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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 prepare lornoxicam solid lipid nanoparticles (Lnxc-SLNs) and study its physicochemical properties. Methods Lnxc-SLN was prepared by solvent diffusion method. Orthogonal experiments were designed to optimize the formulation and process of nanoparticles. Transmission electron microscopy was used to observe the morphology of Lnxc-SLN. Zeta potential and particle size distribution were determined by laser scanning electron microscopy. SLNs and unencapsulated drugs were separated by centrifugation. The entrapment efficiency and drug loading were measured by ultraviolet spectrophotometry. The in vitro release characteristics of Lnxc-SLNs were investigated by membrane dynamic dialysis. Results Orthogonal experiment design and optimization of the best prescription and process: the ratio of lipid to lipid 1:10, glycerol monostearate and soybean phospholipid ratio of 1.5: 1, surfactant poloxamer 188 and Tween 80 were 1.2% and 0.4% respectively, and the ratio of oil to water was 1: 5. The morphology of the nanoparticles was round and spherical. The average particle size was 185.3 nm and the Zeta potential was (-27.65 ± 0.91) mV. (86.24 ± 3.39)%, and the drug loading was (8.62 ± 0.34)%. The drug release was consistent with biphasic kinetic equation at pH6.8PBS. Conclusion The release of SLNs in vitro has a significant sustained release effect and is a promising target vector for intravenous administration.