Cholic acid-functionalized nanoparticles of star-shaped PLGA-vitamin E TPGS copolymer for docetaxel delivery to cervical cancer

We developed a system of nanoparticles (NPs) of cholic acid functionalized, star-shaped block copolymer consisting of PLGA and vitamin E TPGS for sustained and controlled delivery of docetaxel for treatment of cervical cancer, which demonstrated superior in vitro and in vivo performance in comparison with the drug-loaded PLGA NPs and the linear PLGA-b-TPGS copolymer NPs. The star-shaped block copolymer CA-PLGA-b-TPGS of three branch arms was synthesized through the core-first approach and characterized by 1H NMR, GPC and TGA. The drug- or coumarin 6-loaded NPs were prepared by a modified nanoprecipitation technique and then characterized in terms of size and size distribution, surface morphology and surface charge, drug encapsulation efficiency, in vitro release profile and physical state of the encapsulated drug. The CA-PLGA-b-TPGS NPs were found to have the highest cellular uptake efficiency, the highest antitumor efficacy compared with PLGA-b-TPGS NPs and PLGA NPs. The results suggest that such a star-shaped copolymer CA-PLGA-b-TPGS could be used as a new molecular biomaterial for drug delivery of high efficiency.