Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.
Int Immunopharmacol. 2010 Oct;10(10):1305-9. doi: 10.1016/j.intimp.2010.07.015. Epub 2010 Aug 18.
The purpose of the present study was to investigate the skin irritation and pharmacodynamics of penciclovir-loaded microemulsion (PCV-ME). The formulation of PCV-ME was comprised of oleic acid (OA) (5%, w/w), Cremorphor EL (20%, w/w), ethanol (30%, w/w) and water (45%, w/w). PCV-ME presented as spherically shaped under transmission electron microscopy with an average diameter of 36.5 nm, and the solubility of PCV in microemulsion (ME) was 7.41 mg/g, almost 6 times that in water. Skin irritation test was performed in male guinea pigs, which demonstrated that no irritation effect was caused after single or multiple applications of PCV-ME. Likewise, male guinea pigs were employed as animal models which were infected with herpes simplex virus type 1 (HSV-1) in pharmacodynamics study. Real-time PCR was utilized to investigate the inhibition effect on HSV-1 exerted by commercial PCV-cream and PCV-ME. The results indicated that compared with commercial PCV-cream, PCV-ME could significantly inhibit the replication of HSV-1 in skin. In conclusion, PCV-ME could be a promising formulation which possessed the virtues of low irritation and high effectiveness.
本研究旨在考察喷昔洛韦负载微乳（PCV-ME）的皮肤刺激性和药效学。PCV-ME 的配方由油酸（OA）（5%，w/w）、Cremophor EL（20%，w/w）、乙醇（30%，w/w）和水（45%，w/w）组成。透射电子显微镜下，PCV-ME 呈球形，平均直径为 36.5nm，PCV 在微乳中的溶解度为 7.41mg/g，几乎是水的 6 倍。在雄性豚鼠中进行了皮肤刺激性试验，结果表明单次或多次应用 PCV-ME 后不会引起刺激性。同样，雄性豚鼠被用作药效学研究中感染单纯疱疹病毒 1 型（HSV-1）的动物模型。实时 PCR 用于研究商用 PCV 乳膏和 PCV-ME 对 HSV-1 的抑制作用。结果表明，与商用 PCV 乳膏相比，PCV-ME 能显著抑制 HSV-1 在皮肤中的复制。综上所述，PCV-ME 是一种有前途的制剂，具有低刺激性和高效性的优点。
