Issue 18, 2015

Self-assembled micelles of a multi-functional amphiphilic fusion (MFAF) peptide for targeted cancer therapy

Abstract

A new multi-functional amphiphilic fusion (MFAF) peptide comprised of a multi-functional fusion peptide sequence (GFLGR8GDS) and a hydrophobic polycaprolactone (PCL) tail was designed and prepared. In aqueous solution, through the strong hydrophobic interaction among the PCL tails, this MFAF peptide can self-assemble into core–shell micelles at a low concentration with the anti-tumor drug doxorubicin (DOX) loaded in the core and the multi-functional fusion peptide sequence located on the shell. When incubating the DOX-loaded micelles with tumor and normal cells, the micelles can use the RGD and membrane-penetrating peptide (eight continuous arginine residues, R8) sequences to target tumor cells and penetrate cell membranes. Subsequently, cathepsin B, an enzyme over-expressed in late endosomes and lysosomes of tumor cells that can specifically hydrolyze the GFLG sequence, can break the micellar structure and lead to a rapid release and escape of loaded DOX from endosomes, resulting in the apoptosis of tumor cells. The MFAF peptide presents great potential as a new drug delivery platform for targeted cancer chemotherapy.

Graphical abstract: Self-assembled micelles of a multi-functional amphiphilic fusion (MFAF) peptide for targeted cancer therapy

Supplementary files

Article information

Article type
Paper
Submitted
29 Jan 2015
Accepted
18 Mar 2015
First published
19 Mar 2015

Polym. Chem., 2015,6, 3512-3520

Author version available

Self-assembled micelles of a multi-functional amphiphilic fusion (MFAF) peptide for targeted cancer therapy

Y. Cheng, H. Cheng, X. Zhao, X. Xu, R. Zhuo and F. He, Polym. Chem., 2015, 6, 3512 DOI: 10.1039/C5PY00125K

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