载姜黄素纳米混悬剂的制备、表征、药代动力学和组织分布研究，以 TPGS 为稳定剂。
Preparation, characterization, pharmacokinetics, and tissue distribution of curcumin nanosuspension with TPGS as stabilizer.
机构信息
Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, China.
出版信息
Drug Dev Ind Pharm. 2010 Oct;36(10):1225-34. doi: 10.3109/03639041003695139.
BACKGROUND
CUR is a promising drug candidate based on its good bioactivity, but use of CUR is potentially restricted because of its poor solubility and bioavailability.
AIM
The aim of this study was to prepare an aqueous formulation of curcumin nanosuspension (CUR-NS) to improve its solubility and change its in vivo behavior.
METHODS
CUR-NS was prepared by high-pressure homogenization method. Drug state in CUR-NS was evaluated by powder X-ray diffraction. Pharmacokinetics and biodistribution of CUR-NS after intravenous administration in rabbits and mice were studied.
RESULTS
The solubility and dissolution of CUR in the form of CUR-NS were significantly higher than those of crude CUR. X-ray crystallography diffraction indicated that the crystalline state of CUR in nanosuspension was preserved. Pharmacokinetics and biodistribution results of CUR-NS after intravenous administration in rabbits and mice showed that CUR-NS presented a markedly different pharmacokinetic property as compared to the CUR solution. AUC(0-infinity) of CUR-NS (700.43 +/- 281.53 microg/mL, min) in plasma was approximately 3.8-fold greater than CUR solution (145.42 +/- 9.29 microg/mL min), and the mean residence time (194.57 +/- 32.18 versus 15.88 +/- 3.56 minutes) was 11.2-fold longer.
CONCLUSION
Nanosuspension could serve as a promising intravenous drug-delivery system for curcumin.
背景
姜黄素（CUR）是一种很有前途的候选药物，因为它具有良好的生物活性，但是由于其溶解度和生物利用度差，其应用可能受到限制。
目的
本研究旨在制备姜黄素纳米混悬剂（CUR-NS）的水制剂，以提高其溶解度并改变其体内行为。
方法
采用高压匀质法制备 CUR-NS。通过粉末 X 射线衍射评价 CUR-NS 中的药物状态。研究了 CUR-NS 经静脉给药后在兔和小鼠体内的药代动力学和分布。
结果
CUR-NS 形式的 CUR 的溶解度和溶解速度明显高于粗 CUR。X 射线结晶学衍射表明纳米混悬剂中 CUR 的晶型得以保留。兔和小鼠静脉注射 CUR-NS 后的药代动力学和分布结果表明，与 CUR 溶液相比，CUR-NS 呈现出明显不同的药代动力学特性。CUR-NS（700.43±281.53μg/mL，min）在血浆中的 AUC（0-无穷大）约为 CUR 溶液（145.42±9.29μg/mL min）的 3.8 倍，平均驻留时间（194.57±32.18 与 15.88±3.56 分钟）延长了 11.2 倍。
结论
纳米混悬剂可以作为姜黄素的一种有前途的静脉给药系统。
Zotero 插件