Issue 3, 2012

Microfluidic approach for highly efficient synthesis of heparin-based bioconjugates for drug delivery

Abstract

This paper demonstrates the highly efficient synthesis of amphiphilic heparin-folic acid-retinoic acid (HFR) bioconjugates with a high drug coupling ratio by a microfluidic approach. The microfluidic synthesis enabled the conjugation of 17 molecules of retinoic acid to each heparin chain with 21 possible groups for attachment after reacting for several minutes. In contrast, about 11 molecules of the drug were covalently conjugated to one heparin chain after 4 days in the bulk reaction. The microfluidic based-HFR bioconjugates readily self-assembled in aqueous media to form uniform nanoparticles, while the product from the bulk reaction formed non-uniform nanoparticles with broad size distribution. The HFR nanoparticles with high drug content effectively delivered the drug to folate receptor-positive cancer cells with superior cellular uptake and selective cytotoxicity in vitro compared to HFR nanoparticles synthesized in bulk reaction. With the ability to achieve high drug content in heparin carrier within a short reaction time, the microfluidic technique offers new alternatives for the efficient synthesis of polymer-based conjugates for drug delivery.

Graphical abstract: Microfluidic approach for highly efficient synthesis of heparin-based bioconjugates for drug delivery

Supplementary files

Article information

Article type
Paper
Submitted
17 Aug 2011
Accepted
31 Oct 2011
First published
02 Dec 2011

Lab Chip, 2012,12, 589-594

Microfluidic approach for highly efficient synthesis of heparin-based bioconjugates for drug delivery

T. H. Tran, C. T. Nguyen, D. Kim, Y. Lee and K. M. Huh, Lab Chip, 2012, 12, 589 DOI: 10.1039/C1LC20769E

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