Laboratoire de Conception et Application de Molécules Bioactives, Equipe de BioVectorologie, UMR 7199 CNRS/Université de Strasbourg, Faculté de Pharmacie, Illkirch, France.
J Liposome Res. 2013 Mar;23(1):11-9. doi: 10.3109/08982104.2012.717298. Epub 2012 Oct 1.
A modified and derived ethanol injection (MDEI) process was developed to produce liposomes. The aim of the present study was to more efficiently control the vesicle diameter than with the conventional ethanol injection method. A hot ethanolic solution of lipids (60°C) was injected into a hot aqueous buffer (70°C). Then, ethanol was removed by rotary evaporation under reduced pressure. The size of the liposomes could be controlled by the ratio of ethanol to hydroalcoholic solution before evaporation. The concentration of lipids, the charge of lipids, and the type of aqueous phase had little effect on the vesicle diameter when the process involved a ratio of 33% (v/v) ethanol. In addition, it was possible to obtain lipid concentrations 10- to 30-fold higher that the conventional ethanol injection method. The encapsulation of a hydrophilic compound was feasible with this MDEI process. The observation by cryogenic transmission electron microscopy revealed that these liposomes were predominantly unilamellar at a ratio as high as 33 or 50% (v/v) ethanol. Thus, the results showed that MDEI is an appropriate alternative for the manufacture of liposomes with respect to the ethanol injection process.
一种改良和衍生的乙醇注入（MDEI）工艺被开发用于生产脂质体。本研究的目的是比传统的乙醇注入方法更有效地控制囊泡直径。将脂质的热乙醇溶液（60°C）注入热的水性缓冲液（70°C）中。然后，通过减压旋转蒸发除去乙醇。通过蒸发前乙醇与水醇溶液的比例可以控制脂质体的大小。当涉及 33%（v/v）乙醇的比例时，脂质的浓度、脂质的电荷和水相的类型对囊泡直径几乎没有影响。此外，与传统的乙醇注入方法相比，可以获得 10 至 30 倍更高的脂质浓度。这种 MDEI 工艺可以实现亲水性化合物的包封。低温透射电子显微镜观察表明，在高达 33%或 50%（v/v）乙醇的比例下，这些脂质体主要是单分子层的。因此，结果表明，与乙醇注入工艺相比，MDEI 是制造脂质体的一种合适的替代方法。
