负载3-甲基腺嘌呤介孔二氧化硅的制备与释药性能研究  

Preparation and release properties of 3-methyladenine mesoporous silica

作　　者：韩卓越 王秀 巫业振 胡浩然 邢亚群[1] HAN Zhuo-yue;WANG Xiu;WU Ye-zhen;HU Hao-ran;XING Ya-qun(Department of Pharmacy,The Second Affiliated Hospital of Bengbu Medical College,Bengbu Anhui 233000;School of Pharmacy,Bengbu Medical College,Bengbu Anhui 233000)

机构地区：[1]蚌埠医学院第二附属医院药剂科,安徽蚌埠233000 [2]蚌埠医学院药学院,安徽蚌埠233000

出　　处：《中南药学》2024年第2期347-351,共5页Central South Pharmacy

摘　　要：目的制备唑来膦酸(ZOL)修饰的聚多巴胺(PDA)包覆介孔二氧化硅(MSN)纳米颗粒,对其进行表征及释药性能研究。方法将ZOL与氨基-聚乙二醇-巯基连接作为骨靶向配体,通过加成反应修饰在PDA包覆的MSN表面,得到药物载体MSN@PDA-PEG-ZOL,通过1H-NMR、FT-IR、TEM、粒径及Zeta电位等方法对其进行表征。以自噬抑制剂3-甲基腺嘌呤(3-MA)为药物模型,设计不同药物浓度计算载药量及包封率,筛选最佳处方,并考察药物在不同环境下的释放量。结果制备得到的纳米颗粒为分散均匀的球形结构;粒径及Zeta电位分别为(229.1±8.8)nm、-(30.3±0.6)mV;载药浓度在1000μg·mL^(-1)时,其包封率为(90.87±0.05)%,载药量为(37.55±0.02)%。纳米颗粒在pH 7.4的PBS溶液中48 h内的药物释放率为(16.99±0.15)%,在pH 5.0的PBS溶液中的释放率为(65.11±1.64)%,有利于药物在肿瘤微环境中的释放。结论本文成功制备了负载3-MA且具有靶向性和pH响应性的纳米制剂,其分散性好,具有高载药量、高包封率等特点,可为后续研究奠定基础。Objective To prepare polydopamine(PDA)coated mesoporous silica nanoparticles(MSN)nanoparticles modified with zoledronic acid(ZOL),and to determine their characterization and drug release properties.Methods ZOL was connected with amino-pegyl-sulfhydryl group as the bone targeting ligand and modified on PDA-coated MSN surface by addition reaction to obtain MSN@PDA-PEG-ZOL,which was characterized by 1H-NMR,FT-IR,TEM,particle size and Zeta potential.Autophagy inhibitor 3-methyladenine(3-MA)was used as a drug model.Different drug concentrations were designed to calculate the drug loading and encapsulation rate,and screen the optimal prescription.The drug release of in different environments was determined.Results The prepared nanoparticles had uniform spherical structure.The particle size was(229.1±8.8)nm and the Zeta potential was-(30.3±0.6)mV.When the drug loading concentration was 1000μg·mL^(-1),the encapsulation rate was(90.87±0.05)%and the drug loading was(37.55±0.02)%.The drug release rate of nanoparticles was(16.99±0.15)%in PBS solution(pH 7.4)and(65.11±1.64)%in PBS solution(pH 5.0)within 48 h,which was more conducive to drug release in tumor microenvironment.Conclusion Nanometer preparations loaded with 3-MA with targeting and pH response are successfully prepared,with good dispersion,high drug loading and encapsulation rate,etc.,laying the foundation for further research.

关 键 词：介孔二氧化硅 3-甲基腺嘌呤 骨靶向 PH响应 

分 类 号：R914.2[医药卫生—药物化学] R94[医药卫生—药学]