外用甲氨蝶呤柔性纳米脂质体透皮吸收的效果  

Effect of external flexible nanonipsomes of methotrexate on percutaneous absorption

作　　者：王娟[1] 梁清华[1] 范荣[1] 唐涛[1] 熊新贵[1] 陈疆[1] 

机构地区：[1]中南大学湘雅医院中西结合科,湖南省长沙市410008

出　　处：《中国组织工程研究与临床康复》2007年第9期1689-1691,共3页Journal of Clinical Rehabilitative Tissue Engineering Research

基　　金：湖南省科委课题基金资助(05SK3005);湖南省重点学科建设经费资助(湘教通[2001]179号)~~

摘　　要：目的:观察以皮肤给药缓释系统为载体的柔性脂质体甲氨蝶呤柔性纳米脂质体制剂的体外透皮吸收情况。方法:实验于2005-03/11在中南大学湘雅医院中西结合研究所完成。15只健康的SD大鼠随机分为3组:质量分数为0.0025的甲氨蝶呤外敷剂组、质量分数为0.005的外用甲氨蝶呤柔性纳米脂质体组和质量分数为0.0025的外用甲氨蝶呤柔性纳米脂质体组,每组5只。采用Franz扩散池,分别将质量分数为0.0025的外用甲氨蝶呤柔性纳米脂质体0.3g、质量分数为0.005的外用甲氨蝶呤柔性纳米脂质体0.15g和质量分数为0.0025的甲氨蝶呤外敷剂0.3g(含甲氨蝶呤均为0.75mg)均匀涂布于大鼠皮肤角质层表面,分别于2,4,6,8,10,12h用0.45μm微孔滤膜过滤。滤液用生理盐水稀释至10mL,于306nm处测定吸光度值,扣除生理盐水后的吸光度值代入标准曲线,计算累积透过量和12h累积透过率,对比3种制剂经大鼠皮肤的体外透皮吸收差异。结果:质量分数为0.0025,0.005的外用甲氨蝶呤柔性纳米脂质体组累积透过量、12h累积透过率均高于质量分数为0.0025的甲氨蝶呤外敷剂组,差异有显著性意义[12h累积透过率分别为(67.51±0.37)%,(72.79±0.03)%,(24.50±0.08)%,t=325.71,247.24,P<0.01];质量分数为0.0025的外用甲氨蝶呤柔性纳米脂质体组与质量分数为0.005的外用甲氨蝶呤柔性纳米脂质体组累积透过量、12h累积透过率差异无显著性意义(P>0.05)。结论:甲氨蝶呤柔性纳米脂质具有效渗透皮肤组织的作用。AIM： To study the percutaneous absorption in vitro of flexible nanonipsomes of methotrexate （MTX） for external application. METHODS： The experiment was completed .in Institute of Combined Traditional Chinese and Western Medicine, Xiangya Hospital of Central South University between March and November in 2005. Totally 15 healthy SD rats randomly divided into 3 groups： 0.002 5 MTX external application group （n =5）, 0.005 flexible nanonipsomes of MTX for external application group （n =5） and the 0.002 5 flexible nanonipsomes of MTX for external application group （n =5）. Rat keratoderma was evenly coated with 1.5 g of flexible nanonipsomes of MTX for external application （the quality fraction was 0.002 5）, 0.75 g of flexible nanonipsomes of MTX for external application （the quality fraction was 0.005） and 1.5 g of MTX for external application （the quality fraction was 0.002 5） respectively by using Franz diffusion cell （MTX were all 3.75 mg.）. 0.45-um micropore film was used for filtering on the 2^nd, 4^th, 8^th, 10^th and 12^th hours. The filtrate was attenuated to 10 mL with normal saline, and the absorbance on 306 nm was determined. Subtracting the absorbance of the physiologic saline, we used the absorbance in standard curve to compute the accumulated transmit dose and the accumulated transmissivity of 12 hours. Differences among 3 kinds of preparations were compared. RESULTS： The accumulated transmit dose and the accumulated transmissivity of 12 hours of the flexible nanonipsomes of MTX for extemal application, 0.002 5 and 0.005 flexible nanonipsomes of MTX for external application were higher than those of MTX for external application, and the differences were significant [The accumulated transmissMty of 12 hours respectively were （67.51±0.37）%, （72.79±0.03）%, （24.50±0.08）%, t = 325.71,247.24,P 〈 0.01]. While there was no remarkable difference in accumulated transmit dose and the accumulated transmissivity of 12 hours between 0.002 5 and 0.005 flexibl

关 键 词：脂质体 甲氨蝶呤 体外 皮肤渗透 

分 类 号：R318[医药卫生—生物医学工程]