氯诺昔康固体脂质纳米粒的实验研究  

Experiment on lornoxicam-loaded solid lipid nanoparticles

作　　者：解斐[1] 张栋[2] 刘天华[1] 黄桂华[2] 

机构地区：[1]山东大学威海分校海洋学院,山东威海264209 [2]山东大学药学院药剂所,济南250012

出　　处：《山东大学学报（医学版）》2010年第4期155-159,共5页Journal of Shandong University:Health Sciences

基　　金：山东大学威海分校本科生创新课题

摘　　要：目的制备氯诺昔康固体脂质纳米粒(Lnxc-SLNs)并考察其理化性质。方法采用溶剂扩散法制备Lnxc-SLN,在单因素考察的基础上,采用正交试验设计优化纳米粒的处方与工艺;透射电镜下观察其外观形态,激光散射测定Zeta电位与粒度分布,低温高速离心法分离SLNs与未包封的药物,紫外分光光度法(UV)测定其包封率与载药量,膜动态透析法探讨Lnxc-SLNs的体外释药特性。结果正交试验设计优化的最佳处方与工艺:药脂比为1∶10,单硬脂酸甘油酯与大豆磷脂比为1.5∶1,表面活性剂泊洛沙姆188与吐温80分别为1.2%和0.4%,油水相之比为1∶5;纳米粒外观形态圆整,呈类球形实体粒子,平均粒径为185.3nm,Zeta电位为(-27.65±0.91)mV,包封率为(86.24±3.39)%,载药量为(8.62±0.34)%,在pH6.8PBS中释药符合双相动力学方程。结论SLNs体外释放有明显的缓释作用,是静脉注射给药有前景的靶向载体。Objective To develop solid lipid nanoparticles of lornoxicam（Lnxc-SLNs） and evaluate their physicochemical properties. Methods Based on the single-factor experiment,lornoxicam loaded SLNs were prepared with the solvent diffusion method by orthogonal experiment design. Their morphology was investigated by transmission electron microscopy （TEM）. Zeta potential and particle size were evaluated by laser scatter. Entrapment efficiency and drug loading were determined. The in vitro release behavior was investigated with the film dynamic dialyzed method. Results The optimal formula was obtained by an orthogonal design： the ratio of drug and lipid was 1∶ 10,the ratio of glyceryl monostearate and soybean phospholipid was 1. 5∶ 1,1. 2% poloxamer 188 and 0. 4% between 80 were used as the surface acting agent,the ratio of oil phase and aqueous phase was 1∶ 5. The obtained SLNs were spherical,and mean size and Zeta potential of SLNs were 185. 3 nm and （-27. 65 ± 0. 91） mV. Entrapment efficiency of lornoxicam in SLNs was （86. 24 ± 3. 39） % and （8. 62 ± 0. 34） % for drug loading. The in vitro release behavior conformed to bio-exponential kinetics. Conclusion SLNs provide a good sustained-release effect in vitro and may be a promising carrier for intravenous delivery of non-steroid anti-inflammatory drugs（NSAIDs）.

关 键 词：氯诺昔康 非甾体类抗炎药 固体脂质纳米粒 溶剂扩散法 

分 类 号：R927.2[医药卫生—药学]