Self-assembly micelles with lipid core of cholesterol for docetaxel delivery to B16F10 melanoma and HepG2 cells

Abstract

The objective of the present study was to prepare a micellar polymeric carrier for the delivery of Docetaxel (DTX) as a kind of polysorbate free preparation. Pluronic F127 (PF127) was conjugated to cholesterol (Chol) via succinyl linkage and characterized by FTIR and HNMR. DTX-loaded polymeric micelles were prepared via film hydration method. Physicochemical properties of micelles including particle size, zeta potential, drug loading and release efficiency were studied. The critical micelle concentration (CMC) was determined using pyrene as a hydrophobic fluorescent probe. In vitro cytotoxicity of micelles was evaluated in B16F10 melanoma cells and HepG2 cell line. The FTIR and HNMR spectroscopy methods confirmed the conjugation of PF127 to cholesterol via succinyl linkage. The micelles were spherical under scanning electron microscope (SEM) with the mean particle size of 248.2 ± 8–278.8 ± 12.3 nm and zeta potential ranging from −17.2 ± 8.7 to −28.4 ± 12.7 mV. Drug loading efficiency was higher than 98%. The in vitro release study showed the sustained release behavior of DTX within 144 h. The CMC of the micelles was about 41.67 ± 0.17 µg/ml, which was significantly lower than the CMC of pure PF127 micelles. Compared with the free drug, DTX-loaded micelles showed higher cytotoxicity against B16F10 melanoma and HepG2 cell lines.