共轭亚油酸-紫杉醇自组装纳米粒的结构分析  

Structure of the Conjugated Linoleic Acid-Paclitaxel Conjugate Self-Assembled Nanoparticles

作　　者：郑秀钗 徐美琦 刘曼 钟婷 郝艳丽[1,2] 张爽 李展韬[1,2] 李卓越 段晓川 冯振汉 王景茹 李惠 王光雪 廖嫒 张华 刘碧林 张烜 ZHENG Xiu-chai;XU Mei-qi;LIU Man;ZHONG Ting;HAO Yan-li;ZHANG Shuang;LI Zhan-tao;LI Zhuo-yue;DUAN Xiao-chuan;FENG Zhen-han;WANG Jing-ru;LI Hui;WANG Guang-xue;LIAO Ai;ZHANG Hua;LIU Bi-lin;ZHANG Xuan(Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems,School of Pharmaceutical Sciences,Peking University,Beijing 100191,China;Department of Pharmaceutics,School of Pharmaceutical Sciences,Peking University,Beijing 100191,China;Key Laboratory of Xinjiang Phytomedicine Resources and Utilization of Ministry of Education,School of Pharmacy,Shihezi University,Shihezi 832000,China;College of Pharmaceutical Engineering,Chongqing Chemical Industry Vocational College,Chongqing 401228,China)

机构地区：[1]北京大学医学部药学院分子药剂学与新释药系统北京市重点实验室,北京100191 [2]北京大学医学部药学院药剂学系,北京100191 [3]石河子大学药学院新疆植物药资源利用教育部重点实验室,新疆石河子832000 [4]重庆化工职业学院制药工程学院,重庆401228

出　　处：《中国药学杂志》2019年第21期1752-1757,共6页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金项目资助(81773646);国家重点研发计划资助(2017YFA0205600);教育部创新团队项目资助(BMU2017TD003)

摘　　要：目的制备共轭亚油酸-紫杉醇自组装纳米粒(conjugated linoleic acid-paclitaxel conjugate self-assembled nanoparticles,CLA-PTX NPs)。方法本实验采用纳米沉淀法制备,通过动态光散射、核磁共振氢谱、拉曼光谱、傅里叶变换红外光谱及氮元素分布分析等方法对所制备的CLA-PTX NPs的表面和内部基团进行表征,确定CLA-PTX NPs的表面基团和内部基团,为阐述其自组装机制提供依据。结果PTX中C-1位和C-7位的羟基、C-4位和C-10位的乙酰基位于CLA-PTX NPs的表面,CLA碳链、PTX中C-2位和C-3'位的苯环及C-3'位的酰胺键位于CLA-PTX NPs的内部。据此推测CLA-PTX的自组装方式是非极性的CLA碳链因疏水作用而自发向内聚集,PTX中亲水的含氧基团羟基、羰基等在纳米粒表面从而形成纳米粒。结论CLAPTX NPs表面基团的确定也为其可能的表面修饰提供参考和依据。更为重要的是,本实验还为其他自组装纳米粒结构的表征提供了相关可行的方法。OBJECTIVE To prepare,the conjugated linoleic acid-paclitaxel conjugate self-assembled nanoparticles(CLA-PTX NPs)by nanoprecipitation.METHODS The Dynamic light scattering,nuclear magnetic resonance spectroscopy,raman spectroscopy,fourier transform infrared spectroscopy and nitrogen element distribution of CLA-PTX NPs were studied.RESULTS The hydroxyl groups(C-4 and C-10 of PTX)and the acetyl groups(C-1 and C-7 of PTX)were on the surface of CLA-PTX NPs,CLA carbon chain,the benzene ring(C-2 and C-3'of PTX)and the amide bond(C-3'of PTX)were inside the CLA-PTX NPs.CONCLUSION It is speculated that the self-assembly of CLA-PTX is that the non-polar CLA carbon chain spontaneously aggregates inward due to hydrophobic interaction,and the hydrophilic oxygen-containing groups of PTX(hydroxyl group and carbonyl group)are on the surface of the nanoparticle to form nanoparticles.

关 键 词：共轭亚油酸-紫杉醇自组装纳米粒 结构 核磁共振氢谱 拉曼光谱 氮元素分布分析 

分 类 号：R944[医药卫生—药剂学]