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Published on: September 18, 2018
Ursolic acid-loaded chitosan nanoparticles induce potent anti-angiogenesis in tumor
Hua Jin1,2, Jiang Pi1, Fen Yang1
1State Key Laboratory of Quality Research in Chinese Medicines, Macau University of Science and Technology, Macau, 000853, China.
Abstract:
Angiogenesis provides necessary nutrients and oxygen for tumor growth and metastasis; thus, every stage of angiogenesis process is the potential target for cancer therapies. Ursolic acid (UA) is reported to decrease tumor burden through anti-angiogenesis pathway, but its poor water solubility greatly limits its efficiency and clinical application. Here, a simple method for preparing UA-loaded chitosan nanoparticles (CH-UA-NPs) with anti-angiogenesis and anti-tumor activity was demonstrated. In vitro, CH-UA-NPs could significantly inhibit the proliferation, migration, and tube formation of human umbilical vascular endothelial cells (HUVECs). After uptake by HUVECs, CH-UA-NPs were mainly localized in lysosomes and mitochondria, but not nuclei. CH-UA-NPs induced the destruction of lysosome membrane integrity, collapse of mitochondrial membrane potential, and reorganization of cell cytoskeleton. All these changes led to the apoptosis or necrosis in HUVECs. In vivo, CH-UA-NPs could inhibit the angiogenesis in chicken chorioallantoic membrane (CAM) model and H22 xenograft model. Notably, comparing with free UA, such synthesized CH-UA-NPs could save about tenfold of UA doses, implying that this could significantly decrease the side effects induced by high doses of UA in biological organism. Our data showed that CH-UA-NPs and this nanoparticle-based drug delivery system could be as a potential drug candidate for anti-angiogenesis treatment.
Insights
Ursolic acid-loaded chitosan nanoparticles effectively inhibit tumor angiogenesis and growth. This nanoparticle formulation enhances ursolic acid
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Research
Background:
- Angiogenesis is crucial for tumor growth and metastasis, making it a target for cancer therapies.
- Ursolic acid (UA) exhibits anti-angiogenic and anti-tumor properties, but its poor water solubility limits clinical use.
- Developing effective delivery systems for UA is essential to improve its therapeutic efficacy.
Purpose of the Study:
- To develop and evaluate ursolic acid-loaded chitosan nanoparticles (CH-UA-NPs) for enhanced anti-angiogenesis and anti-tumor activity.
- To investigate the in vitro mechanisms of CH-UA-NPs on human umbilical vascular endothelial cells (HUVECs).
- To assess the in vivo efficacy of CH-UA-NPs in preclinical models of angiogenesis and tumor growth.
Main Methods:
- Preparation and characterization of UA-loaded chitosan nanoparticles (CH-UA-NPs).
- In vitro assessment of CH-UA-NPs' effects on HUVEC proliferation, migration, and tube formation.
- In vivo evaluation of CH-UA-NPs using the chicken chorioallantoic membrane (CAM) and H22 xenograft models.
Main Results:
- CH-UA-NPs significantly inhibited HUVEC proliferation, migration, and tube formation.
- CH-UA-NPs induced HUVEC apoptosis/necrosis via lysosomal and mitochondrial pathways.
- In vivo studies demonstrated CH-UA-NPs' ability to inhibit angiogenesis and reduce tumor burden.
- CH-UA-NPs required a tenfold lower dose compared to free UA, suggesting reduced side effects.
Conclusions:
- CH-UA-NPs represent a promising nanoparticle-based drug delivery system for anti-angiogenesis cancer therapy.
- The developed CH-UA-NPs overcome the solubility limitations of ursolic acid, enhancing its therapeutic potential.
- This nanoparticle formulation offers a strategy for more effective and potentially safer cancer treatment by targeting angiogenesis.
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