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曲安奈德多层脂质体:制备、稳定性及特性研究

Multilamellar liposomes of triamcinolone acetonide: preparation, stability, and characterization.

作者信息

Clares B, Gallardo V, Medina M M, Ruiz Ma A

机构信息

Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, Granada, Spain.

出版信息

J Liposome Res. 2009;19(3):197-206. doi: 10.1080/08982100902736571.

Abstract

The aim of this study was to assess and characterize the stability of multilamellar liposomes as a delivery vehicle for triamcinolone acetonide. A standardized preparation method for a liposomal delivery vehicle was developed, after varying composition and storage conditions, and assessing encapsulation efficiency and loss of active principle. The assessment of temperature as a factor in formula stability during storage showed that stability improved under refrigeration (4-6 degrees C) (less early diffusion of active principle through the liposomal wall), in comparison with samples stored at room temperature. To improve stability, cholesterol was added to some formulae, which although resulting in a decrease in average encapsulation efficiency, mitigated subsequent losses of retained active principle (formulae 4, 5, and 6), in comparison with those without cholesterol (formulae 1, 2, and 3). This was evident both under refrigerated and room-temperature conditions. Finally, after testing the effects of adding an antioxidant and/or preservative to the formulae, a liposomal design was achieved with acceptable stability, vesicle dimensions, and encapsulation efficiency.

摘要

本研究的目的是评估和表征多层脂质体作为曲安奈德递送载体的稳定性。在改变组成和储存条件,并评估包封效率和活性成分损失之后,开发了一种脂质体递送载体的标准化制备方法。对温度作为储存期间配方稳定性的一个因素进行评估表明,与室温下储存的样品相比,冷藏(4 - 6摄氏度)时稳定性提高(活性成分通过脂质体壁的早期扩散较少)。为了提高稳定性,向一些配方中添加了胆固醇,与未添加胆固醇的配方(配方1、2和3)相比,虽然这导致平均包封效率降低,但减轻了保留的活性成分随后的损失(配方4、5和6)。这在冷藏和室温条件下均很明显。最后,在测试向配方中添加抗氧化剂和/或防腐剂的效果之后,实现了一种具有可接受的稳定性、囊泡尺寸和包封效率的脂质体设计。

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