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

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• DOI10.5530/jyp.20250155Copy

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