Construction of hydroxypropyl-β-cyclodextrin copolymer nanoparticles and targeting delivery of paclitaxel

Qinghua Miao, Suping Li, Siyuan Han, Zhi Wang, Yan Wu, Guangjun Nie

Research output: Contribution to journalArticlepeer-review

15 Scopus citations


A novel amphiphilic copolymer with p-maleimidophenyl isocyanate- hydroxypropyl-β-cyclodextrin-polylactide-1,2-dipalmitoyl-sn-glycero-3- phosphoethanolamine to generate copolymer nanoparticles (NPs) has been designed. In order to develop an active targeting system, integrin α vβ 3-specific targeting peptide cyclo(Arg-Gly-Asp-D- Phe-Cys), cRGD, was conjugated to the surface of NPs (NPs-RGD). These NPs were used to encapsulate anti-tumor drug, paclitaxel. The resulting NPs exhibited high drug-loading capacity and controlled drug release in vitro at acidic pH. In vitro cytotoxicity assay demonstrates that paclitaxel-loaded NPs-RGD significantly inhibited B16 tumor cell (high α vβ 3) proliferation relative to free paclitaxel and paclitaxel-loaded NPs at high concentrations. Paclitaxel-loaded NPs-RGD localized mainly in lysosomes in B16 cells as revealed by confocal microscopy. These results suggest a novel strategy for fabrication-functionalizing hydroxypropyl-β- cyclodextrin copolymer nanoparticles for targeting delivery of paclitaxel to integrin α vβ 3-rich tumor cells. These nanocarriers can be readily extended to couple other bioactive molecules for active targeting and delivery of various chemotherapeutic drugs.

Original languageEnglish (US)
Article number1043
JournalJournal of Nanoparticle Research
Issue number8
StatePublished - Aug 2012


  • Anti-tumor activity
  • cRGD
  • Hydroxypropyl-β-cyclodextrin
  • Nanomedicine
  • Nanoparticles
  • Paclitaxel

ASJC Scopus subject areas

  • Atomic and Molecular Physics, and Optics
  • Condensed Matter Physics
  • Modeling and Simulation
  • Chemistry(all)
  • Materials Science(all)
  • Bioengineering


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