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

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(英文)

作　　者：刘卫[1] 朱姚亮[2] 陈华兵[1] 杨祥良[1] 

机构地区：[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

出　　处：《Journal of Chinese Pharmaceutical Sciences》2005年第1期18-24,共7页中国药学（英文版）

摘　　要：Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipidnanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate theircharacteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressurehomogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology,particle size with polydispersi-ty index (PI) and zeta potential were examined by atomic forcemicroscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability andin vitro drug release were also studied. The transdermal drug delivery through porcine ear skin wasevaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with theaverage size of (95.5 - 186.2) nm, the zeta potential of (-26.3- -15.7) mV and the entrapmentefficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had goodstability, the release profile in vitro fitted Higuchi equation. In comparison with conventionalhydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition withinporcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is preparedwith stable physicochemical properties. The release profile and improved drug permeation into skinmake it be a promising vehicle for transdermal drug delivery.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：solid lipid nanoparticles carbomer gel triarnconolone-acetonide-acetate characterization transdermal drug delivery 

分 类 号：R943.4[医药卫生—药剂学]