喷昔洛韦固体脂质纳米粒的制备及其经皮渗透作用

山东大学学报(医学版)

喷昔洛韦固体脂质纳米粒的制备及
其经皮渗透作用

吕青志¹，于爱华¹，席延卫¹，宋智梅^1,2，曹丰亮¹，翟光喜¹

（1. 山东大学药学院药物制剂研究所，济南 250012； 2. 济南大学化学院，济南 250022）

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2009-03-16 发布日期:2009-03-16
通讯作者: 翟光喜

Penciclovirloaded solid lipid nanoparticles for topical delivery

Received:1900-01-01 Revised:1900-01-01 Online:2009-03-16 Published:2009-03-16

摘要/Abstract

摘要： 目的制备喷昔洛韦固体脂质纳米粒(SLN)并考察其经皮渗透作用。方法采用W/O/W复乳法制备喷昔洛韦SLN，考察SLN的形态、粒径、Zeta电位、包封率等特性，采用差示量热分析考察其热力学特性，以市售乳膏作对照，考察其经皮渗透作用，并对其透皮机理进行初步研究。结果透射电镜下喷昔洛韦SLN成球状或类球状，平均粒径为(254.9±8.2)nm，Zeta电位为(-25±0.05)mV，平均包封率为(92.40±1.4)%，载药量为(4.62±0.2)%。差示量热分析结果表明，喷昔洛韦以无定形状态包封于SLN中。体外渗透12?h，夫坦乳膏和喷昔洛韦SLN的单位面积累积渗透量分别为(41.07±3.07)μg/cm2和(88.44±4.19)μg/cm2。病理切片结果表明，SLN可使致密的角质层溶胀、疏松。结论SLN能够促进喷昔洛韦的经皮渗透，是一有前景的经皮给药载体。

关键词: 载脂蛋白A-Ⅰ, 大鼠，Wistar, 主动脉, 葡萄子原花青素, 喷昔洛韦, 固体脂质纳米粒, 差示量热分析, 经皮给药, 荧光差异凝胶电泳

Abstract: ObjectiveTo develop solid lipid nanoparticles (SLNs) of penciclovir and evaluate potential of SLNs as a topical carrier for enhanced skin permeation of penciclovir. MethodsPenciclovir loaded SLNs were prepared with the W/O/W double emulsion technique. Its morphology was investigated by TEM. Zeta potential and particle size were evaluated. Entrapment efficiency and drug loading were determined, and thermal behavior was investigated by DSC. The in vitro skin permeation behavior was investigated with a marketed cream as a control. ResultsThe obtained SLNs were spherical, and mean size and Zeta potential of SLNs were (254.9±8.2) nm and (-25±0.05) mV. Entrapment efficiency of penciclovir in SLNs was (92.40±1.4)% and (4.62±0.2)% for drug loading. DSC study showed that penciclovir encapsulated in SLNs was in an amorphous form. Cumulative amounts of penciclovir from cream and SLNs at 12 h after dosing were (41.07±3.07)μg/cm2 and (88.44±4.19)μg/cm2. Microscopic pictures showed that interaction between SLNs and skin surface made morphology of the stratum corneum apparently changed and broke close conjugation of the corneocyte layers, which was possible reason of SLNs resulted in an increased permeation of penciclovir. ConclusionSLNs providea good skin permeation effect and may be a promising carrier for topical delivery of penciclovir.

Key words: Penciclovir, Solid lipid nanoparticle, Differential scanning calorimetry, Topical delivery, Grape seed proanthocyanidin extracts； ApolipoproteinA-Ⅰ； Rats, Wistar； aorta； Difference gel electrophoresis

中图分类号:

R944

吕青志1 ，于爱华1 ，席延卫1 ，宋智梅1,2 ，曹丰亮1 ，翟光喜1
. 喷昔洛韦固体脂质纳米粒的制备及
其经皮渗透作用[J]. 山东大学学报(医学版), 2009, 47(03): 101-105.

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