新型紫杉醇纳米粒的构建及其体外表征  

Construction and in vitro characterization onf ovel Paclitaxel nanoparticles

作　　者：陈金清 黄国颖 李广铨 唐灵 张忠斌 何秋梅 孔祥玉 丁文雅 CHEN Jinqing;HUANG Guoying;LI Guangquan;TANG Ling;ZHANG Zhongbin;HE Qiumei;KONG Xiangyu;DING Wenya(Guangxi Engineering Research Center for Advantageous Chinese Patent Medicine and Ethnic Medicine Development,Key Laboratory of Generic Technology Research and Development of Traditional Chinese Medicine Preparations,Guangxi University of Traditional Chinese Medicine,Nanning,Guangxi,530200 P.R.China)

机构地区：[1]广西中医药大学中药制剂共性技术研发重点实验室、广西优势中成药与民族药开发工程技术研究中心,广西南宁530200

出　　处：《华西药学杂志》2023年第6期599-602,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:82060806);江西中医药大学现代中药制剂教育部重点实验室开放基金项目(zdsys-202207);中医药生物新材料关键技术研究与智能装备开发学科交叉创新团队项目(GZKJ2303);广西中医药大学研究生教育创新项目(YCSZ2022008);广西中医药大学大学生科研训练课题(2021DXS09);广西中医药大学大学生创新创业训练计划项目(S202210600053,S202310600107)。

摘　　要：目的制备紫杉醇/明胶接枝环糊精(Gel-CD)/聚乙二醇2000维生素E琥珀酸酯(TPGS-2000)载药纳米粒,并对其性质及体内分布进行考察。方法采用探头超声波法制备紫杉醇纳米粒,测定其粒径、PDI、Zeta电位、包封率及载药量;采用扫描电镜观察纳米粒的形态;动态透析考察药物的体外释放情况;HPLC法测定药物在小鼠体内的分布情况。结果紫杉醇纳米粒的平均粒径为367.5±1.35 nm,PDI为0.254±0.08,Zeta电位为-6.54±0.05 mV,包封率为83.62%±6.76%,载药量为6.38%±0.29%;外观为乳白色近球形,大小分布均匀;144 h的累积释放率约86%。紫杉醇纳米粒可减少紫杉醇在心脏组织的分布,降低其不良反应。结论紫杉醇/Gel-CD/TPGS-2000纳米粒性质优良,具有明显的缓释效果,可降低紫杉醇的心脏不良反应,为紫杉醇新制剂的研发提供了新思路。OBJECTIVE To prepare Paclitaxel/gelatin grafted cyclodextrin(Gel-CD)/polyethylene glycol 2000 Vitamin E succinate(TPGS-2000)nanoparticles and to investigate its properties and distribution in vivo.METHODS Paclitaxel nanoparticles were prepared by probe ultrasonic method,and the particle size,PDI,Zeta potential,encapsulation rate and drug loading of the nanocapsules were determined.The morphology of the nanoparticles was observed by SEM,the release of the drugs in vitro was investigated by dynamic dialysis,and the distribution of the drugs in vivo was determined by HPLC.RESULTS Paclitaxel nanoparticle was prepared with the average particle size of 367.5±1.35 nm,PDI of 0.254±0.08,Zeta potential of-6.54±0.05 mV,the encapsulation rate of 83.62%±6.76%,and the drug loading of 6.38%±0.29%.The appearance of nanoparticles was milky white,and nearly spherical with uniform size distribution.The cumulative release rate of Paclitaxel nanocrystals at 144 h was about 86%.Paclitaxel has toxic effects on the heart,and Paclitaxel nanoparticles reduce the distribution of Paclitaxel in cardiac tissues,which in turn reduces its side effect.CONCLUSION Paclitaxel/Gel-CD/TPGS-2000 nanoparticles has excellent properties and obvious slow-release effect,which can reduce the cardiotoxicity of Paclitaxel and provide new ideas for the development of new Paclitaxel formulations.

关 键 词：紫杉醇 纳米粒 明胶接枝环糊精 聚乙二醇2000维生素E琥珀酸酯 制备工艺 体外表征 体内分布 

分 类 号：R94[医药卫生—药剂学]