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鼻腔内给予含 CNS 作用药物的纳米结构脂质载体:药效学研究及在血液和脑中的评估。

Intranasal administration of nanostructured lipid carriers containing CNS acting drug: pharmacodynamic studies and estimation in blood and brain.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, India.

出版信息

J Psychiatr Res. 2012 Sep;46(9):1133-8. doi: 10.1016/j.jpsychires.2012.05.014. Epub 2012 Jun 30.

Abstract

The present study was aimed to investigate and compare the efficacy of duloxetine (DLX) loaded nanostructured lipid carriers (NLC) with DLX solution pharmacodynamically following intranasal administration. The study was further conducted to estimate DLX concentration in brain and blood. DLX was administered to albino Wistar rats either intranasally or orally in solution form (DLX solution) or encapsulated in NLC (DLX-NLC). These were evaluated in-vivo for pharmacodynamic studies for depression by forced swimming test and locomotor activity test. Intranasal DLX-NLC treatment exhibited improved behavioural analysis results (swimming, climbing, and immobility) than the DLX solution after 24 h of study. Furthermore, DLX-NLC significantly increased the total swimming and climbing time when compared with control and significantly reduced the immobility period. The intranasal DLX-NLC demonstrated improved locomotor activity when compared with DLX solution. Amount of DLX was quantified in blood and brain after the forced swimming test. The intranasal DLX-NLC demonstrated higher concentration in brain compared with DLX solution. Thus, intranasal DLX-NLC was found to be a promising formulation for the treatment of depression.

摘要

本研究旨在通过鼻腔给药,从药效学角度比较和研究多柔比星(DLX)负载的纳米结构脂质载体(NLC)与 DLX 溶液的疗效。本研究还进一步估算了脑和血液中的 DLX 浓度。将 DLX 以溶液形式(DLX 溶液)或包封在 NLC 中(DLX-NLC)施用于白化 Wistar 大鼠,经鼻腔或口服给药。通过强迫游泳试验和运动活性试验对这些药物进行体内药效学研究。与研究 24 小时后的 DLX 溶液相比,鼻腔内 DLX-NLC 治疗表现出改善的行为分析结果(游泳、攀爬和不动)。此外,与对照组相比,DLX-NLC 显著增加了总游泳和攀爬时间,显著减少了不动期。与 DLX 溶液相比,鼻腔内 DLX-NLC 显示出改善的运动活性。强迫游泳试验后,在血液和大脑中定量了 DLX 的含量。与 DLX 溶液相比,鼻腔内 DLX-NLC 在大脑中的浓度更高。因此,鼻腔内 DLX-NLC 被发现是治疗抑郁症的一种有前途的制剂。

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