醋酸曲安奈德固体脂质纳米粒卡波姆凝胶的性能及经皮给药研究

醋酸曲安奈德固体脂质纳米粒卡波姆凝胶的性能及经皮给药研究

刘卫, 朱姚亮, 陈华兵, 杨祥良^*

1.华中科技大学生命科学与技术学院药物研究所;
2.华中科技大学化学系, 湖北武汉 430074

收稿日期:2004-09-20 修回日期:2005-02-10 出版日期:2005-03-15 发布日期:2005-03-15
通讯作者: 杨祥良*

Characteristics and Transdermal Drug Delivery of Triamcinolone-Acetonide-Acetate-Loaded Solid Lipid Nanoparticles Carbomer Gel

LIU Wei, ZHU Yao-liang, CHEN Hua-bing, YANG Xiang-liang^*

1. Institute of Materia Medica, College of Life Science and Technoloy;
2. Depar tment of Chemistry, Huazhong University of Science and Technology, Wuhan 430074, China

Received:2004-09-20 Revised:2005-02-10 Online:2005-03-15 Published:2005-03-15
Contact: YANG Xiang-liang*

摘要/Abstract

摘要： 目的以醋酸曲安奈德(TAA)为模型药物, 以三棕榈酸甘油酯为脂质材料制备醋酸曲安奈德固体脂质纳米粒(SLN)卡波姆凝胶, 考察其特性以及药物经皮渗透性能。方法采用高压乳匀技术制得TAA-SLN分散液, 并制成卡波姆凝胶, 考察了卡波姆凝胶中SLN的微观形态、粒径、Zeta电位、包封率等理化特性和稳定性、体外药物释放行为。采用改进的Franz扩散池研究了SLN卡波姆凝胶的药物经皮渗透性能。结果制得的TAA-SLN为均匀的球形粒子, 不同载药量SLN粒径为95.5~186.2 nm, Zeta电位为-26.3~-15.7 mV, 包封率为67.43%~90.3%; SLN卡波姆凝胶37 ºC储存三个月后SLN粒径略有增大, Zeta电位无明显变化; SLN卡波姆凝胶体外药物释放符合Higuchi方程(DR% = 6.3979t1/2 + 3.1529, r² = 0.951 8); 经皮渗透实验结果表明, 与相同药物浓度的普通卡波姆凝胶比较, SLN卡波姆凝胶药物经皮渗透速率和药物24 h累积渗透量显著提高。结论 TAA-SLN卡波姆凝胶稳定性好, 对药物释放具有缓控释作用, 能显著促进药物经皮渗透, 有望成为新型经皮给药制剂。

关键词: 固体脂质纳米粒, 固体脂质纳米粒, 固体脂质纳米粒, 卡波姆凝胶, 卡波姆凝胶, 卡波姆凝胶, 醋酸曲安奈德, 醋酸曲安奈德, 醋酸曲安奈德, 经皮给药, 经皮给药, 经皮给药

Abstract: Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipid nanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate their characteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressure homogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology, particle size with polydispersity index (PI) and zeta potential were examined by atomic force microscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability and in vitro drug release were also studied. The transdermal drug delivery through porcine ear skin was evaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with the average size of (95.5-186.2) nm, the zeta potential of (-26.3~-15.7) mV and the entrapment efficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had good stability, the release profile in vitro fitted Higuchi equation. In comparison with conventional hydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition within porcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is prepared with stable physicochemical properties. The release profile and improved drug permeation into skin make it be a promising vehicle for transdermal drug delivery.

Key words: solid lipid nanoparticles, solid lipid nanoparticles, carbomer gel, carbomer gel, triamconol one-acetonide-acetate, triamconol one-acetonide-acetate, characterization, characterization, transdermal drug delivery, transdermal drug delivery

中图分类号:

R943.4

Supporting: ^*Corresponding author. Tel.: 86-27-87794711, 86-27-87794517

刘卫, 朱姚亮, 陈华兵, 杨祥良^*. 醋酸曲安奈德固体脂质纳米粒卡波姆凝胶的性能及经皮给药研究[J]. .

LIU Wei, ZHU Yao-liang, CHEN Hua-bing, YANG Xiang-liang^*. Characteristics and Transdermal Drug Delivery of Triamcinolone-Acetonide-Acetate-Loaded Solid Lipid Nanoparticles Carbomer Gel[J]. .

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