槲皮素纳米晶自稳定Pickering乳液的制备及体外释放研究  

Preparation and in vitro release of quercetin nanocrystals self-stabilized Pickering emulsion

作　　者：王哲[1,2] 胡菲 车智慧 宋青 申宝德 袁海龙 WANG Zhe;HU Fei;CHE Zhi-hui;SONG Qing;SHEN Bao-de;YUAN Hai-long(School of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Department of Pharmacy,Air Force Medical Center,PLA,Beijing 100142,China)

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]空军特色医学中心药学部,北京100142

出　　处：《中国中药杂志》2022年第5期1230-1236,共7页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金面上项目(81873092);军队后勤科研重点项目(BKJ15J005,BKJ16J011)。

摘　　要：为了提高槲皮素的口服吸收,以槲皮素纳米晶(QT-NC)为固体稳定剂,采用高压均质法联合探头超声法制备槲皮素纳米晶自稳定Pickering乳液(QT-NSSPE)。考察了油相比例、槲皮素浓度和水相pH对QT-NSSPE形成的影响,对得到的QT-NSSPE进行表征,并评价其稳定性和体外释放行为。结果得到优化条件下的QT-NSSPE乳滴粒径为15.82μm,载药量为4.87 mg·mL^(-1);扫描电镜观察到QT-NC在乳滴表面包裹成了壳状结构,X-射线衍射图谱表明QT-NSSPE表面吸附的QT-NC的结晶度相比于原料药显著降低;QT-NSSPE在室温条件下至少可以稳定30 d;QT-NSSPE的体外累积释放度比QT原料药显著提高。研究结果表明QT-NSSPE具有较好的稳定性和体外释放行为,有望成为槲皮素的新型口服载药系统。A new quercetin nanocrystals self-stabilized Pickering emulsion(QT-NSSPE)was prepared by high-pressure homogenization combined with probe ultrasonic method.The influences of oil fraction,quercetin(QT)concentration,and pH of water phase on the formation of QT-NSSPE were investigated.On this basis,the QT-NSSPE prepared under optimal conditions was evaluated in terms of microstructure,stability,and in vitro release and the droplet size and drug loading were 15.82μm and 4.87 mg·mL^(-1),respectively.The shell structure formed by quercetin nanocrystals(QT-NC)on the emulsion droplet surface was observed under a scanning electron microscope(SEM).X-ray diffraction(XRD)showed that the crystallinity of adsorbed QT-NC decreased significantly as compared with the raw QT.There were not significant changes of QT-NSSPE properties after 30 days of storage at room temperature.The in vitro release experiment confirmed that QT-NSSPE has a higher accumulative release rate than the raw QT.All these results indicated that QT-NSSPE has a great stability and a satisfactory in vitro release behavior,which is a promising new oral delivery system for QT.

关 键 词：Pickering乳液 槲皮素 纳米晶 自稳定 高压均质法 探头超声法 

分 类 号：R283.6[医药卫生—中药学]