Preparation of amentoflavone‐loaded DSPE‐PEG2000 micelles with improved bioavailability and in vitro antitumor efficacy

Abstract

AbstractTo overcome the poor aqueous solubility and enhance the anticancer effects of amentoflavone (AF), a nontoxic and biodegradable amphiphilic copolymer, poly(ethyleneglycol)‐distearoylphosphatidylethanolamine (DSPE‐PEG2000), was introduced to prepare AF micelles using the thin‐film hydration method. Amentoflavone was successfully encapsulated into the core, achieving an encapsulation efficiency of 98.80 ± 0.24% and a drug loading efficiency of 2.96 ± 0.12%. The resulting micelles exhibited a spherical shape with a particle size of approximately 25.99 nm. The solubility of AF was significant improved by 412‐fold, and cumulative drug release studies showed that AF release was much faster from the micelles compared with the free drug. The release of AF was sustained over time and followed a degradation‐based kinetic model, similar to polymeric systems. After oral administration, the AF‐loaded micelles demonstrated an enhanced oral bioavailability, which was 3.79 times higher than that of free AF. In vitro evaluations of the micelles’ antitumor effects revealed a significantly greater efficacy compared with free AF. These findings highlight the tremendous potential of DSPE‐PEG2000 micelles as a drug delivery carrier for improving the solubility and therapeutic efficacy of AF.