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Cremophor RH40-PEG 400 微乳作为酮洛芬的透皮药物传递载体。

Cremophor RH40-PEG 400 microemulsions as transdermal drug delivery carrier for ketoprofen.

机构信息

Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand. tanasait@ su.ac.th

出版信息

Pharm Dev Technol. 2013 Jul-Aug;18(4):798-803. doi: 10.3109/10837450.2011.627871. Epub 2011 Oct 24.

Abstract

The aim of this study was to prepare novel microemulsion for transdermal drug delivery of ketoprofen (KP). The microemulsion composed of ketoprofen as model drug, isopropyl myristate (IPM) as oil phase, surfactant mixture consisting of polyoxyl 40 hydrogenated castor oil (Cremophor RH40) as surfactant and polyethylene glycol 400 (PEG400) as co-surfactant at the ratio 1:1, and water were prepared. The viscosity, droplet size, pH, conductivity of microemulsions, and skin permeation of KP through shed snake skin were evaluated. The particle size, pH, viscosity and conductivity of microemulsions were in the range of 114-210 nm, 6.3-6.8, 124-799 cPs and 1-45 µS/cm, respectively. The ratio of IPM, and surfactant mixture played the important role in the skin permeation of KP microemulsions. As the amount of surfactant mixture and IPM increased, the skin permeation of KP decreased. The formulation composed of 30% IPM, 45% surfactant mixture and 25% water showed the highest skin permeation flux. The incorporation of terpenes in the 2.5% KP microemulsions resulted in significant enhancement in skin permeation of KP. The rank order of enhancement ratio for skin permeation enhancement of terpenes was α-pinene > limonene > menthone. The results suggested that the novel microemulsion system containing IPM, water, Cremophor RH40:PEG400 and terpenes can be applied for using as a transdermal drug delivery carrier.

摘要

本研究旨在制备新型酮洛芬(KP)透皮给药微乳。该微乳由酮洛芬作为模型药物、肉豆蔻酸异丙酯(IPM)作为油相、由聚氧乙烯 40 氢化蓖麻油(Cremophor RH40)和聚乙二醇 400(PEG400)组成的表面活性剂混合物(比例为 1:1)和水组成。评价了微乳的粘度、粒径、pH 值、电导率以及 KP 通过脱皮蛇皮的透皮情况。微乳的粒径、pH 值、粘度和电导率分别在 114-210nm、6.3-6.8、124-799cPs 和 1-45µS/cm 范围内。IPM 和表面活性剂混合物的比例对 KP 微乳的透皮情况起着重要作用。随着表面活性剂混合物和 IPM 的用量增加,KP 的透皮量减少。由 30%IPM、45%表面活性剂混合物和 25%水组成的配方表现出最高的透皮通量。将萜烯加入到 2.5%KP 微乳中,可显著提高 KP 的透皮渗透。萜烯对 KP 透皮渗透增强的顺序为α-蒎烯>柠檬烯>薄荷酮。结果表明,含有 IPM、水、Cremophor RH40:PEG400 和萜烯的新型微乳系统可作为透皮给药载体应用。

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