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Article

Maleimide-Functionalized Liposomes: Prolonged Retention and Enhanced Efficacy of Doxorubicin in Breast Cancer with Low Systemic Toxicity

by
Chuane Tang
1,†,
Dan Yin
1,†,
Tianya Liu
2,
Rui Gou
2,
Jiao Fu
1,
Qi Tang
3,
Yao Wang
3,
Liang Zou
1,* and
Hanmei Li
1,*
1
Key Laboratory of Coarse Cereal Processing, School of Food and Biological Engineering, Chengdu University, Chengdu 610106, China
2
School of Mechanical Engineering, Chengdu University, Chengdu 610106, China
3
Sichuan Industrial Institute of Antibiotics, School of Pharmacy, Chengdu University, Chengdu 610106, China
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2022, 27(14), 4632; https://doi.org/10.3390/molecules27144632
Submission received: 21 June 2022 / Revised: 11 July 2022 / Accepted: 13 July 2022 / Published: 20 July 2022
(This article belongs to the Special Issue Reactive Oxygen Species-Based Dynamic Therapy of Cancer)
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Abstract

Cell surface thiols can be targeted by thiol-reactive groups of various materials such as peptides, nanoparticles, and polymers. Here, we used the maleimide group, which can rapidly and covalently conjugate with thiol groups, to prepare surface-modified liposomes (M-Lip) that prolong retention of doxorubicin (Dox) at tumor sites, enhancing its efficacy. Surface modification with the maleimide moiety had no effect on the drug loading efficiency or drug release properties. Compared to unmodified Lip/Dox, M-Lip/Dox was retained longer at the tumor site, it was taken up by 4T1 cells to a significantly greater extent, and exhibited stronger inhibitory effect against 4T1 cells. The in vivo imaging results showed that the retention time of M-Lip at the tumor was significantly longer than that of Lip. In addition, M-Lip/Dox also showed significantly higher anticancer efficacy and lower cardiotoxicity than Lip/Dox in mice bearing 4T1 tumor xenografts. Thus, the modification strategy with maleimide may be useful for achieving higher efficient liposome for tumor therapy.
Keywords: breast cancer; liposome; maleimide; doxorubicin; sustained release breast cancer; liposome; maleimide; doxorubicin; sustained release

Share and Cite

MDPI and ACS Style

Tang, C.; Yin, D.; Liu, T.; Gou, R.; Fu, J.; Tang, Q.; Wang, Y.; Zou, L.; Li, H. Maleimide-Functionalized Liposomes: Prolonged Retention and Enhanced Efficacy of Doxorubicin in Breast Cancer with Low Systemic Toxicity. Molecules 2022, 27, 4632. https://doi.org/10.3390/molecules27144632

AMA Style

Tang C, Yin D, Liu T, Gou R, Fu J, Tang Q, Wang Y, Zou L, Li H. Maleimide-Functionalized Liposomes: Prolonged Retention and Enhanced Efficacy of Doxorubicin in Breast Cancer with Low Systemic Toxicity. Molecules. 2022; 27(14):4632. https://doi.org/10.3390/molecules27144632

Chicago/Turabian Style

Tang, Chuane, Dan Yin, Tianya Liu, Rui Gou, Jiao Fu, Qi Tang, Yao Wang, Liang Zou, and Hanmei Li. 2022. "Maleimide-Functionalized Liposomes: Prolonged Retention and Enhanced Efficacy of Doxorubicin in Breast Cancer with Low Systemic Toxicity" Molecules 27, no. 14: 4632. https://doi.org/10.3390/molecules27144632

APA Style

Tang, C., Yin, D., Liu, T., Gou, R., Fu, J., Tang, Q., Wang, Y., Zou, L., & Li, H. (2022). Maleimide-Functionalized Liposomes: Prolonged Retention and Enhanced Efficacy of Doxorubicin in Breast Cancer with Low Systemic Toxicity. Molecules, 27(14), 4632. https://doi.org/10.3390/molecules27144632

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