Abstract

Relationship between the transfection efficiency and the supramolecular structure of the lipoplexes consisting of DNA, a benzyl amine derivative (BA), and two neutral co-lipids (DOPE and DLPC) were examined. At a composition of BA:DOPE:DLPC = 1:2:1; where the highest efficiency was attained, SAXS showed that the micelles before adding DNA formed a hexagonally-packed cylinder and addition of DNA improved the packing order. This phenomenon may be interpreted by intercalation of DNA between the preformed micellar cylinders. At a composition of BA: DLPC=1:1, where the lowest efficiency was observed, the micelle adopted a spherical form and addition of DNA induce a structural transition from the sphere to a hexagonally packed cylinder, and then a lamellar form. Fitting with a multilayer model suggested that DNA was included into the hydrophobic layer of the complex. Comparison of these two compositions suggests that difference in the DNA location in the lipoplex is related to the transfection efficiency.

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