Singh Sanjay, Muthu Madaswamy S
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221005, India.
Nanomedicine (Lond). 2007 Apr;2(2):233-40. doi: 10.2217/17435889.2.2.233.
The aim of this work was to prepare poly(epsilon-caprolactone) nanoparticles of risperidone and to characterize them.
Risperidone-loaded poly(epsilon-caprolactone) nanoparticles were prepared by the nanoprecipitation method using poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock polymeric stabilizer (PluronicF-68). The particles were characterized for particle size by photon correlation spectroscopy and transmission electron microscopy. The free dissolved drug in the nanosuspension was determined by the bulk equilibrium reverse dialysis bag technique. In vitro release studies were carried out using the dialysis bag diffusion technique.
The particle size of the prepared nanoparticles ranged from 90 to 300 nm. Nanoparticles of risperidone were obtained with high encapsulation efficiency (70-80%). The drug release from the risperidone nanoparticles was sustained in some batches for more than 24 h with 80% drug release, whereas release from risperidone in polyethylene glycol 400 solution showed release within 2 h.
These studies suggest the feasibility of formulating risperidone-loaded poly(epsilon-caprolactone) nanoparticles for the treatment of psychotic disorders.
本研究旨在制备利培酮聚(ε-己内酯)纳米粒并对其进行表征。
采用纳米沉淀法,以聚(环氧乙烷)-聚(环氧丙烷)-聚(环氧乙烷)三嵌段聚合物稳定剂(普朗尼克F-68)制备载有利培酮的聚(ε-己内酯)纳米粒。通过光子相关光谱和透射电子显微镜对颗粒的粒径进行表征。采用大容量平衡反向透析袋技术测定纳米混悬液中游离溶解的药物。采用透析袋扩散技术进行体外释放研究。
制备的纳米粒粒径范围为90至300nm。获得了具有高包封率(70-80%)的利培酮纳米粒。部分批次的利培酮纳米粒药物释放持续超过24小时,药物释放率达80%,而利培酮在聚乙二醇400溶液中的释放则在2小时内完成。
这些研究表明,制备载有利培酮的聚(ε-己内酯)纳米粒用于治疗精神障碍具有可行性。