Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan, China.
Int J Pharm. 2009 May 8;372(1-2):191-8. doi: 10.1016/j.ijpharm.2009.01.014. Epub 2009 Jan 22.
The objective of this investigation was to develop solid lipid nanoparticles (SLNs) of penciclovir and evaluate the potential of SLNs as the carrier of penciclovir for topical delivery. Penciclovir-loaded SLNs were prepared by a double (W/O/W) emulsion technique. The SLNs presented spherical with the mean diameter of 254.9 nm. The entrapment efficiency, drug loading and zeta potential were 92.40%, 4.62% and -25.0 mV, respectively. DSC study showed that penciclovir encapsulated in SLNs was in the amorphous form. The cumulative amount of penciclovir penetrated through excised rat skin from SLNs was more than 2-fold that of the commercial cream as a control at 12h after administration. There was no significant difference of penciclovir content deposited in epidermis between the cream and SLNs administrated for 2, 6 and 12h, while SLNs increased the cumulative uptake of penciclovir in dermis significantly at the same intervals. Microscopic pictures showed that the interaction between SLNs and the skin surface changed the apparent morphology of stratum corneum and broke the close conjugation of corneocyte layers, which was the possible reason that SLNs increased the permeation of penciclovir into skin dermis. It can be concluded from our study that SLNs provide a good skin targeting effect and may be a promising carrier for topical delivery of penciclovir.
本研究旨在制备喷昔洛韦固体脂质纳米粒（SLNs），并评估 SLNs 作为喷昔洛韦局部递药载体的潜力。采用复乳（W/O/W）乳化技术制备载喷昔洛韦 SLNs。SLNs 呈球形，平均粒径为 254.9nm。包封率、载药量和 Zeta 电位分别为 92.40%、4.62%和-25.0mV。DSC 研究表明，包封于 SLNs 中的喷昔洛韦呈无定形态。给药 12h 后，与市售乳膏（对照）相比，SLNs 中喷昔洛韦透过大鼠离体皮肤的累积渗透量增加了 2 倍以上。在给药 2、6 和 12h 时，乳膏和 SLNs 沉积在表皮中的喷昔洛韦含量无显著差异，但 SLNs 显著增加了皮内的累积吸收量。显微镜照片显示，SLNs 与皮肤表面的相互作用改变了角质层的表观形态，打破了角质细胞层的紧密连接，这可能是 SLNs 增加喷昔洛韦渗透进入皮肤真皮的原因。综上所述，SLNs 提供了良好的皮肤靶向效果，可能是喷昔洛韦局部递药的有前途的载体。
