Exploration of using α-crocin for drug encapsulation and delivery

Abstract

Facile and efficient drug loading and delivery strategies hold paramount importance in the development of advanced pharmaceutical formulations, enhancing both the efficacy and accessibility of treatments. In this study, we successfully prepared dimethylcurcumin (DMC)-loaded α-crocin nanoparticles with varying drug loadings (15.2 % and 21.7 %) using a solvent diffusion method, which exhibit excellent lyophilization stability, relatively small and uniform particle sizes. DMC is encapsulated in an amorphous state within α-crocin nanoparticles, forming strong π-π stacking interactions. Dissipative particle dynamics simulations and transmission electron microscope images confirm the core-shell structure, with DMC aggregates forming the cores and α-crocin coating the surfaces. The drug loading studies on various drugs with different structure and properties show that hydrophobic drugs with π-conjugated systems and planar structures can be efficiently encapsulated with α-crocin. The nanoparticles exhibit sustained drug release in pH 7.4 and pH 5.0 conditions and demonstrate enhanced antitumor activity in vitro compared to free drugs, with DMC@α-Crocin (15.2 %) nanoparticles showing superior performance due to higher cellular uptake. Pharmacokinetic study reveals prolonged blood half-life and increased area under curve for DMC@α-Crocin (15.2 %) nanoparticles, indicating improved drug delivery. This work validates the potential of α-crocin-based drug encapsulation for enhanced cellular uptake, antitumor activity, and prolonged blood circulation, providing new insights into the development of efficient drug delivery system.