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含透明质酸微乳剂的研制与表征

Development and characterization of microemulsions containing hyaluronic acid.

作者信息

Alkrad Jamal Alyoussef, Mrestani Yahya, Neubert Reinhard H H

机构信息

Faculty of Pharmacy, Isra University, PO Box 22 and 23, Amman, Jordan.

Institute of Applied Dermatopharmacy, Weinbergweg 23, 06120 Halle/Saale, Germany.

出版信息

Eur J Pharm Sci. 2016 Apr 30;86:84-90. doi: 10.1016/j.ejps.2016.02.008. Epub 2016 Feb 20.

DOI:10.1016/j.ejps.2016.02.008
PMID:26902172
Abstract

Tween80 and Span20 were used as surfactant mixture for developing non-ionic microemulsions (MEs) containing hyaluronic acid 22 kDa (HA). The effect of Tween80:Span20 ratio (T:S ratio) on microemulsion (ME) water intake and stability was studied. Moreover, the effect of HA on the consumed surfactant amount which is for stabilizing the MEs, for reducing water intake was investigated. Two W/O MEs containing HA were optimized. The first ME was composed of 2% HA, 13.8% Tween:80:Span20 (2:3), 4.2% water and 79.9% isopropylpalmitate (IPP). The second was composed of 2% HA, 16% Span20, 9.6% water:dimethyl sulfoxide (W:DMSO) (6:3.6) and 72.4% medium chain triglycerides (MCTG). The droplet sizes of MEs were determined using dynamic light scattering (DLS). The multilayer membrane system (MLMS) was used for testing the release of HA from both MEs and the released amount of HA was quantified using capillary zone electrophoresis (CZE). Furthermore, three phase diagrams and relevant rheological characteristics were generated. The droplet size of the ME without HA decreased and increased with increasing the temperature. Furthermore, the droplet size of the IPP-ME and MCTG-ME without HA and of the MCTG-ME with HA decreased with increasing temperature. In contrast to this results, the droplet size of the IPP-ME with HA increased with increased temperature. This ME belongs to the Newtonian fluids. Compared to the first ME, the second ME shows droplet sizes at 25 °C of 6.5 nm without and 37 nm with HA. The droplet size in the second ME decreased proportionally with an increase of the temperature with and without HA. The release of HA was faster from the IPP ME compared to the MCTG-ME. The two developed MEs were stable, isotropic and their properties comply with ME properties concerning the droplet size and viscosity.

摘要

吐温80和司盘20用作表面活性剂混合物,用于制备含22 kDa透明质酸(HA)的非离子微乳(ME)。研究了吐温80:司盘20比例(T:S比例)对微乳(ME)吸水量和稳定性的影响。此外,还研究了HA对用于稳定微乳、减少吸水量的表面活性剂消耗量的影响。优化了两种含HA的油包水微乳。第一种微乳由2% HA、13.8%吐温80:司盘20(2:3)、4.2%水和79.9%异丙基棕榈酸酯(IPP)组成。第二种由2% HA、16%司盘20、9.6%水:二甲基亚砜(W:DMSO)(6:3.6)和72.4%中链甘油三酯(MCTG)组成。使用动态光散射(DLS)测定微乳的液滴大小。采用多层膜系统(MLMS)测试两种微乳中HA的释放情况,并使用毛细管区带电泳(CZE)对HA的释放量进行定量。此外,绘制了三相图和相关流变特性。不含HA的微乳的液滴大小随温度升高先减小后增大。此外,不含HA的IPP - ME和MCTG - ME以及含HA的MCTG - ME的液滴大小随温度升高而减小。与该结果相反,含HA的IPP - ME的液滴大小随温度升高而增大。这种微乳属于牛顿流体。与第一种微乳相比,第二种微乳在25℃时不含HA的液滴大小为6.5 nm,含HA的为37 nm。第二种微乳中含HA和不含HA时,液滴大小均随温度升高成比例减小。与MCTG - ME相比,HA从IPP - ME中的释放更快。所开发的两种微乳稳定、各向同性,其性质在液滴大小和粘度方面符合微乳的性质。

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