Chen Zhi-Lan, Huang Man, Wang Xia-Rong, Fu Jun, Han Min, Shen You-Qing, Xia Zheng, Gao Jian-Qing
Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, PR China.
Department of General Intensive Care Unit,The Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, China.
Nanomedicine. 2016 Feb;12(2):421-30. doi: 10.1016/j.nano.2015.10.021. Epub 2015 Dec 19.
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.
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.
α-山竹黄酮（α-M）是一种多酚类氧杂蒽酮，可保护并提高大鼠大脑皮质神经元在抵抗Aβ寡聚体诱导的毒性时的存活率。α-M是治疗阿尔茨海默病（AD）的潜在候选药物。然而，该药物透过血脑屏障（BBB）的能力较差，限制了其疗效。在本研究中，我们用转铁蛋白（Tf）修饰α-M脂质体，并研究了脂质体在bEnd3细胞中的细胞内分布。此外，还检测了Tf(α-M)脂质体组中α-M穿过血脑屏障的情况。体外研究表明，Tf(α-M)脂质体能够以完整脂质体的形式穿过血脑屏障。关于α-M在脑中分布的体内研究结果表明，Tf(α-M)脂质体提高了α-M向脑内的递送。这些结果表明，Tf脂质体是α-M治疗AD的潜在载体。
已有报道称α-山竹黄酮（α-M）可作为治疗阿尔茨海默病（AD）的潜在药物。然而，其应用受到血脑屏障穿透性差的限制。作者在本研究中研究了用转铁蛋白修饰的脂质体对该药物的递送情况。阳性结果可能指向一种更好的脑靶向药物递送系统。
