Preparation and Evaluation of mPEG-PLGA Block Copolymer Micelles Loaded with a Sarsasapogenin Derivative

Sarsasapogenin derivative 5n (SGD 5n) is a new compound with potent antitumor efficacy, but the low solubility severely affects its absorption and bioavailability. Therefore, the SGD 5n-loaded mPEG-PLGA block copolymer micelles were developed to improve the value of SGD 5n in clinical application. The polymeric micelles were prepared by an organic solvent evaporation method, and the encapsulation efficiency (EE), drug loading (DL), critical micelle concentrations (CMC), morphology, particle size, and zeta potential were determined. The cytotoxicity was examined by the MTT assay, and the cellular uptake study was performed by confocal laser scanning microscopy. A model of tumor-bearing mouse was established to study the antitumor activity in vivo. The results demonstrated that the particle size of the prepared micelle was 124.6 ± 9.6 nm, the encapsulation efficiency was 82.0 ± 2.9%, and the drug loading was 8.3 ± 0.4%. The results of cytotoxicity and cellular uptake demonstrated that the SGD 5n-loaded micelles could efficiently enter tumor cells, and the cellular uptake of SGD 5n presented concentration and time dependence. This study demonstrated that the prepared SGD 5n-loaded polymeric micelles had significant antitumor activity and provided a basis for clinical development of new compound SGD 5n.