Issue 37, 2015

An unusual role of folate in the self-assembly of heparin–folate conjugates into nanoparticles

Abstract

Tumor targeting agents including antibodies, peptides, and small molecules, are often used to improve the delivery efficiency of nanoparticles. Despite numerous studies investigating the abilities of targeting agents to increase the accumulation of nanosized therapeutics within diseased tissues, little attention has been focused on how these ligands can affect the self-assembly of the nanoparticle's modified polymer constituents upon chemical conjugation. Here we present an actively tumor targeted nanoparticle constructed via the self-assembly of a folate modified heparin. Folate conjugation unexpectedly allowed the self-assembly of heparin, where a majority of the folate molecules (>80%) resided inside the core of the nanoparticle. The folate–heparin nanoparticles could also physically encapsulate lipophilic fluorescent dyes, enabling the use of the constructs as activatable fluorescent probes for targeted in vivo tumor imaging.

Graphical abstract: An unusual role of folate in the self-assembly of heparin–folate conjugates into nanoparticles

Supplementary files

Article information

Article type
Paper
Submitted
19 May 2015
Accepted
29 Jul 2015
First published
13 Aug 2015

Nanoscale, 2015,7, 15185-15190

Author version available

An unusual role of folate in the self-assembly of heparin–folate conjugates into nanoparticles

J. Wang, D. Ma, Q. Lu, S. Wu, G. Y. Lee, L. A. Lane, B. Li, L. Quan, Y. Wang and S. Nie, Nanoscale, 2015, 7, 15185 DOI: 10.1039/C5NR03303A

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