Nanomedicine: Nanotechnology, Biology and Medicine
Volume 8, Issue 2 , Pages 194-203, February 2012

A novel dextran-oleate-cRGDfK conjugate for self-assembly of nanodrug

  • Zhe Wang, PhD
  • ,
  • Ting Yee Lee, BSc
  • ,
  • Paul C. Ho, PhD

      Affiliations

    • Corresponding Author InformationCorresponding author: Laboratory for Experimental and Applied Pharmacokinetics and Pharmacodynamics (LEAP2), Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.

Received 21 March 2011; accepted 5 June 2011. published online 27 June 2011.

Abstract 

We report a novel synthetic biocompatible material: a conjugate with a fatty acid-substituted dextran decorated with cRGDfK peptide, which was used as a stable coating material instead of the conventional poly(ethylene glycol) for nanodrug preparation. This novel dextran-oleate-cRGDfK conjugate (DO-cRGDfk) could self-assemble into a micellar structure in aqueous solution, and was used as a surfactant to formulate nanodrug with poly(d,l-lactic-co-glycolic) acid as matrix to encapsulate paclitaxel with high drug-loading efficiency. The conjugate allowed the fabrication of nanodrug with a targeting moiety on its surface in a simple and robust step. The resultant nanoparticles could induce cellular apoptosis more effectively than that of the commercial paclitaxel formulation, Taxol. Thus, DO-cRGDfk could be used as an alternative to poly(ethylene glycol) as a biocompatible surface coating polymeric material for nanoparticle preparation.

From the Clinical Editor

The authors describe a novel synthetic biocompatible conjugate, which consists of a fatty acid-substituted dextran decorated with cRGDfK peptide. This conjugate was used as a stable coating material for nanodrug preparation, and can be used in place of conventional PEG.

Graphical Abstract 

A novel biocompatible and biodegradable material - a conjugate with a fatty acid substituted dextran decorated with cRGDfK peptide which can be used as a surfactant to prepare integrin targeting nanodrug in a single step with PLGA as the matrix and without the need for further particle surface modification for targeting. This new conjugate could be regarded as an alternative to PEG as a surface coating material for the preparation of nanoparticle.

Key words: Dextran, Poly(ethylene glycol), Nanoparticle, Paclitaxel, Cyclic (Arg-Gly-Asp-D-Phe-Lys) (cRGDfk)

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 This research is supported by Academic Research Funding grants R148-000-097-112 and R148-000-128-112 from the National University of Singapore.

PII: S1549-9634(11)00259-0

doi:10.1016/j.nano.2011.06.006

Nanomedicine: Nanotechnology, Biology and Medicine
Volume 8, Issue 2 , Pages 194-203, February 2012