Development, characterization and in vitro evaluation of docetaxel-loaded polymeric micelles / 中国药学杂志

ABSTRACT

OBJECTIVE: To employ PEG-PCL diblock copolymers to prepare DTX-loaded polymeric micelles (PEG-PCL-DTX micelles, DTX-PMs) which addressed the issue of DTX's drug loading capacity, encapsulation efficiency and in vitro release. We also studied its effectiveness for the cytotoxicity on prostate cancer. METHODS: The polymeric micelles were screened by its shape using transmission electron microscope and were also characterized in terms of particle size, Zeta potential, drug loading efficiency, in vitro release and cytotoxicity by using laser particle size analyzer and HPLC. Cytotoxicity against LNCap-C4-2B prostate cancer cells of the DTX-PMs and commercial product of Duopafei® were evaluated by MTT assay. RESULTS: The average particle size and Zeta potential of DTX-PMs were found to be 25.1 nm and 0.64 mV. The micelles' drug loading and encapsulation efficiency were 8.72% and 98.1%, respectively. Cytotoxicity assay showed that DTX-PMs exerted significant anti-proliferation activity on LNCap-C4-2B prostate cancer cells. CONCLUSION: Slightly soluable DTX successfully formulated into the PEG-PCL micells, exhibiting small partical size and good stability. Delayed release in vitro and maintained quite a constant concentration in plasma for a long period, which was favorable for its clinic application. In conclusion, DTX-PMs developed here sufficiently solubilized DTX and increase the concentration of DTX in aqueous phase, offering a sustained in vitro release and effective cytotoxicity on LNCap-C4-2B prostate cancer.