Peptide-modified vemurafenib-loaded liposomes for targeted inhibition of melanoma via the skin
Abstract
Vemurafenib is a chemotherapeutic drug recently approved by the FDA to treat melanoma. Because the drug is usually delivered orally, the route of administration readily causes damage to major organs with limited antitumor efficacy and bioavailability. In this study, we developed a peptide-modified vemurafenib-loaded liposome for the targeted inhibition of subcutaneous melanoma via the skin. First, the peptide-modified vemurafenib-loaded liposomes (Vem-TD-Lip) were prepared and characterized with respect to the size, shape and charge; the loading efficiency of vemurafenib; and the stability. Then, the intracellular uptake of these liposomes, their limited cytotoxicity, the selective inhibition of melanoma cells harboring BRAF mutations, and the liposome permeation ability were confirmed through in vitro experiments. Finally, the safety and antitumor activity of Vem-TD-Lip were evaluated in vivo. The results showed that transdermal delivery of Vem-TD-Lip effectively targeted and inhibited subcutaneous melanoma in male mice, the administration of Vem-TD-Lip through skin was better than that through oral administration and intravenous injection in terms of reducing damage to major organs and enhancing antitumor efficacy, and the peptide TD significantly enhanced the delivery of Vem-TD-Lip across the skin. This work provides a new strategy for delivering vemurafenib to target and inhibit subcutaneous melanoma.
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TD-modified vemurafenib liposomes significantly increase Vem penetration in cells.
“Zou et al. prepared TD-modified vemurafenib-loaded liposomes (Vem-TD-Lip). After modification, the penetration amount of Vem in the cell was significantly increased. This shows that TD peptide promotes the delivery of Vem-TD-Lip on the skin.232”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [232]
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Smart nanoparticles for cancer therapy
Sun, L., Liu, H., Ye, Y., Lei, Y., Islam, R., Tan, S., Tong, R., Miao, Y.-B., & Cai, L. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01642-x · Cited by 1,073 · see citing works
- Authors
- Zou, L., Ding, W., Zhang, Y., Cheng, S., Li, F., Ruan, R., Wei, P., & Qiu, B.
- Affiliations
- University of Science and Technology of China (CN)
- Corresponding author
- Ding, Weiping
- Venue
- Biomaterials
- Publisher
- Elsevier BV
- Published
- 2018-11
- Volume
- 182
- Pages
- 1-12
- ISSN
- 0142-9612 (ISSN-L)
- OpenAlex
- W2885666326
- Cited by
- 92
- References
- 59
- Citations by year
- 2026: 5 · 2025: 21 · 2024: 14 · 2023: 13 · 2022: 12 · 2021: 15 · 2020: 8 · 2019: 3 · 2018: 1
- FWCI
- 3.16
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Biomaterials (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (81601600, 81701763, 81571768)
- China Postdoctoral Science Foundation (2016M590576, 2017M612098)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- vemurafenib, liposomes, transdermal drug delivery, melanoma, BRAF mutation, targeted drug delivery, skin permeation, subcutaneous tumor, antitumor efficacy, drug toxicity reduction
- MeSH terms
- Vemurafenib, Administration, Cutaneous, Animals, Antineoplastic Agents, Humans, Liposomes, Male, Melanoma, Mice, Inbred BALB C, Peptides, Skin, Skin Neoplasms, Drug Delivery Systems, Rats, Wistar, Cell Line, Tumor, Human Umbilical Vein Endothelial Cells
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