Liu F, Yang J, Huang L, Liu D
Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pennsylvania 15261, USA.
Pharm Res. 1996 Nov;13(11):1642-6. doi: 10.1023/a:1016480421204.
To study the structure-function relationship of non-ionic surfactants in emulsion-mediated gene delivery.
Four different types of non-ionic surfactants including Tween, Span, Brij and pluronic copolymers were used as co-emulsifiers for preparation of emulsions composed of Castor oil, dioleoylphosphatidylethanolamine (DOPE) and 3 beta [N-(N', N'-dimethylaminoethane) carbamoyl] cholesterol (DC-Chol). The effect of different surfactants on the formation of DNA/emulsion complexes and transfection activity were analyzed using plasmid DNA containing luciferase cDNA as a reporter gene.
Non-ionic surfactants containing branched polyoxyethylene chains as the hydrophilic head group were more effective in preventing the formation of large DNA/emulsion complexes than those containing one or no polyoxyethylene chain. All emulsion formulations except those containing Brij 700 exhibited high activity in transfecting mouse BL-6 cells in the absence of serum. In the presence of serum, however, transfection activity of each formulation varied significantly. Emulsions containing Tween, Brij 72, pluronic F68 and F127 demonstrated increased activity in transfecting cells in the presence of 20% serum. In contrast to emulsions containing Span, long chain polyoxyethylene of Brij showed decreased transfection activity. The particle size of the DNA/emulsion complexes and their ability to transfect cells are dependent on the concentration of non-ionic surfactant in the formulation.
The structure of the hydrophilic head group of the non-ionic surfactants in the emulsion is important in determining how DNA molecules interact with emulsions and the extent to which DNA is transferred inside the cell.
研究非离子表面活性剂在乳液介导的基因递送中的结构-功能关系。
使用四种不同类型的非离子表面活性剂，包括吐温、司盘、Brij和普朗尼克共聚物作为助乳化剂，制备由蓖麻油、二油酰磷脂酰乙醇胺（DOPE）和3β-[N-(N',N'-二甲基氨基乙烷)氨基甲酰]胆固醇（DC-Chol）组成的乳液。以含有荧光素酶cDNA的质粒DNA作为报告基因，分析不同表面活性剂对DNA/乳液复合物形成和转染活性的影响。
含有支链聚氧乙烯链作为亲水头部基团的非离子表面活性剂比含有一个或没有聚氧乙烯链的表面活性剂在防止形成大的DNA/乳液复合物方面更有效。除了含有Brij 700的那些乳液制剂外，所有乳液制剂在无血清情况下转染小鼠BL-6细胞时均表现出高活性。然而，在有血清存在时，每种制剂的转染活性差异显著。含有吐温、Brij 72、普朗尼克F68和F127的乳液在20%血清存在下转染细胞的活性增加。与含有司盘的乳液相反，Brij的长链聚氧乙烯表现出降低的转染活性。DNA/乳液复合物的粒径及其转染细胞的能力取决于制剂中非离子表面活性剂的浓度。
乳液中非离子表面活性剂亲水头部基团的结构对于确定DNA分子与乳液的相互作用方式以及DNA在细胞内的转移程度很重要。
