缓释米诺环素的介孔纳米生物玻璃载药系统  

Mesoporous nano-bioactive glass microspheres as a drug delivery system of minocycline

作　　者：朱林 王聿栋 董艳梅[1] 陈晓峰 ZHU Lin;WANG Yu-dong;DONG Yan-mei;CHEN Xiao-feng(Department of Cariology and Endodontology,Peking University School and Hospital of Stomatology&National Engineering Laboratory for Digital and Material Technology of Stomatology&Beijing Key Laboratory of Digital Stomatology,Beijing 100081,China;National Engineering Research Center for Human Tissue Restoration&Reconstruction,South China University of Technology,Guangzhou 510640,China)

机构地区：[1]北京大学口腔医学院·口腔医院,牙体牙髓科,口腔数字化医疗技术和材料国家工程实验室,口腔数字医学北京市重点实验室,北京100081 [2]华南理工大学材料科学与工程学院生物医学工程系,国家人体组织功能重建工程技术研究中心,广州510640

出　　处：《北京大学学报（医学版）》2018年第2期249-255,共7页Journal of Peking University:Health Sciences

基　　金：国家自然科学基金(51072005)资助

摘　　要：目的:构建介孔纳米生物活性玻璃(mesoporous nano-bioactive glasses,MNBG)微球装载及缓释米诺环素的载药系统。方法:采用溶胶-凝胶法制备MNBG微球作为药物载体,组分为SiO_2、CaO和P_2O_5,根据硅的含量分为60S、70S、80S和90S组。使用扫描电子显微镜(scanning electron microscope,SEM)观察材料表面结构与粒径;氮气吸脱附实验计算材料的比表面积与孔径大小;傅里叶(Fourier)红外光谱及热重分析计算MNBG颗粒对米诺环素的装载率;紫外光分光光度计测定载药系统在21 d内的药物累积释放情况;琼脂扩散实验检测载药颗粒磷酸盐缓冲液(phosphate buffer saline,PBS)对粪肠球菌生成抑菌环的大小。结果:MNBG微球为分散良好,粒径较为均一的介孔纳米球形颗粒。MNBG颗粒对米诺环素盐酸盐的装载率与其孔径大小相关,其中含60S的载药率高于70S、80S和90S组,达到16.33%。60S载药系统在PBS溶液中对米诺环素的释放于24 h内呈现突释,达到总载药量的28%;随后药物缓慢释放,在第21天时米诺环素的释放量累积达到总载药量的35%,维持药物浓度达到47 mg/L。琼脂扩散实验结果显示60S载药系统可以抑制粪肠球菌生长。结论:60S MNBG可有效装载、缓释米诺环素,是较为理想的载药材料。Objective:To construct mesoporous nano-bioactive glass(MNBG)microspheres load-release minocycline as an antibacterial drug delivery system.Methods:Sol-gel method was used to synthesze MNBG microspheres as drug carrier.The MNBG consisted of SiO2,CaO,and P2O5.According to the content of silicon,MNBG microspheres were divided into four groups(60S,70S,80S and 90S).Scanning electron microscopy(SEM)was used to observe the surface characteristic and particle size of MNBG;Nitrogen adsorption-desorption experiment was performed to calculate the MNBG’s specific surface area and the pore sizes;The Fourier transform infrared spectrum(FT-IR)and the thermogravimetric analysis were conducted to calculate the loading efficiencies of minocycline hydrochloride;UV spectrophotometric was used to determine the cumulative release of minocycline from drug-loaded particles in PBS solution within 21 d.Agar diffusion test(ADT)was performed to evaluate the antibacterial properties on Enterococcus faecalis.The inhibition zone was observed and the diameter was measured.Results:The MNBG microspheres had good dispersion,large surface area,and even particle size.The pore sizes ranged from 4.77 nm to 7.33 nm.The loading experiment results showed that the minocycline hydrochloride loading efficiency of MNBG was related to the pore size of the microspheres.Among 60S,70S,80S and 90S,60S MNBG had the highest loading efficiency of 16.33%due to its high calcium content and large pore sizes.A slow minocycline release rate from MNBG particles in PBS solution until d 21 was observed.It was showed that a burst release of 28%of the total drug for the first 24 h.A cumulative release of 35%was found,and the final concentration of minocycline maintained at about 47 mg/L.ADT showed that mino-MNBG had inhibitory effect on the growth of Enterococcus faecalis.1 g/L minocycline,1 g/L mino-MNBG,and 0.1 g/L minocycline presented inhibition zone,however,PBS and 1 g/L MNBG didn’t.The diameter of the inhibition zone of minocycline groups was significant larger than

关 键 词：介孔生物活性玻璃 米诺环素 载药系统 装载 释放 

分 类 号：R781.3[医药卫生—口腔医学]