摘要
目的制备黄芩苷-聚乙二醇-聚乳酸羟基乙酸共聚物(PEG-PLGA)载药纳米胶束,并研究其体外释药性能及在急性心肌缺血模型大鼠体内的组织分布。方法采用正交试验优选黄芩苷PEG-PLGA纳米胶束的制备工艺,优化的黄芩苷PEG-PLGA纳米胶束再进行粒径、Zeta电位和透射电子显微镜(TEM)检测表征,采用体外释放实验、组织分布实验对该载药系统进行评价。结果黄芩苷PEG-PLGA纳米胶束优选的制备工艺条件为黄芩苷-PEG-PLGA的质量比为1∶10,旋转蒸发仪转动速率为80 r/min,水化温度为40℃,优化的黄芩苷PEG-PLGA纳米胶束粒径为(18.5±0.5)nm,Zeta电位为(-10.9±0.7)mV,载药量为(7.9±0.3)%,包封率为(86.2±2.5)%。采用芘测定法检测PEG-PLGA纳米胶束的临界胶束质量浓度为3.8μg/mL,TEM检测发现黄芩苷PEG-PLGA纳米胶束呈现粒径均一的圆球型;体外释放实验表明,黄芩苷PEG-PLGA纳米胶束具有明显的缓释特征;组织分布实验表明黄芩苷PEG-PLGA纳米胶束在正常大鼠脏器中分布大小顺序为肝>脾>心>肾>肺>脑,而在急性心肌缺血模型大鼠脏器分布大小顺序为肝>心>脾>肾>肺>脑,与正常大鼠比较,急性心肌缺血模型大鼠心脏中药物浓度在各时间段都呈现明显升高的趋势,在120 min时最高药物质量浓度可达(2 897±135)ng/mL,显著高于正常大鼠中心脏的最高药物浓度(2 411±89)ng/mL,该结果表明,黄芩苷PEG-PLGA纳米胶束在急性心肌缺血区域具有良好的靶向性。结论黄芩苷PEG-PLGA纳米胶束具有良好的载药性能,体外释药缓慢,且可以将药物蓄积于缺血心肌部位,具有良好的心脏靶向性。
Objective To compare the effects of different drying methods on six bioactive constituents of Zingiberis Rhizoma（ZR）, and explore the dynamic changes of bioactive constituents and water content during the drying process. Methods The multiple components in ZR were simultaneously measured by HPLC, and 6-gingerol, 8-gingerol, 10-gingerol, 6-shogaol, α-curcumene,（E）-β-farnesene were used as indexes to evaluate ZR obtained from different drying methods. The Weibull function was used to simulate the dynamic change of water content, which was combined with the dynamic changes of components during the drying process of ZR to explore the principle of drying process. Results A total of 12 kinds of drying methods had a certain effect on the multiple components of ZR, and the components presented the fluctuation change in the drying process. The coefficient of correlation of Weibull functional simulation of ZR drying process was greater than 0.990. Conclusion ZR obtained by drying at 60 ℃ was better. Water content range of 6% — 15% was suitable for processing ZR. 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol were significantly negatively correlated with the moisture content of ZR. The Weibull distribution model could well simulate the fluctuation change of water content in the drying process, and it was of great significance for the prediction and quality control of ZR during drying process, which could also provide a technical basis for the use of modern drying technology to dry ZR at the same time.
作者
赵炎军
王建平
吴凡
谢瑞
周定荣
ZHAO Yan-jun;WANG Jian-pingl;WU Fanl;XIE Ruil;ZHOU Ding-rong(Department of Pharmacy,Zhejiang Provincial Hospital of Traditional Chinese Medicine,Hangzhou 310006,China;Central Laboratory of The Second Xiangya Hospital of Central South University,Changsha 41001 l,China)
出处
《中草药》
CAS
CSCD
北大核心
2018年第18期4269-4276,共8页
Chinese Traditional and Herbal Drugs
基金
湖南省卫计委基金资助项目(C201800141)
