葛根素纳米晶自稳定Pickering乳液的制备可行性研究  

Study on feasibility of puerarin nanocrystalline self-stabilizied Pickering emulsion

作　　者：张焦[1] 王帆[1] 王计瑞 易涛[2] 张继芬[1] ZHANG Jiao WANG Fan WANG Ji-rui YI Tao ZHANG Ji-fen(College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China School of Health Sciences, Macao Polytechnic Institute, Macao 00853, China)

机构地区：[1]西南大学药学院,重庆400716 [2]澳门理工学院高等卫生学校,澳门00853

出　　处：《中草药》2017年第1期75-84,共10页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81603304);西南大学基本科研业务费专项资金项目(XDJK2016E131);澳门理工学院资助研究项目(RP/ESS-06/2014);澳门科学技术发展基金(001/2016/A1)

摘　　要：目的考察葛根素纳米晶能否作为固体微粒稳定剂,制备出稳定的Pickering乳液,即葛根素纳米晶自稳定Pickering乳液(puerarin nanocrystalline self-stabilized Pickering emulsion,Pu-NSSPE)。方法采用高压匀质法制备Pu-NSSPE。以室温静置过程中Pu-NSSPE的外观、乳滴粒径变化为指标,考察药物加入顺序、油相组成、药物加入量、油水体积比、匀质压力和水相pH值等因素对Pu-NSSPE成型与稳定的影响,优化Pu-NSSPE的制备工艺,考察其稳定性,并用荧光倒置显微镜(FIMS)进行微观结构表征。结果制备时药物先分散于水相难以形成稳定的乳液。三相接触角和水相pH值是影响Pu-NSSPE成型与稳定的关键因素:药物/油/水三相接触角接近90°,水相pH值呈碱性,有利于Pu-NSSPE的形成与稳定。葛根素加入量在1.0~5.0 mg/mL时,可形成稳定的Pu-NSSPE;油水体积比越大,越容易分层析出油相;匀质压力低于80 MPa时,乳液不稳定。最终优化制得的Pu-NSSPE乳滴粒径为(13.86±1.56)μm,载药量为4.28 mg/mL,Zeta电位为(-41.60±2.45)mV。室温放置6个月后,外观、乳滴形态、Zeta电位和载药量等均无显著性变化,粒径略有增大。FIMS可观察到葛根素在油水界面吸附聚集。结论葛根素纳米晶自身能稳定形成Pickering乳液,所制得的Pickering乳液稳定性好,有望成为葛根素口服剂型。Objective To investigate the feasibility of Pickering emulsion stabilized by puerarin nanocrystalline. Methods The new puerarin nanocrystalline self-stabilized Picketing emulsion （Pu-NSSPE） has been developed using the high pressure homogenization method. The influences of drug addition sequence, property, and construction of oil phase, drug concentration, oil/water ratio, homogenization pressure, and pH value of water phase on the formation and stability of Pu-NSSPE were investigated to optimize the preparation technology of Pu-NSSPE. Results The stability and structure of optimized Pu-NSSPE were studied. It was difficult to form stable Pu-NSSPE ifpuerarin was first added into water during preparation. The three-phase contact angle and pH value of water phase were key factors for the formation and stability ofPu-NSSPE. Pickering emulsion could be stabilized by puerarin nanocrystalline only when three-phase contact angle of puerarin approaches 90° and water phase was alkaline. When the drug concentration was between 1.0--5.0 mg/mL, stable Pu-NSSPE could be formed. The higher oil/water ratio was, the more oil creamed from Pu-NSSPE was. Low homogenization pressure （below 80 MPa） could not form stable Pu-NSSPE. The size of emulsion droplet of optimized Pu-NSSPE was （10.66±4.81） pan, and drug content was 4.28 mg/mL. The appearance, morphology, and size of emulsion droplets, Zeta potential and drug content were not changed significantly after storage for six months at room temperature. The adsorption of puerarin at the surface of oil droplets was observed by fluorescence microscope. Conclusion Nanocrystalline of puerarin could stabilize Pickering emulsions, which will provide a promising drug delivery system for puerarin.

关 键 词：Pickering乳液 葛根素 纳米晶 自稳定 制各 可行性 稳定剂 高压匀质法 三相接触角 

分 类 号：R283.6[医药卫生—中药学]