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一种使用膜接触器制备脂质体的新方法。

A new method for liposome preparation using a membrane contactor.

机构信息

Université de Lyon, Lyon, France.

出版信息

J Liposome Res. 2011 Sep;21(3):213-20. doi: 10.3109/08982104.2010.517537. Epub 2010 Sep 22.

Abstract

In this article, we present a novel, scalable liposomal preparation technique suitable for the entrapment of pharmaceutical agents into liposomes. This new method is based on the ethanol-injection technique and uses a membrane contactor module, specifically designed for colloidal system preparation. In order to investigate the process, the influence of key parameters on liposome characteristics was studied. It has been established that vesicle-size distribution decreased with a decrease of the organic-phase pressure, an increase of the aqueous-phase flow rate, and a decrease of the phospholipid concentration. Additionally, special attention was paid on reproducibility and long-term stability of lipid vesicles, confirming the robustness of the membrane contactor-based technique. On the other hand, drug-loaded liposomes were prepared and filled with two hydrophobic drug models. High entrapment-efficiency values were successfully achieved for indomethacin (63%) and beclomethasone dipropionate (98%). Transmission electron microscopy images revealed nanometric quasispherical-shaped multilamellar vesicles (size ranging from 50 to 160 nm).

摘要

在本文中,我们提出了一种新颖的、可扩展的脂质体制备技术,适用于将药物包封到脂质体中。这种新方法基于乙醇注入技术,并使用了专门设计用于胶体系统制备的膜接触器模块。为了研究该工艺,我们研究了关键参数对脂质体特性的影响。结果表明,随着有机相压力的降低、水相流速的增加和磷脂浓度的降低,囊泡的粒径分布减小。此外,我们特别关注脂质体的重现性和长期稳定性,证实了基于膜接触器的技术的稳健性。另一方面,我们制备了载药脂质体并填充了两种疏水性药物模型。成功地实现了吲哚美辛(63%)和倍氯米松二丙酸酯(98%)的高包封效率。透射电子显微镜图像显示出纳米级准球形多层囊泡(尺寸范围为 50 至 160nm)。

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