ORIGINAL RESEARCH article

Front. Oncol.

Sec. Cancer Molecular Targets and Therapeutics

Volume 15 - 2025 | doi: 10.3389/fonc.2025.1573628

This article is part of the Research TopicNovel Molecular Targets in Cancer TherapyView all 27 articles

Preparation of RGD-modified liposome encapsulated with shikonin and its targeted anti-melanoma effects

Provisionally accepted
Hao  ZhangHao ZhangYing  ZhaoYing ZhaoTingting  ChenTingting ChenXinliang  MaoXinliang MaoJiping  LiJiping LiLi  FanLi FanMin  LiMin LiXianchun  WenXianchun Wen*
  • Qiqihar Medical University, Qiqihar, China

The final, formatted version of the article will be published soon.

Melanoma is the most aggressive skin tumour and conventional treatment is incurable. Studies have shown that shikonin derived from traditional Chinese medicine Lithospermum erythrorhizon has various anticancer activities. In this work, RGD-modified liposome encapsulated with shikonin (RGD-Lip-SHK) was prepared, which could highly recognize the integrin αVβ3 on the surface of melanoma cells. RGD-Lip-SHK appeared as spheroid-like vesicles and particle size about 120 nm and their ξ-potential was negative. RGD-Lip-SHK maintained stable in serum within 48 h and possessed sustained-release effect. In vitro, compared with nontargeted liposomes (Lip-SHK), RGD-Lip-SHK were more efficiently taken up and had higher cytotoxicity, and were better targeted to inhibit cell growth, migration, invasion and boosted cell apoptosis by regulating the expression of Bcl-2 and Bax proteins in melanoma cells. In vivo, RGD-Lip-SHK had the strongest targeted antimelanoma effect by αVβ3-mediated endocytosis with a long circulation time, and inhibited tumour growth in B16F10 tumour-bearing mice compared to other groups. Furthermore, Histology of major organs and the bodyweight of mice showed RGD-Lip-SHK had few toxicity. In short, these results indicated that RGD-Lip-SHK had great potential for targeted treatment of melanoma, thereby presenting a novel and high effective therapeutic strategy for tumour targeted therapy.

Keywords: Shikonin, Melanoma, Liposomes, RGD, αvβ3 integrin

Received: 09 Feb 2025; Accepted: 09 Apr 2025.

Copyright: © 2025 Zhang, Zhao, Chen, Mao, Li, Fan, Li and Wen. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

* Correspondence: Xianchun Wen, Qiqihar Medical University, Qiqihar, China

Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.

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