Quetiapine Nanoemulsion for Intranasal Drug Delivery: Evaluation of Brain-Targeting Efficiency
Quetiapine Nanoemulsion for Intranasal Drug Delivery: Evaluation of Brain-Targeting Efficiency
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DOI：
10.1208/s12249-016-0552-9
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发表时间：
2017-04-01
影响因子：
3.3
通讯作者：
Pokharkar, Varsha
中科院分区：
文献类型：
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作者：
Boche, Mithila;Pokharkar, Varsha
为了评价改善富马酸奎替鲁胺（QTP）药物递送的可能性，开发了用于鼻内递送的纳米乳系统。研究了Emalex LWIS 10、PEG 400和Transcutol P作为助表面活性剂的不同HLB值对以Capmul MCM（CPM）为油相、Tween 80为表面活性剂和水组成的纳米乳液体系拟三元相图各向同性区域的影响。对纳米乳的相行为、粒径大小、透射电镜照片及脑靶向性进行了研究。平均直径为144 +/- 0.5 nm的优化纳米乳制剂的体外溶出研究显示，与纯药物相比，药物释放增加了两倍以上。根据Wistar大鼠体内组织分布研究结果，与静脉给药相比，鼻内给药QTP纳米乳的Tmax较短。纳米乳实现了更高的药物转运效率（DTE%）和直接鼻-脑药物转运（DTP%）。纳米乳系统可能是一种有前途的脑靶向给药策略。
To evaluate the possibility of improved drug delivery of quetiapine fumarate (QTP), a nanoemulsion system was developed for intranasal delivery. Effects of different HLBs of Emalex LWIS 10, PEG 400 and Transcutol P, as co-surfactants, were studied on isotropic region of pseudoternary-phase diagrams of nanoemulsion system composed of capmul MCM (CPM) as oil phase, Tween 80 as surfactant and water. Phase behaviour, globule size, transmission electron microscope (TEM) photographs and brain-targeting efficiency of quetiapine nanoemulsion were investigated. In vitro dissolution study of optimised nanoemulsion formulation, with mean diameter 144 +/- 0.5 nm, showed more than twofold increase in drug release as compared with pure drug. According to results of in vivo tissue distribution study in Wistar rats, intranasal administration of QTP-loaded nanoemulsion had shorter T-max compared with that of intravenous administration. Higher drug transport efficiency (DTE%) and direct nose-to-brain drug transport (DTP%) was achieved by nanoemulsion. The nanoemulsion system may be a promising strategy for brain-targeted delivery of QTP.