醋酸曲安奈德纳米结构脂质载体的制备及其透皮吸收研究  

Preparation and transdermal absorption of triamcinolone-acetonide-acetate loaded nanostructured lipid carriers

作　　者：朱姚亮[1] 刘卫[1] 陈华兵[1] 徐辉碧[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,武汉430074

出　　处：《中国药科大学学报》2007年第1期30-34,共5页Journal of China Pharmaceutical University

基　　金：湖北省科技攻关资助项目(No.2004AA301B02)~~

摘　　要：目的:制备醋酸曲安奈德(TAA)纳米结构脂质载体(nanostructured lipid carriers,NLC),考察醋酸曲安奈德纳米结构脂质载体(TAA-NLC)对离体猪耳皮肤的透皮吸收行为。方法:采用高压乳匀法制备了TAA-NLC,并对其微观形态、药物和脂质材料的物理状态、粒径及粒径分布、Zeta电位、包封率等进行研究,用改进的Franz扩散池研究TAA-NLC的透皮吸收行为,高效液相色谱法测定TAA含量。结果:TAA-NLC的微观形貌呈类球形粒子,NLC中液态脂质的加入使固体脂质的结晶度降低,药物在NLC中可能以无定形或分子状态存在。NLC粒径分布均匀,平均粒径为(106.47±4.65)nm,多分散指数(PI)为0.176±0.035,Zeta电位为-(45.18±2.73)mV,包封率为(93.06±3.52)%,药物体外释放符合Higuchi方程(Q%=11.762t1/2+0.9383,r=0.9804),24h药物累计透皮量明显低于对照制剂(市售TAA溶液剂),皮肤滞留量达对照制剂的6.82倍。结论:所制备的TAA-NLC可以降低TAA皮肤透过量,显著增加药物在皮肤中的滞留量,有望成为TAA的新型局部给药制剂。Aim： To prepare triamcinolone-acetonide-acetate （TAA） loaded nanostructured lipid carriers （NLC） and investigate their transdermal absorption behavior. Methods：The high-pressure homogenization technique was used to prepare TAA-loaded NLC（TAA-NLC）. The morphology,physical structure,particle size with polydispersity index（PI） and Zeta potential were examined by atomic force mieroseopy（AFM）, differential scanning calorimetry（DSC）and photon correlation spectroscopy（PCS）, respectively. The entrapment efficiency, stability and in vitro drug release were also studied. The transdermal drug permeation through porcine ear skin was evaluated using modified Franz diffusion cells. Results： The obtained TAA-NLC assumed spherical shape with the average size of （ 106.47 ± 4.65） nm, PI of 0. 176 ± 0.035,Zeta potential of - （45.18± 2.73）mV and the entrapment efficiency of （93.06 ± 3.52）%. Drug release profile in vitro was in accordance with Higuehi equation and TAA-NLC had good stability. In comparison with TAA ethanol solution, TAA-NLC resulted in higher drug deposition within porcine ear skin after 24 h penetration experiment. Conclusion：These results indicated that the studied TAA-NLC system with improved drug permeation into skin might be a novel vehicle for the topical use of TAA.

关 键 词：纳米结构脂质载体 醋酸曲安奈德 高压乳匀法 透皮吸收 

分 类 号：R944[医药卫生—药剂学]