title: Vitamin E succinate-conjugated F68 micelles for mitoxantrone delivery in enhancing anticancer activity.
abstract: Mitoxantrone (MIT) is a chemotherapeutic agent with promising anticancer efficacy. In this study, Pluronic F68-vitamine E succinate (F68-VES) amphiphilic polymer micelles were developed for delivering MIT and enhancing its anticancer activity. MIT-loaded F68-VES (F68-VES/MIT) micelles were prepared via the solvent evaporation method with self-assembly under aqueous conditions. F68-VES/MIT micelles were found to be of optimal particle size with the narrow size distribution. Transmission electron microscopy images of F68-VES/MIT micelles showed homogeneous spherical shapes and smooth surfaces. F68-VES micelles had a low critical micelle concentration value of 3.311 mg/L, as well as high encapsulation efficiency and drug loading. Moreover, F68-VES/MIT micelles were stable in the presence of fetal bovine serum for 24 hours and maintained sustained drug release in vitro. Remarkably, the half maximal inhibitory concentration (IC50) value of F68-VES/MIT micelles was lower than that of free MIT in both MDA-MB-231 and MCF-7 cells (two human breast cancer cell lines). In addition, compared with free MIT, there was an increased trend of apoptosis and cellular uptake of F68-VES/MIT micelles in MDA-MB-231 cells. Taken together, these results indicated that F68-VES polymer micelles were able to effectively deliver MIT and largely improve its potency in cancer therapy.
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People's Republic of China.
authors.forename: Yuling
authors.initials: Y
authors.lastname: Liu
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, People's Republic of China.
authors.forename: Yingqi
authors.initials: Y
authors.lastname: Xu
authors.affiliation: Department of Cell Biology and Anatomy, School of Medicine, University of Florida, Gainesville, FL, USA.
authors.forename: Minghui
authors.initials: M
authors.lastname: Wu
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People's Republic of China.
authors.forename: Lijiao
authors.initials: L
authors.lastname: Fan
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, People's Republic of China.
authors.forename: Chengwei
authors.initials: C
authors.lastname: He
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, People's Republic of China.
authors.forename: Jian-Bo
authors.initials: JB
authors.lastname: Wan
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, People's Republic of China.
authors.forename: Peng
authors.initials: P
authors.lastname: Li
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, People's Republic of China.
authors.forename: Meiwan
authors.initials: M
authors.lastname: Chen
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People's Republic of China.
authors.forename: Hui
authors.initials: H
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D003692:Delayed-Action Preparations / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D004705:Endocytosis / Q000187:drug effects; D005260:Female; D006801:Humans; D061986:MCF-7 Cells; D008823:Micelles; D008942:Mitoxantrone / Q000494:pharmacology*; D020442:Poloxamer / Q000138:chemical synthesis / Q000737:chemistry*; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared; D014810:Vitamin E / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D008823:Micelles; D020442:Poloxamer; D014810:Vitamin E; D008942:Mitoxantrone; C014225:tocophersolan
keywords: F68; cancer therapy; mitoxantrone; polymer micelles; vitamin E succinate