摘要
目的制备合适尺寸的负载药物的纳米制剂,通过表面修饰,获取一种具有缓控释性的脑组织药物递送系统。方法琥珀酸胆甾醇酯(CHS)与普鲁兰多糖经酯化反应形成疏水改性普鲁兰多糖(CHP)。CHP再通过透析法负载长春新碱(VCR)及通过乳化作用对聚山梨酯80(PS-80)进行表面修饰,得到VCR-CHP-PS纳米粒子。利用傅立叶红外光谱仪(FTIR)、核磁共振氢谱仪(^(1)H-NMR)对聚合物进行表征,动态光散射仪表征纳米粒子的粒径及电位。透射电镜观测CHP形态,并用等温滴定量热法测定载药纳米粒子VCR-CHP对PS-80的吸附特性。结果FTIR和^(1)H-NMR证明CHS和CHP已成功合成。VCR-CHP-PS纳米粒子的平均粒径为414.2 nm,平均PDI为0.325,平均Zeta电位约为-19.5 mV。PS-80在CHP纳米粒子上的覆盖率为(149±43.5)%。VCR-CHP纳米粒子中VCR的载药量约为5.36%,包封率约为61.14%,72 h释放量约为61.43%。结论疏水改性普鲁兰多糖纳米制剂具有较好的载药量和包封率及一定的缓释功能,有望成为脑靶向纳米药物载体。
ObjectiveTo prepare the drug-loaded nano-preparation of suitable size, through surface modification, to attain a brain tissue drug delivery system with sustained function.MethodsCholesterol succinate(CHS) was esterified with pullulan polysaccharide to form hydrophobic modified pullulan polysaccharide(CHP). CHP was loaded with vincristine(VCR) by dialysate and emulsified with surface modification of polysorbate 80(PS-80) to obtain the VCR-CHP-PS nanoparticles. The polymer was characterized by Fourier transform infrared spectroscopy(FTIR) and nuclear magnetic resonance hydrogen spectrometer(^(1) H-NMR). The particle size and potential of nanoparticles were characterized by dynamic light scattering instrument. The morphology of CHP was observed by transmission electron microscope, and the adsorption properties of drug-loaded nanoparticles(VCR-CHP) for polysorbate 80 were studied by isothermal titration calorimetry.ResultsFTIR and^(1) H-NMR proved CHS and CHP were successfully synthetized. The average particle size of VCR-CHPPS was 414.2 nm, and the average PDI was 0.325, and the average potential was about-19.5 mV. The coverage of PS-80 on CHP nanoparticles was(149±43.5)%. In VCR-CHP nanoparticles, the drug loading of VCR was about 5.36%, and the entrapment efficiency was about 61.14%. The drug release amount reached to 61.43% after 72 hours.ConclusionHydrophobic modified pullulan nanoparticles have good drug loading, entrapment efficiency and certain sustained release function, and are expected to be the carrier of brain-targeting nanopharmaceuticals.
作者
郑永强
付俊伟
朱慧敏
陶晓军
ZHENG Yongqiang;FU Junwei;ZHU Huimin;TAO Xiaojun(Department of Neurology,Second People's Hospital of Three Gorges University,Yichang,Hubei,443099,China;Pharmacy Teaching and Research Office,School of Medicine,Hunan Normal University,Changsha,Hunan,410081,China)
出处
《肿瘤药学》
CAS
2021年第5期547-553,共7页
Anti-Tumor Pharmacy
基金
湖北省卫生健康委员会面上项目(NO:WJ2019M065)
湖北省教育厅科研项目(B2019025)
宜昌市科学技术局医疗卫生研究项目(NO:A20-2-034)
湖南省大学生研究性学习和创新性实验计划项目(201910542035)。
