A novel polymer micelle as a targeted drug delivery system for 10-hydroxycamptothecin with high drug-loading properties and anti-tumor efficacy

A novel polyethylene glycol-polycaprolactone-poly-l-tyrosine (MPEG-PCL-PTyr) amphiphilic triblock copolymer micelle was synthesized for the first time. 10-hydroxycamptothecin (HCPT) was embedded in MPEG-PCL-PTyr nanomicelles using the emulsion solvent evaporation method. A series of was conducted to confirm the structure of the compound and to evaluate the physical properties of the MPEG-PCL-PTyr nanomicelles. Cellular uptake, cytotoxicity, and apoptosis were assessed using flow cytometry and MTT assays. Confocal microscopy and flow cytometry results demonstrated that the nanocapsules carrying HCPT had significantly increased anti-tumor activity against HepG2 cells and could target HepG2 cell lysosomes with obvious liver targeting. In addition, the drug-loaded nanomicelles could significantly block the S phase of cancer cells and induce apoptosis; thus, they could be potential carriers for future 10-HCPT delivery and cancer treatment. [Display omitted] •In this paper, A novel polyethylene glycol-polycaprolactone-poly-l-tyrosine (MPEG-PCL-Ptyr) amphiphilic triblock copolymer micelle was synthesized for the first time.•10-HCPT was embedded in MPEG-PCL-Ptyr nanomicelle by emulsion solvent evaporation method. A series of experiment were conducted to confirm the structure of compound and evaluate physical properties of MPEG-PCL-Ptyr nanomicelle.•The article results show that drug-loaded nanomicelles can significantly block the S phase of cancer cells and induce apoptosis. It will be a potential carrier for future 10-HCPT delivery and cancer treatment.