Monteiro-Riviere N A, Inman A O, Mak V, Wertz P, Riviere J E
Center for Cutaneous Toxicology and Residue Pharmacology, North Carolina State University, Raleigh, USA.
Pharm Res. 2001 Jul;18(7):992-8. doi: 10.1023/a:1010944529387.
To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig.
Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yorkshire pigs. Three solvent extraction stages were I, cyclohexane (5 ml for three, 1-min extractions): II, cyclohexane/ethanol (4:1) (5 ml for three, 1-min extractions): and III, cyclohexane/ethanol (1:4) (5 ml for three, 3-min extractions) extracted as follows: Site A, Stage I: Site B, Stage I and II; Site C, Stage I, II and III. Erythema, edema, and TEWL were assessed in control, tape-stripped, and extracted sites at 0, 6, and 24 h. The extracted lipids were analyzed by thin layer chromatography and quantified by densitometry for ceramide, cholesterol, cholesterol esters, fatty acids, and triglycerides.
The change in TEWL (delta TEWL) in 14 of the 15 sites was the highest at 24 h and generally increased with each additional extraction. The greatest changes were present in the back. Each extraction stage removed specific lipids in reproducible quantities that caused the delta TEWL to increase from 0 to 24 h. Lipid removal was verified by transmission electron microscopy. The mean total lipid concentration depended on extraction solvents and body region, and was reproducible across sites and regions at equivalent stages of lipid extraction. Relative proportions of individual lipids extracted were similar across all body regions. Higher concentrations of total lipids were extracted from the back. CONCLUSIONS. These studies demonstrate that extraction of lipids increased the delta TEWL to a level similar to repeated tape stripping at all body sites in the pig. This study suggested that strategies that could biochemically alter epidermal lipid composition may increase absorption of simultaneously administered topical compounds and may be useful to enhance drug delivery.
评估选择性脂质提取和胶带剥离对猪三个身体部位经表皮水分流失(TEWL)的影响。
采用三种不同的溶剂提取程序或对约克夏猪进行玻璃纸胶带剥离(15次),从腹部、腹股沟和背部提取脂质。三个溶剂提取阶段分别为:I,环己烷(5毫升,每次提取1分钟,共提取三次);II,环己烷/乙醇(4:1)(5毫升,每次提取1分钟,共提取三次);III,环己烷/乙醇(1:4)(5毫升,每次提取3分钟,共提取三次),提取方式如下:部位A,阶段I;部位B,阶段I和II;部位C,阶段I、II和III。在0、6和24小时对对照部位、胶带剥离部位和提取部位的红斑、水肿和TEWL进行评估。提取的脂质通过薄层色谱法进行分析,并通过密度测定法定量分析神经酰胺、胆固醇、胆固醇酯、脂肪酸和甘油三酯。
15个部位中有14个部位的TEWL变化(ΔTEWL)在24小时时最高,并且通常随着每次额外提取而增加。背部的变化最大。每个提取阶段去除的特定脂质数量可重复,导致ΔTEWL从0小时到24小时增加。通过透射电子显微镜验证了脂质的去除。平均总脂质浓度取决于提取溶剂和身体部位,并且在脂质提取的等效阶段跨部位和区域具有可重复性。所有身体部位提取的单个脂质的相对比例相似。从背部提取的总脂质浓度更高。结论。这些研究表明,脂质提取使猪所有身体部位的ΔTEWL增加到与重复胶带剥离相似的水平。本研究表明,能够生物化学改变表皮脂质组成的策略可能会增加同时给药的局部化合物的吸收,并且可能有助于增强药物递送。