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

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-targ...

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Bibliographic Details
Published in:Biomaterials science 2020-04, Vol.8 (8), p.2274-2282
Main Authors: Cai, Yue, Xu, Zhuomin, Shuai, Qi, Zhu, Fangtao, Xu, Jiao, Gao, Xin, Sun, Xuanrong
Format: Article
Language:English
Subjects:
Anticancer properties
Bioavailability
Block copolymers
Breast cancer
Chemotherapy
Drug delivery systems
Micelles
Nanoparticles
Peptides
Side effects
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Summary: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. PEG-PLA micelles are modified with F3 peptides, thus endowing the micelles with active-targeting ability due to the nucleolin-binding ability of the F3 peptides.
ISSN:2047-4830
2047-4849
DOI:10.1039/c9bm02036e