基于新型树枝状大分子姜黄素纳米粒的制备及体外释放  

Preparation and In Vitro Release of Curcumin Nanoparticles with A Novel Codendrimer as Stabilizer

作　　者：李然[1,2] 赵燕娜[1,3] 王婷[1,2] 韩美华[1] 王向涛[1] 阎雪莹[2] 郭一飞[1] 

机构地区：[1]中国医学科学院北京协和医学院药用植物研究所,北京100193 [2]黑龙江中医药大学,哈尔滨150040 [3]聊城大学生物制药研究院,聊城150040

出　　处：《医药导报》2017年第5期538-543,共6页Herald of Medicine

基　　金：国家自然科学基金资助项目(21444003)

摘　　要：目的研究提高姜黄素(CUR)的溶解度和生物利用度的方法。方法选用一种新型的树枝状大分子(PGD)作为稳定剂制备姜黄素纳米粒。采用超声沉淀联合高压均质法制备CUR-PGD纳米粒。考察CUR-PGD纳米粒在0.9%氯化钠溶液、5%葡萄糖溶液、磷酸盐缓冲液(PBS)及血浆中的稳定性。结果 CUR-PGD纳米粒载药量高达41.2%,CUR在水中的溶解度较原药提高50倍,达到1.5 mg·mL^(-1)。CUR-PGD纳米粒粒径438.0 nm,扫描电镜观察为球形,电位41.4 mV。纳米粒在0.9%氯化钠溶液、5%葡萄糖溶液、PBS及血浆中均稳定,无红细胞溶血现象,适合于静脉注射给药。CUR-PGD纳米粒DSC及XRD图谱显示,CUR在纳米粒中以晶型形式存在。CUR-PGD纳米粒在不同释放介质中缓释效果明显。结论 PGD可作为一种有效的稳定剂制备CUR-PGD纳米粒,该纳米粒有望作为一种新型的药物输送系统扩展姜黄素在临床中的应用。Objective To enhance the solubility and bioavailability of curcumin （CUR）.Methods A novel curcumin nanoparticles were prepared.The CUR-PGD nanoparticles were prepared by the method of ultrasound precipitation combined with high-pressure homogenization using codendrimer PAMAM-co-0.25OEG （PGD） as stabilizer.The stability of CUR-PGD nanoparticles was measured in 0.9% sodium chloride solution,5% glucose, PBS and plasma.Results The drug loading capacity （DL%） of CUR-PGD nanoparticles was 41.2%, the solubility of CUR was increased to 1.5 mg·mL-1 （50 times of CUR bulk powder）.The mean diameter of the nanoparticles was 438.0 nm with spherical morphology and the zeta potential was 41.4 mV.The nanoparticles was stable in 0.9% sodium chloride solution,5% glucose, PBS and plasma and there was no hemolytic phenomenon, which meant they were suitable for intravenous administration.The DSC and XRD spectra of CUR-PGD nanoparticles showed that the CUR was presented as crystal morphology in the nanoparticles.The CUR released from nanoparticles was detected in different releasing medium and presented obvious controlled release behavior.Conclusion PGD may be an effective stabilizer for the preparation of CUR-PGD nanoparticles and CUR-PGD nanoparticles are a promising drug delivery system for CUR application in clinic.

关 键 词：姜黄素纳米粒 树枝状大分子 释放 体外 

分 类 号：R944.9[医药卫生—药剂学] TQ460.6[医药卫生—药学]