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盐酸倍他司汀经皮给药微乳的物理特性表征、生物物理评估、共聚焦成像和渗透研究。

Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

出版信息

Colloids Surf B Biointerfaces. 2013 Oct 1;110:254-60. doi: 10.1016/j.colsurfb.2013.05.007. Epub 2013 May 13.

Abstract

Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(®), Transcutol(®) and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.50±0.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride.

摘要

研究了盐酸倍他司汀包封在不同的油酸乙酯、Capryol 90(®)、Transcutol(®)和水微乳液制剂中的经皮给药。为所研究的微乳液系统构建了两种不同类型的相图。所研究的微乳液表现出了更适合皮肤给药的假塑性流动。建议采用平衡的双连续微乳液制剂,并显示出最高的渗透通量(0.50±0.030mgcm(-2)h(-1))。考察了微乳液对皮肤电阻的影响,以解释所获得的高渗透通量。共聚焦激光扫描显微镜用于确认渗透增强作用,并揭示渗透途径。研究结果表明,目前工作中提出的微乳液系统可以作为盐酸倍他司汀的一种有前途的替代给药方式。

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