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

Biophys Chem. 2021 Dec:279:106679. doi: 10.1016/j.bpc.2021.106679. Epub 2021 Sep 17.

Abstract

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.

Keywords: 10-hydroxycamptothecin; Cellular uptake; Cytotoxicity; MPEG-PCL-PTyr block copolymer micelles; Nanoparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Camptothecin / analogs & derivatives
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Micelles*
  • Particle Size
  • Polyethylene Glycols / chemistry
  • Polymers* / chemistry

Substances

  • Drug Carriers
  • Micelles
  • Polymers
  • Polyethylene Glycols
  • 10-hydroxycamptothecin
  • Camptothecin