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Updated: Feb 7, 2026

Generating a Murine Orthotopic Metastatic Breast Cancer Model and Performing Murine Radical Mastectomy
Published on: November 29, 2018
Liposomal borrelidin for treatment of metastatic breast cancer
Moonkyoung Jeong1, Heegon Kim1, Sunghoon Kim2,3
1Department of Bio and Brain Engineering and KAIST Institute for Health Science and Technology, KAIST, Daejeon, Republic of Korea.
Abstract:
Borrelidin is an inhibitor of threonyl-tRNA synthetase with both anticancer and antiangiogenic activities. Although borrelidin could be a potent drug that can treat metastatic cancer through synergistic therapeutic effects, its severe liver toxicity has limited the use for cancer therapeutics. In this study, we developed a liposomal formulation of borrelidin to treat metastatic breast cancer effectively through its combined anticancer and antiangiogenic effects while reducing the potential liver toxicity. The liposomal formulation was optimized to maximize loading stability and efficiency of lipophilic borrelidin in the liposomal membrane and its delivery efficiency to primary tumor in a mouse model of metastatic breast cancer. Liposomal borrelidin showed significant in vitro therapeutic effects on proliferation and migration of tumor cells and angiogenesis of endothelial cells. Furthermore, liposomal borrelidin exhibited superior inhibitory effects on primary tumor growth and lung metastasis in vivo compared to free borrelidin. More importantly, liposomal borrelidin did not induce any significant systemic toxicity in the mouse model after multiple injections.
Insights
Liposomal borrelidin effectively treats metastatic breast cancer by combining anticancer and antiangiogenic effects. This formulation enhances tumor delivery and significantly reduces liver toxicity compared to free borrelidin.
Area of Science:
- Pharmacology
- Oncology
- Nanotechnology
Background:
- Borrelidin, an inhibitor of threonyl-tRNA synthetase, exhibits anticancer and antiangiogenic properties.
- Severe liver toxicity limits the clinical application of borrelidin for metastatic cancer treatment.
- Developing targeted drug delivery systems can mitigate toxicity and enhance therapeutic efficacy.
Purpose of the Study:
- To develop and optimize a liposomal formulation of borrelidin for metastatic breast cancer treatment.
- To evaluate the efficacy of liposomal borrelidin in inhibiting tumor growth and metastasis.
- To assess the safety profile of liposomal borrelidin, focusing on liver toxicity.
Main Methods:
- Liposomal formulation of borrelidin was developed and optimized for stability and drug loading.
- In vitro studies assessed the effects of liposomal borrelidin on tumor cell proliferation, migration, and endothelial cell angiogenesis.
- In vivo studies in a mouse model of metastatic breast cancer evaluated tumor growth inhibition, metastasis reduction, and systemic toxicity.
Main Results:
- Liposomal borrelidin demonstrated significant in vitro anticancer and antiangiogenic activities.
- Liposomal borrelidin showed superior inhibition of primary tumor growth and lung metastasis compared to free borrelidin in vivo.
- Multiple injections of liposomal borrelidin did not induce significant systemic toxicity in the mouse model.
Conclusions:
- Liposomal formulation is a promising strategy to enhance the therapeutic potential of borrelidin for metastatic breast cancer.
- Liposomal borrelidin effectively targets primary tumors and reduces metastasis while minimizing liver toxicity.
- This approach offers a safer and more effective treatment option for metastatic breast cancer.
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