title: Transferrin-modified liposome promotes α-mangostin to penetrate the blood-brain barrier.
abstract: α-Mangostin (α-M) is a polyphenolic xanthone that protects and improves the survival of cerebral cortical neurons against Aβ oligomer-induced toxicity in rats. α-M is a potential candidate as a treatment for Alzheimer's disease (AD). However, the efficacy was limited by the poor penetration of the drug through the blood-brain barrier (BBB). In this study, we modified the α-M liposome with transferrin (Tf) and investigated the intracellular distribution of liposomes in bEnd3 cells. In addition, the transport of α-M across the BBB in the Tf(α-M) liposome group was examined. In vitro studies demonstrated that the Tf(α-M) liposome could cross the BBB in the form of an integrated liposome. Results of the in vivo studies on the α-M distribution in the brain demonstrated that the Tf(α-M) liposome improved the brain delivery of α-M. These results indicated that the Tf liposome is a potential carrier of α-M against AD.
  
  
  BACKGROUND
  The use of α-Mangostin (α-M) as a potential agent to treat Alzheimer's disease (AD) has been reported. However, its use is limited by the poor penetration through the blood brain barrier. The delivery of this agent by transferrin-modified liposomes was investigated by the authors in this study. The positive results could point to a better drug delivery system for brain targeting.
authors.affiliation: Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, PR China. Electronic address: chenzhilan786@163.com.
authors.forename: Zhi-Lan
authors.initials: ZL
authors.lastname: Chen
authors.affiliation: Department of General Intensive Care Unit,The Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, China. Electronic address: huangman@zju.edu.cn.
authors.forename: Man
authors.initials: M
authors.lastname: Huang
authors.affiliation: Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, PR China. Electronic address: wxrniki@163.com.
authors.forename: Xia-Rong
authors.initials: XR
authors.lastname: Wang
authors.affiliation: Institute of Clinical trial, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai, China. Electronic address: sy_gcp@126.com.
authors.forename: Jun
authors.initials: J
authors.lastname: Fu
authors.affiliation: Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, PR China. Electronic address: hanmin@zju.edu.cn.
authors.forename: Min
authors.initials: M
authors.lastname: Han
authors.affiliation: Center for Bionanoengineering and State Key Laboratory of Chemical Engineering, Zhejiang University, Hangzhou, PR China. Electronic address: shenyq@zju.edu.cn.
authors.forename: You-Qing
authors.initials: YQ
authors.lastname: Shen
authors.affiliation: Laboratory Animal Research Center, Zhejiang Chinese Medical University, Hangzhou, China. Electronic address: volcano_xia@163.com.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Xia
authors.affiliation: Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, PR China. Electronic address: gaojianqing@zju.edu.cn.
authors.forename: Jian-Qing
authors.initials: JQ
authors.lastname: Gao
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy; D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism*; D001921:Brain / Q000378:metabolism; D002460:Cell Line; D016503:Drug Delivery Systems; D029762:Garcinia mangostana / Q000737:chemistry; D008081:Liposomes / Q000378:metabolism*; D051379:Mice; D018696:Neuroprotective Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D017207:Rats, Sprague-Dawley; D014168:Transferrin / Q000378:metabolism*; D044004:Xanthones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D008081:Liposomes; D018696:Neuroprotective Agents; D014168:Transferrin; D044004:Xanthones; C021053:mangostin
keywords: Alzheimer's disease; Brain-targeting; Liposome; Transferrin; α-Mangostin