Nguyen Julia, Ita Kevin B, Morra Matthew J, Popova Inna E
College of Pharmacy, Touro University California, Mare Island-Vallejo, CA 94592, USA.
Department of Plant, Soil and Entomological Sciences, University of Idaho, Moscow, ID 83844, USA.
Pharmaceutics. 2016 Nov 15;8(4):33. doi: 10.3390/pharmaceutics8040033.
The aim of this project was to examine the effect of microneedle rollers on the percutaneous penetration of tiagabine hydrochloride and carbamazepine across porcine skin in vitro. Liquid chromatography-mass spectrometric analysis was carried out using an Agilent 1200 Series HPLC system coupled to an Agilent G1969A TOF-MS system. Transdermal flux values of the drugs were determined from the steady-state portion of the cumulative amount versus time curves. Following twelve hours of microneedle roller application, there was a 6.74-fold increase in the percutaneous penetration of tiagabine hydrochloride (86.42 ± 25.66 µg/cm²/h) compared to passive delivery (12.83 ± 6.30 µg/cm²/h). For carbamazepine in 20% ethanol, passive transdermal flux of 7.85 ± 0.60 µg/cm²/h was observed compared to 10.85 ± 0.11 µg/cm²/h after microneedle treatment. Carbamazepine reconstituted in 30% ethanol resulted in only a 1.19-fold increase in drug permeation across porcine skin (36.73 ± 1.83 µg/cm²/h versus 30.74 ± 1.32 µg/cm²/h). Differences in flux values of untreated and microneedle-treated porcine skin using solid microneedles for the transdermal delivery of tiagabine were statistically significant. Although there were 1.38- and 1.19-fold increases in transdermal flux values of carbamazepine when applied as 20% and 30% ethanol solutions across microneedle-treated porcine skin, respectively, the increases were not statistically significant.
本项目旨在研究微针滚轮对盐酸替加宾和卡马西平经猪皮体外渗透的影响。采用安捷伦1200系列高效液相色谱系统与安捷伦G1969A飞行时间质谱系统联用进行液相色谱 - 质谱分析。根据累积量与时间曲线的稳态部分确定药物的透皮通量值。在应用微针滚轮12小时后，盐酸替加宾的经皮渗透量（86.42±25.66μg/cm²/h）相较于被动给药（12.83±6.30μg/cm²/h）增加了6.74倍。对于卡马西平在20%乙醇中的情况，观察到被动透皮通量为7.85±0.60μg/cm²/h，而微针处理后为10.85±0.11μg/cm²/h。以30%乙醇复溶的卡马西平经猪皮的药物渗透仅增加了1.19倍（36.73±1.83μg/cm²/h对30.74±1.32μg/cm²/h）。使用固体微针进行替加宾透皮给药时，未处理和微针处理的猪皮通量值差异具有统计学意义。尽管卡马西平分别以20%和30%乙醇溶液应用于微针处理的猪皮时，透皮通量值分别增加了1.38倍和1.19倍，但增加量无统计学意义。
