PREPARATION AND CHARACTERIZATION OF ORAL NANOSUSPENSION LOADED WITH CURCUMIN
PREPARATION AND CHARACTERIZATION OF ORAL NANOSUSPENSION LOADED WITH CURCUMIN
复制标题
姜黄素口服纳米混悬剂的制备及表征
DOI：
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发表时间：
2018
期刊：
影响因子：
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通讯作者：
R. Hirlekar
中科院分区：
文献类型：
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作者：
Sneha Dekate Shreeram Hirlekar;S. Bhairy;R. Hirlekar
目的：通过减小姜黄素的粒径来提高其生物利用度。以泊洛沙姆-188（P188）为表面活性剂制备了CUR纳米混悬剂。方法：对制备NS所需的溶剂、反溶剂和表面活性剂进行筛选，并对制备的NS进行粒径、多分散性指数（PDI）、Zeta电位、载药量、饱和溶解度和释药动力学等表征。采用沉淀-高速均质法（HSH），以选定的组分制备NS。对NS的粒径、PDI、载药量、饱和溶解度和体外药物释放进行了评价。结果：优化处方的粒径为596.5±5 nm，PDI为0.233±0.010，Zeta电位为-23 ±2 mV。所有制剂的pH在5-6的范围内，这在与药物稳定性相关时是可接受的。与普通CUR混悬液（S）相比，优化制剂在水和磷酸盐缓冲液（pH 6.8）中的饱和溶解度增加。药代动力学研究结果表明，CUR S与CUR NS相比，Cmax和AUC 0 -6分别增加了8倍和10倍。结论：以P188为稳定剂制备CUR NS是可行的。在各种稳定剂中，筛选出的P188呈现稳定的NS，其粒径在纳米范围内。药代动力学研究显示，CUR NS的性能优于普通CUR S。
Objective: The principle objective of the present research work was to improve the bioavailability of curcumin (CUR) by decreasing its particle size. Nanosuspension (NS) of CUR was prepared using poloxamer-188 (P188) as a surfactant. The prepared NSs were characterized for particle size, polydispersity index (PDI), zeta potential, drug loading, saturation solubility, and drug release kinetic studies.Methods: Components required for NS preparation, such as solvent, anti-solvent and surfactant were screened. Precipitation high-speed homogenization (HSH) method was used for the preparation of NS using selected components. Evaluation of NS for particle size, PDI, drug loading, saturation solubility and in vitro drug release was done. Pharmacokinetic studies of the NS in sprague dawley (SD) rats were performed.Results: The particle size, PDI and zeta potential of the optimized formulation was 596.5±5 nm, 0.233±0.010 and-23±2 mV respectively. The pH of all the formulations was in the range of 5-6 which is acceptable when related to drug stability. The optimized formulation showed an increase in saturation solubility in water and phosphate buffer pH 6.8 when compared to plain CUR suspension (S). Results of pharmacokinetic studies indicated that Cmax and AUC0-6 were increased 8 and 10 times respectively from plain CUR S to CUR NS.Conclusion: CUR NS was prepared using P188 as the stabilizer. Amongst various stabilizers screened P188 rendered a stable NS with the particle size in nano range. Pharmacokinetic studies revealed the better performance of CUR NS as compared to plain CUR S.