Active-targeting docetaxel-loaded mixed micelles for enhancing antitumor efficacy

Abstract

Active targeting agents can identify patients with receptors overexpressed on the surface of cancer cells. The selective and efficient drug delivery to tumor cells can remarkably improve different cancer therapeutic effect. Folic acid (FA) conjugation is a facile approach for targeting folate receptor-expressing tissues for personalized treatment. In the present study, ethoxy poly(ethylene glycol)- folic acid (FA-PEG) is introduced as the potent targeting moieties in docetaxel (DTX)-loaded micelles. The spherical FA-PEG/PEO–PPO–PCL mixed micelles revealed a narrow distributed size at 106.1 ± 0.3 nm. The low critical micelle concentration (CMC) of the mixed micelles (about 3.8 μg mL−1) indicated the excellent self-assembly ability in water and predominant stability against dilution in the circulation. The in vitro drug release of DTX in micelles presented a controlled and sustained release pattern. Moreover, in vitro cytotoxicity results showed the FA-PEG/PEO–PPO–PCL micelles exerted higher cytotoxicity compared with PEO–PPO–PCL micelles on FR-positive MCF-7 cells. Cellular uptake studies clearly demonstrated that FA-PEG micelles were more efficiently accumulated in MCF-7 cells via FRs mediated endocytosis. Therefore, the prepared FA-PEG/PEO–PPO–PCL micelles can provide a promising tumor-targeting drug delivery system for efficient cancer therapy.