Tunable pH-Responsive Polymeric Micelle for Cancer Treatment

Xiaolan Zhang, Yixian Huang, Mohammed Ghazwani, Peng Zhang, Jiang Li, Stephen H. Thorne, Song Li*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

The development of bioresponsive polymers is important in drug delivery systems. Herein, we reported the construction of a series of pH-sensitive micelles by conjugating the hydrophilic polyethylene glycol (PEG) segment to a hydrophobic farnesylthiosalicylate derivative, FTS-hydrazide (FTS-H), with a hydrazone linker, whose cleavability can be conveniently modulated by choosing various lengths of the carbon chain or appropriate electron-withdrawing groups with different steric environment around the hydrazone linker. We examined the hydrolysis rates of these pH-sensitive micelles in both neutral and acidic conditions. One of the pH-sensitive micelles (PHF-2) was found to be highly sensitive to acidic conditions while being fairly stable in neutral conditions. Furthermore, PHF-2 micelles well retained the antitumor activity of free FTS-H. We further evaluated the use of PHF-2 micelles as a carrier for delivering paclitaxel (PTX) and the triggered release of PTX under the acidic environment. PTX-loaded PHF-2 micelles showed enhanced antitumor activity compared with free PTX, likely because of the combinational effect between PHF-2 micelles and loaded PTX.

Original languageEnglish (US)
Pages (from-to)620-623
Number of pages4
JournalACS Macro Letters
Volume4
Issue number6
DOIs
StatePublished - Jun 16 2015
Externally publishedYes

ASJC Scopus subject areas

  • Organic Chemistry
  • Polymers and Plastics
  • Inorganic Chemistry
  • Materials Chemistry

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