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Open AccessArticle

Anticancer Effect of Metformin in Herceptin-Conjugated Liposome for Breast Cancer

by Ji-Yeon Lee 1,†, Dae Hwan Shin 2 and Jin-Seok Kim 1,*
Drug Information Research Institute (DIRI), College of Pharmacy, Sookmyung Women’s University, Cheongparo 47 gil 100, Yongsan gu, Seoul 04310, Korea
College of Pharmacy, Chungbuk National University, Cheongju 28160, Korea
Author to whom correspondence should be addressed.
Present address: Kolon Pharma R&D Center, 45 18-gil, Munpyeongseo-ro, Daedeog-gu, Daejeon 34302, Korea.
Pharmaceutics 2020, 12(1), 11;
Received: 22 October 2019 / Revised: 27 November 2019 / Accepted: 18 December 2019 / Published: 20 December 2019
(This article belongs to the Special Issue Advances in Liposome-Based Drug Delivery Systems)
Metformin (MET) is an anti-diabetic drug effective against breast cancer, targeting breast cancer stem cells (BCSCs). MET-encapsulating liposome (LP-MET) and Herceptin-conjugated LP-MET (Her-LP-MET) were evaluated for their anti-cancer effect in vitro and in vivo. Size and zeta potentials of LP-MET and Her-LP-MET were suitable for enhanced permeability and retention effects. Her-LP-MET yielded greater inhibition of BCSC proliferation in vitro than free MET or LP-MET, as well as a dose-dependent long-term anti-proliferation effect. Further, the anti-migration effect of Her-LP-MET on BCSCs was superior to that of MET or LP-MET, and was enhanced when used in concert with doxorubicin (DOX). In a mouse model, Her-LP-MET combined with free DOX was more effective than free MET, free DOX, or Her-LP-MET. Moreover, Her-LP-MET combined with free DOX yielded tumor remission, whereas free DOX alone resulted in metastasis or death. As such, Her-LP-MET formulation is expected to provide a new therapeutic modality targeting BCSCs. View Full-Text
Keywords: Metformin; Herceptin; breast cancer stem cell; liposome; targeting Metformin; Herceptin; breast cancer stem cell; liposome; targeting
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MDPI and ACS Style

Lee, J.-Y.; Shin, D.H.; Kim, J.-S. Anticancer Effect of Metformin in Herceptin-Conjugated Liposome for Breast Cancer. Pharmaceutics 2020, 12, 11.

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