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

Jianyu Ma, Zhouzhou Liao, Jinbo Li, Xiao Li, Hongling Guo, Qiyu Zhong, Jianyun Huang, Xintao Shuai, Shuqin Chen
Biomaterials science · 2025 · vol. 13(4) , pp. 1045–1058 · doi:10.1039/d4bm01506a · PMID:39829388 · W4406599506
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A cRGD-modified liposome loaded with artesunate targets endometriosis lesions to inhibit angiogenesis by suppressing the HIF-1α/VEGF pathway, improving efficacy and reducing side effects.

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

mesh:D004715endometriosis

MeSH descriptors

Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors Angiogenesis Inhibitors

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Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

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