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

93 Citations (Scopus)

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

Fingerprint

Micelles
Pharmaceutical Preparations
Ovarian Neoplasms
irinotecan
Paclitaxel
Heterografts
Cholic Acids
Cholic Acid
Neoplasms
Optical Imaging
Etoposide
Drug Delivery Systems
Bovine Serum Albumin
Particle Size
Nude Mice
Serum Albumin
Polymers
Arm
Ethanol
Dogs

Keywords

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

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Medicine(all)

Cite this

A novel size-tunable nanocarrier system for targeted anticancer drug delivery. / Li, Yuanpei; Xiao, Kai; Luo, Juntao; Lee, Joyce S; Pan, Shirong; Lam, Kit.

In: Journal of Controlled Release, Vol. 144, No. 3, 06.2010, p. 314-323.

Research output: Contribution to journalArticle

Li, Yuanpei ; Xiao, Kai ; Luo, Juntao ; Lee, Joyce S ; Pan, Shirong ; Lam, Kit. / A novel size-tunable nanocarrier system for targeted anticancer drug delivery. In: Journal of Controlled Release. 2010 ; Vol. 144, No. 3. pp. 314-323.
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