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Tumor-targeting peptide functionalized PEG-PLA micelles for efficient drug delivery

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Abstract

Because of their excellent capacity to significantly improve the bioavailability and solubility of chemotherapy drugs, block copolymer micelles are widely utilized for chemotherapy drug delivery. In order to further improve the anti-tumor ability and reduce unwanted side effects of drugs, tumor-targeting peptides were used to functionalize the surface of polymer micelles so that the micelles can target tumor tissues. Herein, we synthesized a kind of PEG-PLA that is maleimide-terminated and then conjugated with a specific peptide F3 which revealed specific capacity binding to nucleolin that is overexpressed on the surface of many tumor cells. Then, F3 conjugated, paclitaxel loaded nanoparticles (F3-NP-PTX) were prepared as stable micelles that displayed an enhanced accumulation via a peptide-mediated cellular association in human breast cancer cells (MCF-7). Furthermore, F3-NP-PTX showed a prominent anti-tumor efficacy compared with non-targeting nanoparticles (NP-PTX) both in vitro and in vivo, and showed great potential as an efficacious targeting drug delivery system for breast cancer treatment.

Graphical abstract: Tumor-targeting peptide functionalized PEG-PLA micelles for efficient drug delivery

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Article information


Submitted
18 Dec 2019
Accepted
17 Feb 2020
First published
25 Feb 2020

Biomater. Sci., 2020, Advance Article
Article type
Paper

Tumor-targeting peptide functionalized PEG-PLA micelles for efficient drug delivery

Y. Cai, Z. Xu, Q. Shuai, F. Zhu, J. Xu, X. Gao and X. Sun, Biomater. Sci., 2020, Advance Article , DOI: 10.1039/C9BM02036E

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