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避免超变形脂质体在脱水时复溶失败。

Avoiding failed reconstitution of ultradeformable liposomes upon dehydration.

机构信息

Programa de Nanomedicinas, Laboratorio de Diseño de estrategias de Targeting de Drogas, Departamento de Ciencia y Tecnología, Universidad Nacional de Quilmes, Roque Saenz Peña 352, Bernal, Buenos Aires, Argentina.

出版信息

Int J Pharm. 2009 May 8;372(1-2):184-90. doi: 10.1016/j.ijpharm.2009.01.012. Epub 2009 Jan 21.

Abstract

Although freeze-drying is an ordinarily used technique to dehydrate conventional liposomes, we have found that ultradeformable liposomes (UDLs) suffered irreversible aggregation when rehydrated upon freeze-drying (99.4% water elimination), even in high sugar content (4/1 sucrose/lipid mass ratio). When dehydrated by speed vac and vacuum drying, two alternative techniques that rendered less pronounced dehydration (94.27 and 96.2% water elimination, respectively) and avoid ice formation, however, UDL could only be successfully rehydrated when vacuum dried in 4/1 sucrose/lipid mass ratios. Conventional liposomes, on the other hand, were successfully reconstituted upon dehydrated by the three methods in lower sugar content (2/1 sucrose/lipid mass ratio). These results indicated that the 27% mole sodium cholate within the UDL lipid matrix was responsible for a greater and differential mechanical sensitivity of the bilayers to the different dehydration stress, as compared to conventional liposomes.

摘要

虽然冷冻干燥是一种常用的技术来使普通脂质体脱水,但我们发现超变形脂质体(UDL)在冷冻干燥(去除 99.4%的水分)后再水合时会发生不可逆的聚集,即使在高糖含量(蔗糖/脂质质量比为 4/1)下也是如此。当通过超速真空和真空干燥进行脱水时,这两种替代技术的脱水程度较低(分别去除 94.27%和 96.2%的水分,且避免了冰的形成),然而,只有在蔗糖/脂质质量比为 4/1 且采用真空干燥时,UDL 才能成功水合。另一方面,普通脂质体在较低糖含量(蔗糖/脂质质量比为 2/1)下,通过这三种方法均可成功重建。这些结果表明,与普通脂质体相比,UDL 脂质基质内 27%摩尔的胆酸钠使双层膜对不同脱水应激的机械敏感性更大且不同。

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