Physicochemical Characterization, Drug Release, Stability, and Cytotoxicity of Cross-Linked Curdlan-Based Nanosponges for α-Amyrin and Higenamine Delivery

INTRODUCTION: In this study, the primary goal was to establish the combined beneficial anticancer impacts of Nanosponges (NS) containing alpha-amyrin (AMY) and higenamine (HGN) on MCF-7 breast cancer cells. These cells are recognized for their resilience against conventional chemotherapy drugs and apoptosis-triggering agents. NS have emerged as promising drug delivery systems in cancer therapy due to their ability to encapsulate and deliver therapeutic agents efficiently.
METHODS: NS was developed utilizing a solvent evaporation technique that incorporated dichloromethane (DCM) as a crosslinker and curdlan as a polymer. A comprehensive randomized 3² factorial design was employed to vary curdlan content (X1) and stirring rate (RPM) (X2) to investigate their influence on particle size (Y1) and entrapment efficiency (Y2). Following this, the optimized formulation underwent in vitro investigations, encompassing evaluations of apoptosis and cell cycle study via the MCF-7 breast cancer cell line.
RESULTS: The prepared NS (F1-F9) exhibited optimal physical and chemical characteristics. The optimization process led to the development of formulation F10, which achieved a particle size of 280.9 nm and an entrapment efficiency(EE) of 63%. In vitro cell line study of prepared NS demonstrated promising anti-cancer activity, showing that the combination of AMY and HGN had synergistic anticancer effects compared to AMY alone which significantly influenced the cell cycle of MCF-7 cells, leading to cell cycle apprehension in the G1 phase and reduced cell propagation by flow cytometry analysis.
DISCUSSION AND CONCLUSION: The synergistic anticancer activity observed with AMY and HGN nanosponges, along with sustained drug release properties and modulation of the cell cycle in MCF-7 cells, underscores the value of this combination as a promising approach for more effective cancer treatment.