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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
引用本文: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]. 中国药学, 2005, 14(1): 18-24
作者姓名:刘卫  朱姚亮  陈华兵  杨祥良
作者单位:华中科技大学生命科学与技术学院药物研究所,华中科技大学化学系,华中科技大学生命科学与技术学院药物研究所,华中科技大学生命科学与技术学院药物研究所 湖北武汉430074
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 . 2nm ,Zeta电位为 - 2 6 .3~ - 15 . 7mV ,包封率为 6 7. 4 3%~ 90 . 3% ;SLN卡波姆凝胶 37℃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. 15 2 9,r2 =0 . 95 18) ;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 2 4h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  卡波姆凝胶  醋酸曲安奈德  经皮给药

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. Characteristics and Transdermal Drug Delivery of Triamcinolone-Acetonide-Acetate-Loaded Solid Lipid Nanoparticles Carbomer Gel[J]. Journal of Chinese Pharmaceutical Sciences, 2005, 14(1): 18-24
Authors:LIU Wei  ZHU Yao-liang  CHEN Hua-bing  YANG Xiang-liang
Abstract:Aim To prepare triamcinolone-acetonide-acetate (T AA)-loaded solid lipid nanoparticles (SLN) carbomer gel with tripalmitin glycer ide (TPG), and investigate their characteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressure homogeni zation technique, and then mixed with carbomer gel matrix to get SLN gel. The mo rphology, particle size with polydispersity index (PI) and zeta potential were e xamined by atomic force microscopy (AFM) and photon correlation spectroscopy (PC S). The entrapment efficiency, stability and in vitro drug release were also studied. The transdermal drug delivery through porcine ear skin was evaluated u sing modified Franz diffusion cells. Results The SLN had a sph erical 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 di fferent TAA encapsulated compounds. TAA-SLN carbomer gel had good stability, the releas e profile in vitro fitted Higuchi equation. In comparison with conventional hydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and d rug deposition within porcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is prepared with stable physicochem ical properties. The release profile and improved drug permeation into skin make it be a promising vehicle for transdermal drug delivery.
Keywords:solid lipid nanoparticles  carbomer gel  triamconol one-acetonide-acetate  characterization  transdermal drug delivery
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