The Endocytic Mechanism and Cytotoxicity of Boron-Containing Vesicles

Chem Pharm Bull (Tokyo). 2020 Jul 1;68(7):618-627. doi: 10.1248/cpb.c19-00971. Epub 2020 May 12.

Abstract

A novel polymer (PEG2000-carborane), self-assembling into spherical vesicles (boron-containing vesicles, BCVs), could be quickly taken up by tumor cells and had an enhance stability in the bloodstream in previous study. To have more comprehensive understanding of BCVs, endocytic mechanism and cytotoxicity assessment were conducted. The results showed that BCVs were taken up in the intact form with cholesterol-dependent pathway during endocytosis, and BCVs exhibited nearly no cytotoxicity. BCVs could accumulate within tumors for at least 24 h. The data would provide reference information and guidance for BCVs' multifunctional application serving as a boron delivery agent for boron neutron capture therapy (BNCT), a hydrophilic and/or hydrophobic drug carrier and a diagnostic imaging fluorescent probe.

Keywords: boron-containing vesicle (BCV); cytotoxicity; endocytic mechanism.

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Boron / chemistry
  • Boron / pharmacology*
  • Boron Neutron Capture Therapy*
  • Cell Cycle / drug effects
  • Cell Line
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry
  • Endocytosis / drug effects*
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacology*
  • Glioma / diagnostic imaging*
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Mice
  • Neoplasms, Experimental / diagnostic imaging
  • Optical Imaging
  • Particle Size
  • Surface Properties

Substances

  • Drug Carriers
  • Fluorescent Dyes
  • Boron