A cRGD-modified liposome for targeted delivery of artesunate to inhibit angiogenesis in endometriosis

  • Biomater Sci. 2025 Jan 20. doi: 10.1039/d4bm01506a.
Jianyu Ma  1  2 ,  Zhouzhou Liao  1  2 ,  Jinbo Li  1  2 ,  Xiao Li  1  2 ,  Hongling Guo  3 ,  Qiyu Zhong  1  2 ,  Jianyun Huang  1  2 ,  Xintao Shuai  4 ,  Shuqin Chen  1  2
Affiliations
  • 1. Department of Gynecology, The Sixth Affiliated Hospital, Sun Yat-Sen University, Guangzhou, Guangdong 510655, China. [email protected].
  • 2. Biomedical Innovation Center, The Sixth Affiliated Hospital, Sun Yat-Sen University, Guangzhou, Guangdong 510655, China.
  • 3. Department of Gynecology, The Seventh Affiliated Hospital, Sun Yat-Sen University, Shenzhen, Guangdong 518012, China.
  • 4. Nanomedicine Research Center, The Third Affiliated Hospital of Sun Yat-sen University, Guangzhou 510630, China. [email protected].
PMID: 39829388 DOI: 10.1039/d4bm01506a
Abstract

Currently, hormonal therapy for endometriosis faces challenges in achieving a balance between treatment and preserving the chance of pregnancy. Therefore, the development of non-hormonal therapy holds significant clinical importance. Angiogenesis is a hallmark of endometriosis, and anti-angiogenic therapies targeting the hypoxia-inducible factor-1α (HIF-1α) pathway are considered potential approaches for endometriosis. However, angiogenesis is also involved in numerous physiological processes, including pregnancy, and systemic anti-angiogenesis may lead to severe adverse effects. To address this, a cRGD-modified Liposome nanodrug (cRGD-LP-ART) is synthesized, which enhances drug efficacy while reducing adverse reactions. Artesunate (ART), a non-hormonal drug used to treat malaria, has shown anti-angiogenic effects beyond its original indications in various benign and malignant diseases. With cRGD modification, cRGD-LP-ART can target ectopic lesions and inhibit local angiogenesis by suppressing the HIF-1α/vascular endothelial growth factor (VEGF) pathway. Furthermore, cRGD-LP-ART exhibits better therapeutic effects than free ART, without affecting ovarian function or causing atrophy of the eutopic endometrium, making it a promising new option for non-hormonal therapy of endometriosis. As a combination of liposomes and a clinically approved drug, cRGD-LP-ART holds great potential and clinical prospects for the treatment of endometriosis.

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