Issue 37, 2014

pH-sensitive short worm-like micelles targeting tumors based on the extracellular pH

Abstract

We developed novel photosensitizing drug-carrying worm-like micelles using a pH-sensitive AB2 miktoarm block copolymer consisting of one methoxy-poly(ethylene glycol) (mPEG) block (A) and two 3-diethylaminopropylated poly(L-lysine) [poly(Lys-DEAP)] blocks (B2). In particular, the Y-shaped AB2 miktoarm block copolymer structure mimicking the phospholipid structure enabled the facile preparation of worm-like micelles. The unique feature of pH-responsive DEAP as a hydrophobic moiety (non-protonated DEAP) at pH 7.4 and as a hydrophilic moiety (protonated DEAP) at pH 6.8 modulated acidic pH-activated micellar disintegration. These worm-like micelles serve as a basic transformer whose assembled conformation disintegrates in the acidic milieu (∼pH 6.8) of solid tumors, resulting in improved phototoxicity due to triggered drug release from disintegrated micelles at acidic tumor sites and high-yield generation of cytotoxic singlet oxygen from the photosensitizing drug. As a result, the tumor volume in the nude mice treated with these worm-like micelles was approximately 5.2 times smaller than those treated with free drug. We anticipate that this system will provide great potential for tumor therapy.

Graphical abstract: pH-sensitive short worm-like micelles targeting tumors based on the extracellular pH

Supplementary files

Article information

Article type
Paper
Submitted
14 May 2014
Accepted
15 Jul 2014
First published
16 Jul 2014

J. Mater. Chem. B, 2014,2, 6363-6370

Author version available

pH-sensitive short worm-like micelles targeting tumors based on the extracellular pH

J. O. Lee, K. T. Oh, D. Kim and E. S. Lee, J. Mater. Chem. B, 2014, 2, 6363 DOI: 10.1039/C4TB00779D

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements