sustained release profile, with 90% of the drug released over 26.1 hr following a diffusion-erosion mechanism. This was a substantial extension over the rapid release of the pure drug.Conclusion: The findings confirm the successful development of a chitosan-based nanoparticle system capable of offering sustained release of palbociclib, highlighting its significant potential for enhancing oral drug delivery in cancer treatment.

Keywords: Chitosan; Drug release; Folic Acid; Kinetics Palbociclib; Particles Size; Particles Charge