Lecithin vesicles for topical delivery of diclofenac
Lecithin vesicles for topical delivery of diclofenac
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DOI：
10.1016/s0939-6411(03)00143-7
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发表时间：
2003-11-01
影响因子：
4.9
通讯作者：
Jasti, BR
中科院分区：
文献类型：
--
作者：
Boinpally, RR;Zhou, SL;Jasti, BR
局部应用双氯芬酸的皮肤渗透性对于风湿性疾病和光化性角化病的治疗非常重要。我们研究了四种卵磷脂泡囊制剂和几种市售的半固体制剂对双氯芬酸体外透皮吸收的影响。将卵磷脂和胆酸钠以1：1的甲醇-氯仿混合溶液溶解，真空蒸发溶剂，用水或10%乙醇使脂层水化，制得卵磷脂泡囊制剂。超声作用5min以减小囊泡的大小，并对其大小和Zeta电位进行了表征。在含有胆酸钠和10%乙醇的卵磷脂微囊中，双氯芬酸的累积量和最大流量分别为69.7+/-40.3和4.77+/-3.16µg/h cm(2)，是所研究的所有处方中最高的。其他制剂的累积量和平均最大通量分别为2.46+/-1.98-29.9+/-10.1杯和0.53+/-0.46-3.61+/-0.86杯/小时厘米(2)。根据这些结果，双氯芬酸卵磷脂微囊似乎更有利于双氯芬酸的局部给药。(C)2003爱思唯尔B.V.保留所有权利。
Skin penetration of topically applied diclofenac is important for the treatment of rheumatic diseases and actinic keratoses. We have studied the permeation of diclofenac across human cadaver epidermis in-vitro from four lecithin vesicle formulations and a few marketed semi-solid preparations. The lecithin vesicle formulations were prepared by dissolving the lipid contents (lecithin and sodium cholate) in a 1:1 mixture of methanol-chloroform, evaporating the solvents under vacuum, and hydrating the lipid layer with the drug solution in water or 10% ethanol. The vesicles were sonicated for 5 min to reduce the vesicle size and their size and Zeta potential were characterized. The cumulative amount and maximum flux of diclofenac was 69.7 +/- 40.3 mug and 4.77 +/- 3.16 mug/h cm(2) from lecithin vesicles containing sodium cholate and 10% ethanol, and is the highest of all formulations studied. The cumulative amount and mean maximum flux obtained from other formulations were in the range of 2.46 +/- 1.98-29.9 +/- 10.1 mug and 0.53 +/- 0.46-3.61 +/- 0.86 mug/h cm(2). Based on the results, lecithin vesicles of diclofenac appear to be advantageous for the topical delivery of diclofenac. (C) 2003 Elsevier B.V. All rights reserved.