Virani Amitkumar, Puri Vinam, Mohd Hana, Michniak-Kohn Bozena
Ernest Mario School of Pharmacy, Rutgers-The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA.
Center for Dermal Research, Rutgers-The State University of New Jersey, 145 Bevier Road, Piscataway, NJ 08854, USA.
Pharmaceutics. 2023 Jan 4;15(1):183. doi: 10.3390/pharmaceutics15010183.
Oxcarbazepine (OXC) is an anticonvulsant drug, indicated for the treatment of the neurological disorder, epilepsy. The objective of the present study was to evaluate the transdermal delivery of OXC from microemulsions using different penetration enhancers. Transcutol® P (TRC), oleic acid (OA), cineole (cin), Labrasol (LS), Tween 80 (T80) and N-Methyl-Pyrrolidone (NMP) were used as penetration enhancers as well as microemulsion components. Simple formulations of OXC in propylene glycol (PG) incorporating various penetration enhancers and combination of penetration enhancers were also evaluated for transdermal delivery. Drug delivery and penetration enhancement were studied using human cadaver skin on Franz diffusion cells. The results showed that all penetration enhancers improved the rate of permeation of OXC compared to the control. The flux of drug delivery from the various formulations was found to be, in decreasing order, cin > OA + TRC > NMP > TRC > OA. Overall, microemulsions prepared using cineole, Tween 80 and Transcutol® P (TRC) were shown to be provide the best penetration enhancement for OXC.
奥卡西平（OXC）是一种抗惊厥药物，用于治疗神经系统疾病癫痫。本研究的目的是评估使用不同渗透促进剂时奥卡西平从微乳剂中的透皮给药情况。二乙二醇单乙基醚（Transcutol® P，TRC）、油酸（OA）、桉叶油素（cin）、Labrasol（LS）、吐温80（T80）和N-甲基吡咯烷酮（NMP）既用作渗透促进剂，也用作微乳剂成分。还评估了奥卡西平在丙二醇（PG）中加入各种渗透促进剂以及渗透促进剂组合的简单制剂的透皮给药情况。使用人尸体皮肤在Franz扩散池上研究药物递送和渗透增强情况。结果表明，与对照相比，所有渗透促进剂均提高了奥卡西平的渗透速率。发现各种制剂的药物递送通量按降序排列为：桉叶油素＞油酸+二乙二醇单乙基醚＞N-甲基吡咯烷酮＞二乙二醇单乙基醚＞油酸。总体而言，使用桉叶油素、吐温80和二乙二醇单乙基醚（TRC）制备的微乳剂对奥卡西平显示出最佳的渗透增强效果。
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