a School of Pharmaceutical Science , Xiamen University , Xiamen , China .
b Department of Pharmacy , Xiamen University Hospital , Xiamen , China .
Drug Deliv. 2015;22(6):757-64. doi: 10.3109/10717544.2014.898713. Epub 2014 Apr 11.
The purpose of the present investigation was to develop and optimize the microemulsion (ME) as a transdermal system for Pd-Ia, a poor water soluble and low bioavailable drug. The pseudo-ternary phase diagrams were constructed for various ME formulations including oleic acid as the oil phase, Cremophor RH40 as the surfactant, ethanol as the cosurfactant, and water. The maximum cumulative amount permeated through rat abdominal skins per unit area in 32 h (Q32), and the maximum flux were evaluated using the Franz diffusion cell in order to optimize the ME formulation. The results indicated that the optimized ME formulation was composed of oleic acid (5%, W/W), Cremophor RH40 (13.33%, W/W), ethanol (26.67%, W/W), and water (55%, W/W); the maximum cumulative amount of Pd-Ia was 354.330 ± 12.006 μg cm(-2), the maximum flux was 11.467 ± 0.500 μg cm(-2)h(-1). ME-gel was administered transdermally to rats. The mean plasma concentration of Pd-Ia following transdermal application of ME-gel could be maintained for 32 h at least and the half-life was evidently prolonged. It shows that the ME-gel could be a promising vehicle for dermal delivery of Pd-Ia.
本研究旨在开发和优化微乳（ME）作为一种透皮系统，用于 Pd-Ia，一种水溶性差且生物利用度低的药物。构建了各种 ME 制剂的伪三元相图，包括油酸作为油相、Cremophor RH40 作为表面活性剂、乙醇作为助表面活性剂和水。通过Franz 扩散池评估 32 小时内单位面积透皮累积量（Q32）和最大通量，以优化 ME 制剂。结果表明，优化的 ME 制剂由油酸（5%，W/W）、Cremophor RH40（13.33%，W/W）、乙醇（26.67%，W/W）和水（55%，W/W）组成；Pd-Ia 的最大累积量为 354.330±12.006μg·cm-2，最大通量为 11.467±0.500μg·cm-2·h-1。ME-凝胶经皮给药。ME-凝胶经皮给药后 Pd-Ia 的平均血浆浓度至少可维持 32 小时，半衰期明显延长。这表明 ME-凝胶可能是 Pd-Ia 经皮给药的一种有前途的载体。
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