共载姜黄素与胡椒碱纳米结构脂质载体的体外释放研究  

In vitro release of curcumin and piperine nanostructured lipid carriers

作　　者：吴赵莉 韩新宇 田思宇 张程皓 任金妹 唐景玲[1] WU Zhao-li;HAN Xin-yu;TIAN Si-yu;ZHANG Cheng-hao;REN Jin-mei;TANG Jing-ling(College of Pharmacy,Harbin Medical University,Harbin 150086;Qingpu Branch of Zhongshan Hospital Affiliated to Fudan University,Shanghai 201700)

机构地区：[1]哈尔滨医科大学药学院,哈尔滨150086 [2]复旦大学附属中山医院青浦分院,上海201700

出　　处：《中南药学》2023年第6期1436-1440,共5页Central South Pharmacy

基　　金：黑龙江省自然科学基金项目(No.H2018013);哈尔滨医科大学药学院杰出人才基金项目(No.2019-JQ-03);上海市青浦区科技发展基金项目(No.QKY2019-18);复旦大学附属中山医院青浦分院院级课题(No.QYP2020-03)。

摘　　要：目的 制备姜黄素/胡椒碱纳米结构脂质载体(CP-NLCs)并对其外观性状、包封率、载药量和体外药物释放进行考察。方法 本研究使用乳化蒸发-高压均质法制备CP-NLCs,并对制备的CP-NLCs进行质量评价,包括利用透射电镜对CP-NLCs的外观形态进行观察;Malvern激光粒度仪测定CP-NLCs的粒径、Zeta电位和多分散系数(PDI);采用超滤离心法测定CP-NLCs的包封率和载药量;利用正向动态透析法研究CP-NLCs以及姜黄素、胡椒碱溶液的体外释放行为。结果 测得CP-NLCs外观为类球状颗粒,平均粒径为38.59 nm,PDI为0.217,Zeta电位为-6.86 mV。CP-NLCs中姜黄素的包封率为(99.48±0.41)%,载药量为(13.26±0.06)%;胡椒碱的包封率为(97.28±0.19)%,载药量为(6.48±0.13)%。体外释放实验显示姜黄素溶液在48 h释放69.30%,胡椒碱溶液在24 h释放68.86%,而CP-NLCs中的姜黄素在48 h内累积释放86.02%,CP-NLCs中的胡椒碱在24 h内累积释放90.35%。结论CP-NLCs粒径较小,包封率、载药量较高,具有一定的缓释作用,并能显著增加难溶性药物的释放量。Objective To prepare nanostructured lipid carriers co-loaded with curcumin and piperine(CPNLCs),and measure their appearance,encapsulation efficiency,drug loading and drug release in vitro.Methods CP-NLCs were prepared with emulsification evaporation-high pressure homogenization method.The quality of the CP-NLCs was evaluated,including observing the appearance and morphology of CPNLCs by transmission electron microscopy.Malvern laser particle sizer was used to measure the particle size,Zeta potential,and polydispersity index(PDI)of CP-NLCs.The encapsulation efficiency and drug loading of CP-NLCs were measured by ultrafiltration centrifugation.Forward dynamic dialysis was used to determine the in vitro release behaviors of CP-NLCs.Results Transmission electron microscopy showed that freshly prepared CP-NLCs had smooth spherical particles without aggregation and adhesion,with small particle size and good dispersion.The optimized CP-NLCs demonstrated mean particle size of 38.59 nm,Zeta potential of-6.86 mV,and PDI of 0.217.The encapsulation rate of curcumin in CP-NLCs was(99.48±0.41)%,and the drug loading was(13.26±0.06)%.The encapsulation rate of piperine was(97.28±0.19)%,and the drug loading was(6.48±0.13)%.The in vitro release showed that the curcumin solution released 69.30%at 48 h,and the curcumin in CP-NLCs released 86.02%at 48 h.The piperine solution released 68.86%at 24 h,and the piperine in CP-NLCs released 90.35%at 24 h.Conclusion CP-NLCs have small particle size,high entrapment efficiency and drug loading,and has sustained release effect and can greatly increase the release of insoluble drugs.

关 键 词：姜黄素 胡椒碱 纳米结构脂质载体 体外释放 

分 类 号：R283[医药卫生—中药学]