Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, Haryana 125 001, India.
J Microencapsul. 2011;28(1):37-45. doi: 10.3109/02652048.2010.523794.
In this study, diclofenac-loaded Eudragit S100-based nanosuspension was prepared by nanoprecipitation method and characterised for particle size, morphology, in vitro release, and for its in vivo ocular anti-inflammatory activity. The diclofenac-loaded Eudragit S100 nanosuspension was found to have a particle size of 172 nm, polydispersibility index of 0.14 and zeta potential of -23.7 +/- 6.07 mV, indicating that the nanosuspension is fairly stable. The nanosuspended particles were found to be spherical in shape. The nanosuspension was found to provide a sustained in vitro release, following the Higuchi square-root release kinetics. The results indicated that the nanosuspension released the drug by combination of dissolution and diffusion. The in vivo evaluation of nanosuspension in PGE(2)-induced ocular inflammation in rabbit model revealed a significantly (p < 0.05) higher inhibition of PGE(2)-induced polymorphonuclear leukocytes migration and lid-closure scores as compared with the aqueous solution of diclofenac.
在这项研究中，通过纳米沉淀法制备了负载双氯芬酸的 Eudragit S100 纳米混悬剂，并对其粒径、形态、体外释放以及体内抗炎活性进行了表征。研究发现，载双氯芬酸的 Eudragit S100 纳米混悬剂的粒径为 172nm，多分散指数为 0.14，zeta 电位为-23.7±6.07mV，表明纳米混悬剂相当稳定。纳米悬浮颗粒呈球形。纳米混悬剂表现出持续的体外释放，符合 Higuchi 平方根释放动力学。结果表明，纳米混悬剂通过溶解和扩散的结合释放药物。在兔 PGE（2）诱导的眼内炎症模型中对纳米混悬剂的体内评价表明，与双氯芬酸钠水溶液相比，纳米混悬剂显著（p<0.05）抑制了 PGE（2）诱导的多形核白细胞迁移和眼睑闭合评分。
