A novel size-tunable nanocarrier system for targeted anticancer drug delivery

Yuanpei Li, Kai Xiao, Juntao Luo, Joyce S Lee, Shirong Pan, Kit Lam

Research output: Contribution to journalArticle

96 Scopus citations

Abstract

We have developed a nanocarrier drug-delivery system based on micelles formed by a new class of well-defined linear PEGylated two-arm oligomer of cholic acids in aqueous solution. By varying the length of the linear PEG chains and the configuration of cholic acid oligomer, one can easily fine-tune the physicochemical properties of the amphiphilic polymers and the resulting micelles. These include particle size, critical micelle concentration, and drug-loading capacity. High level of hydrophobic anticancer drugs such as PTX, etoposide and SN-38 can be readily loaded into such nanocarriers. The loading capacity of the nanocarrier for PTX (PTX) is extremely high (12.0mg/mL), which is equivalent to 37.5% (w/w) of the total mass of the micelle. PTX-loaded nanocarriers are much more stable than Abraxane® (PTX/human serum albumin nanoaggregate) when stored in bovine serum albumin solution or dog plasma. PTX release profile from the micelles is burst-free and sustained over a period of seven days. The anti-tumor activity of PTX-loaded nanocarriers against ovarian cancer cell line in vitro, with continuous drug exposure, is similar to Taxol® (formulation of PTX dissolved in Cremophor EL and ethanol) or Abraxane®. Targeted drug delivery to tumor site with these novel micelles was demonstrated by near infrared fluorescence (NIRF) imaging in nude mice bearing ovarian cancer xenograft. Furthermore, PTX-loaded nanocarriers demonstrated superior anti-tumor efficacy compared to Taxol® at equivalent PTX dose in ovarian cancer xenograft model.

Original languageEnglish (US)
Pages (from-to)314-323
Number of pages10
JournalJournal of Controlled Release
Volume144
Issue number3
DOIs
StatePublished - Jun 2010

Keywords

  • Cholic acid
  • High loading
  • Micelle
  • Nanocarrier
  • Size tunable
  • Tumor targeting

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Medicine(all)

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