Design, Characterization, and Anti-Cancer Activity Evaluation of Palbociclib-Loaded Nanosponges in A498 and Mcf-7 Cell Models

Abstract

Objective: To formulate and evaluate palbociclib-loaded nanosponges (PB-NSPs) as a controlled drug delivery system to improve the solubility, stability, and release behavior of palbociclib for cancer therapy. Methods: PB-NSPs were prepared using β-cyclodextrin (β-CD) and characterized for particle size, zeta potential, encapsulation efficiency, and morphology. Cytotoxicity was evaluated by MTT assay against MCF-7 and A498 cell lines. In vitro drug release studies were performed to assess the release characteristics of the formulation. Results: The optimized PB-NSPs exhibited a particle size of 149.7±2.6 nm, zeta potential of −23.6±2.16 mV, and encapsulation efficiency of 77.33±2.82%. Cytotoxicity studies demonstrated concentration-dependent reduction in cell viability. Pure palbociclib showed IC₅₀ values of 43.168 µg/ml in MCF-7 cells and 58.11 µg/ml in A498 cells, whereas PB-NSPs showed IC₅₀ values of 54.054 µg/ml and 63.77 µg/ml, respectively. Although PB-NSPs exhibited slightly higher IC₅₀ values than the pure drug in the 48 h assay, the formulation demonstrated sustained drug release and favorable physicochemical properties. Conclusion: PB-NSPs demonstrated desirable physicochemical characteristics and controlled release behavior, indicating their potential as a promising nanosponge-based drug delivery system for prolonged and targeted delivery of palbociclib in cancer therapy.