Decoration of pH-sensitive copolymer micelles with tumor-specific peptide for enhanced cellular uptake of doxorubicin
Open accessAbstract
To improve the targeting efficacy of hyaluronic acid (HA)-based micelles, pH-sensitive mixed micelles based on HA-g-poly(L-histidine) (PHis) and d-α-tocopheryl polyethylene glycol 2000 copolymers were prepared and decorated with human epidermal growth factor receptor 2 (Her2) peptide, a tumor cell-specific peptide ligand, on their surface. The doxorubicin-loaded micelles (HA-PHis/peptide-d-α-tocopheryl polyethylene glycol 2000 mixed micelles [PHTM]) were characterized to have a unimodal size distribution and pH-dependent drug release pattern. In vitro tumor targeting studies demonstrated that PHTM exhibited the pronounced cytotoxicity and efficient internalization in MDA-MB-231 cells overexpressing CD44 and Her2 receptors. In vivo investigation into micelles in MDA-MB-231 tumor-bearing mice confirmed that PTHM could reach the tumor site more effectively and exert excellent tumor killing activity. In general, Her2 peptide decoration can enhance the selective cytotoxicity and antitumor activity of HA-based micelles.
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Her2-modified HA-based pH-responsive micelle can reach the tumor site more effectively and has good tumor killing activity.
“Chen et al. prepared a hyaluronic acid (HA)-based pH-responsive mixture micelle, modified with Her2 peptide, which can reach the tumor site more effectively and has good tumor killing activity.225”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [225]
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Smart nanoparticles for cancer therapy
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- Authors
- Chen, Q., Long, M., Qiu, L., Zhu, M., Li, Z., Qiao, M., Hu, H., Zhao, X., & Chen, D.
- Affiliations
- Shenyang Pharmaceutical University (CN)
- Jiangnan University (CN)
- Corresponding author
- Chen, Dawei
- Venue
- International Journal of Nanomedicine
- Publisher
- Informa UK Limited
- Published
- 2016-10
- Volume
- Volume 11
- Pages
- 5415-5427
- ISSN
- 1176-9114 (ISSN-L)
- 1178-2013
- PMC
- PMC5077130
- OpenAlex
- W2538843590
- Cited by
- 16
- References
- 49
- Citations by year
- 2025: 5 · 2023: 3 · 2021: 1 · 2020: 1 · 2019: 2 · 2018: 4
- FWCI
- 0.82
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- International Journal of Nanomedicine (publishedVersion, cc-by-nc)
- PubMed Central (publishedVersion, cc-by-nc)
- PubMed (publishedVersion)
- Dove Medical Press (Taylor and Francis Group) (submittedVersion, cc-by-nc)
- Funders
- National Natural Science Foundation of China (81573370, 81302713, 81503007)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Physical Sciences › Materials Science › Polymers and Plastics › Dendrimers and Hyperbranched Polymers
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- pH-responsive micelles, hyaluronic acid, poly-L-histidine, tumor targeting, doxorubicin delivery, mixed micelles, CD44, MDA-MB-231 breast cancer, pH-dependent drug release, anticancer drug delivery
- MeSH terms
- Animals, Biological Transport, Doxorubicin, Drug Carriers, Female, Histidine, Humans, Hyaluronic Acid, Hydrogen-Ion Concentration, Micelles, Peptides, Polyethylene Glycols, Erb-b2 Receptor Tyrosine Kinases, Receptor, ErbB-2, Hyaluronan Receptors, alpha-Tocopherol, Cell Line, Tumor, Mice
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