Tumor cells-specific targeting delivery achieved by A54 peptide functionalized polymeric micelles
Abstract
The delivery of all of administrated chemotherapeutics into tumor cells is an extreme object for tumor targeting therapy to enhance the curative effect and eliminate the side effect. However, until now, the targeting delivery has only partial been realized by passive targeting, which was called "enhanced permeability and retention" effect, and only few targeting delivery system was commercialized. Here, we designed and synthesized a hepatocarcinoma-binding peptide (A54 peptide, which was identified from a phage-display random peptide library) functionalized and PEGylated stearic acid grafted chitosan (A54-PEG-CS-SA) micelles for targeting therapy of doxorubicin. The A54-PEG-CS-SA micelles presented special internalization ability into human hepatoma cells (BEL-7402) when the cells were co-incubated with normal liver cells in vitro, and high distribution ability to liver and hepatoma tissue in vivo. In vitro and in vivo anti-tumor activity results showed that A54-PEG-CS-SA micelles loading doxorubicin treatments suppressed tumor growth more effectively and reduced toxicity compared with commercial adriamycin injection.
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A54-functionalized PEG-CS-SA micelle exhibits special internalization ability for liver cancer cells in vitro, high distribution in liver and liver cancer tissues in vivo, more effectively inhibits tumor growth, and reduces toxicity.
“It exhibits special internalization ability for liver cancer cells in vitro, and has a high distribution ability in liver and liver cancer tissues in vivo. It can more effectively inhibit tumor growth and reduce toxicity.223”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [223]
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Smart nanoparticles for cancer therapy
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- Authors
- Du, Y.-Z., Cai, L.-L., Liu, P., You, J., Yuan, H., & Hu, F.-Q.
- Affiliations
- Zhejiang University (CN)
- Venue
- Biomaterials
- Publisher
- Elsevier BV
- Published
- 2012-12
- Volume
- 33
- Issue
- 34
- Pages
- 8858-8867
- ISSN
- 0142-9612 (ISSN-L)
- OpenAlex
- W2007514493
- Cited by
- 54
- References
- 42
- Citations by year
- 2025: 3 · 2024: 1 · 2023: 2 · 2022: 6 · 2021: 2 · 2020: 3 · 2019: 2 · 2018: 10 · 2017: 5 · 2016: 5 · 2015: 7 · 2014: 7 · 2013: 1
- FWCI
- 1.95
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Biomaterials (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- polymeric micelles, chitosan, PEGylation, doxorubicin, hepatocellular carcinoma, phage display, passive targeting, enhanced permeability and retention effect, BEL-7402 cells, anticancer activity
- MeSH terms
- Animals, Antibiotics, Antineoplastic, Doxorubicin, Drug Carriers, Carcinoma, Hepatocellular, Humans, Liver, Liver Neoplasms, Mice, Inbred BALB C, Mice, Nude, Micelles, Oligopeptides, Polyethylene Glycols, Stearic Acids, Drug Delivery Systems, Cell Line, Tumor, Chitosan, Mice, Rats
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