Transferrin-modified liposome promotes α-mangostin to penetrate the blood-brain barrier

alpha-Mangostin (alpha-M) is a polyphenolic xanthone that protects and improves the survival of cerebral cortical neurons against A beta oligomer-induced toxicity in rats. alpha-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 alpha-M liposome with transferrin (Tf) and investigated the intracellular distribution of liposomes in bEnd3 cells. In addition, the transport of alpha-M across the BBB in the Tf(alpha-M) liposome group was examined. In vitro studies demonstrated that the Tf(alpha-M) liposome could cross the BBB in the form of an integrated liposome. Results of the in vivo studies on the alpha-M distribution in the brain demonstrated that the Tf(alpha-M) liposome improved the brain delivery of alpha-M. These results indicated that the Tf liposome is a potential carrier of alpha-M against AD. From the Clinical Editor: The use of alpha-Mangostin (alpha-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. (c) 2015 Elsevier Inc. All rights reserved.