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[介孔纳米生物活性玻璃微球作为米诺环素的药物递送系统]

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

作者信息

Zhu L, Wang Y D, Dong Y M, Chen X F

机构信息

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.

出版信息

Beijing Da Xue Xue Bao Yi Xue Ban. 2018 Apr 18;50(2):249-253.

PMID:29643523
Abstract

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 that of mino-MNBG group (P<0.05), which was also significant larger than those of PBS and MNBG groups (P<0.05). It showed that mino-MNBG drug delivery system had antibacterial properties on Enterococcus faecalis.

CONCLUSION

The 60S MNBG that can effectively load and release minocycline may be an ideal drug carrier.

摘要

目的

构建负载并释放米诺环素的介孔纳米生物活性玻璃(MNBG)微球作为抗菌药物递送系统。

方法

采用溶胶 - 凝胶法合成MNBG微球作为药物载体。MNBG由SiO₂、CaO和P₂O₅组成。根据硅含量,MNBG微球分为四组(60S、70S、80S和90S)。采用扫描电子显微镜(SEM)观察MNBG的表面特征和粒径;进行氮吸附 - 脱附实验计算MNBG的比表面积和孔径;通过傅里叶变换红外光谱(FT - IR)和热重分析计算盐酸米诺环素的负载效率;采用紫外分光光度法测定载药颗粒在PBS溶液中21天内米诺环素的累积释放量。进行琼脂扩散试验(ADT)评估对粪肠球菌的抗菌性能。观察抑菌圈并测量其直径。

结果

MNBG微球具有良好的分散性、较大的表面积和均匀的粒径。孔径范围为4.77 nm至7.33 nm。负载实验结果表明,MNBG对盐酸米诺环素的负载效率与微球孔径有关。在60S、70S、80S和90S中,60S MNBG由于其高钙含量和大孔径,负载效率最高,为16.33%。观察到MNBG颗粒在PBS溶液中米诺环素释放速率缓慢直至第21天。结果显示,在前24小时总药物有28%的突释。累积释放量为35%,米诺环素的最终浓度维持在约47 mg/L。ADT表明米诺 - MNBG对粪肠球菌的生长有抑制作用。1 g/L米诺环素、1 g/L米诺 - MNBG和0.1 g/L米诺环素呈现抑菌圈,然而,PBS和1 g/L MNBG没有。米诺环素组的抑菌圈直径显著大于米诺 - MNBG组(P<0.05),也显著大于PBS和MNBG组(P<0.05)。表明米诺 - MNBG药物递送系统对粪肠球菌具有抗菌性能。

结论

能够有效负载和释放米诺环素的60S MNBG可能是一种理想的药物载体。

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