期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 271, 期 1-2, 页码 5-10出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2003.09.018
关键词
skin penetration enhancer; DDAIP; mechanism; dipalmitoylphosphatidylcholine liposomes; differential scanning calorimetry
Differential scanning calorimetry (DSC) was used to investigate the mechanism of action of a proprietary skin penetration enhancer, dodecyl-2-(N,N-dimethylamino)propionate (DDAIP) in dipalmitoylphosphatidylcholine (DPPC) liposomes. Furthermore, the effect of enhancer concentration on lipid thermotropic transitions was investigated. With increasing concentrations of DDAIP (from 5 to 50 mol%), the main transition peak shifted to lower temperatures and became more broad. The pretransition peak also shifted to lower temperatures with increasing concentrations of DDAIP and disappeared completely above an enhancer concentration of 20 mol%. Main transition and pretransition enthalpies of reaction decreased with increasing DDAIP concentration, indicating that enhancer treatment destabilized both rippled gel and liquid crystal phases within the bilayer. At and above a DDAIP concentration of 33.3 mol%, an additional transition was evident, indicating the presence of two phases of enhancer-lipid complex. Results suggest that DDAIP enhances drug transport by interacting with the polar region of the phospholipid bilayer and also by increasing the motional freedom of lipid hydrocarbon chains. (C) 2003 Elsevier B.V. All rights reserved.
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