Use of Liposomes on Modification of Stratum Corneum Lipids and Enhancement of Transdermal Drug Permeation

利用脂质体修饰角质层脂质并增强药物透皮渗透

基本信息

批准号：
13672264
负责人：
KITAGAWA Shuji
金额：
$ 2.3万
依托单位：
Nigata University of Phermacy and Applied Life Sciences
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2001
资助国家：
日本
起止时间：
2001 至 2003
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-13672264/
关键词：
skin stratum corneum lipids cationic liposomes ceramide cationic surfactant retinoic acid transdermal permeation erythrocyte membrane 二本鎖カチオン性界面活性剤 ESR 吸収促進剤界面活性剤スピンラベル

项目摘要

With the aim of efficient delivery of lipids and lipid analogs to skin, we studied the stability of cationic liposomes containing double-chained cationic surfactants, the interaction of the liposomes with erythrocyte membrane as well as that with skin. Dimethyldipalmitylammonium formed stable liposomes in the presence of phosphatidylcholines with unsaturated acy1 chains, whereas 1,2-dioleoyl-3-trimethylammonium propane formed the stable liposomes even in the presence of phosphatidylcholines with saturated acy1 chains. These cationic liposomes induced aggregation and fusion of the erythrocytes. By using such interaction of the liposomes with biological membranes we tried to deliver ceramide to lipid deficient skin. We confirmed that ceramide and dimethyl-dipalmitylammonium formed stable bilayer vesicles in the presence of cholesterol at a molar ratio of 1:1:1. The addition of the cationic liposomes to 80% ethanol-treated delipidized guinea pig dorsal skin slightly recovered the rigidity of the stratum corneum lipid lamella and had a tendency to recover its barrier function. We furthermore found the enhanced incorporation of retinoic acid using cationic liposomes. Through these findings we clarified the usefulness of the cationic liposomes to efficient delivery of lipids and lipid analogs to skin.

为了将脂质和脂质类似物有效递送至皮肤，我们研究了含有双链阳离子表面活性剂的阳离子脂质体的稳定性、脂质体与红细胞膜以及与皮肤的相互作用。二甲基二棕榈基铵在具有不饱和 acy1 链的磷脂酰胆碱存在下形成稳定的脂质体，而 1,2-二油酰基-3-三甲基丙烷即使在具有饱和 acy1 链的磷脂酰胆碱存在下也形成稳定的脂质体。这些阳离子脂质体诱导红细胞聚集和融合。通过利用脂质体与生物膜的这种相互作用，我们尝试将神经酰胺递送至脂质缺乏的皮肤。我们证实，神经酰胺和二甲基二棕榈基铵在胆固醇存在下以 1:1:1 的摩尔比形成稳定的双层囊泡。将阳离子脂质体添加到经80%乙醇处理的脱脂豚鼠背部皮肤中，可使角质层脂层的刚性略有恢复，并有恢复其屏障功能的趋势。我们还发现使用阳离子脂质体增强了视黄酸的掺入。通过这些发现，我们阐明了阳离子脂质体在将脂质和脂质类似物有效递送至皮肤方面的有用性。