莫西沙星/纳米纤维素缓释膜的制备及其释药性能研究

doi:10.3969/j.issn.1673-5854.2018.01.001

摘要/Abstract

摘要： 将2，2，6，6-四甲基哌啶-1-氧化物自由基（TEMPO）氧化纳米纤维素（NFC）与广谱抗菌剂莫西沙星通过物理共混、真空抽滤制备出具有缓释和抗菌特性的莫西沙星/NFC缓释膜。研究了NFC的羧基含量、制备NFC时的均质次数对莫西沙星/NFC缓释膜的力学性能、溶胀性能以及药物释放性能的影响，同时探究了缓释膜的抑菌效果。结果表明：当NFC含羧基为1.13 mmol/g，NFC制备时的均质次数为8次时，莫西沙星/NFC缓释膜的弹性模量为3.48 GPa，其平衡溶胀率比NFC膜高，可达到6.03，药物负载率为21%，在体外8 h释药量为19.96%。不同羧基含量的莫西沙星/NFC缓释膜的药物释放曲线均符合Peppas方程；均质次数和pH值增加时，缓释膜的药物释放由渗透和溶胀释放为主转为浓度差驱动的扩散释放为主，相应地其释放曲线由符合Higuchi方程转为符合Peppas方程。莫西沙星/NFC缓释膜对标准金黄色葡萄球菌的抑菌圈直径在4.38~6.33 mm范围内，有着明显的抗菌作用，含羧基1.70 mmol/g，均质次数8次的莫西沙星/NFC缓释膜抑菌效果最好。

关键词: 莫西沙星, 纳米纤维素, 缓释膜, 释药性能, 抑菌效果

Abstract: Moxifloxacin/nanofibrillated cellulose(NFC) sustained-release films were prepared by compounding the TEMPO oxidized NFC with the broad-spectrum antibacterial moxifloxacin through the vacuum filtration. The influences of the NFC carboxyl contents and homogenizing times on mechanical properties, swelling properties and drug release properties of sustained-release films were investigated. The antibacterial effect of sustained-release films was also explored. Results showed that when the NFC carboxyl contents was 1.13 mmol/g, homogenizing times were 8 times, the sustained-release film exhibited the elastic modulus of 3.48 GPa and the equilibrium swelling ratio of 6.03 which was higher than that of the NFC film; and when the drug-loading rate of the moxifloxacin/NFC sustained-release films was 21 %, the moxifloxacin was released about 19.96 % within 8 h. The drug release curves of moxifloxacin/NFC sustained-release films with different carboxyl contents all conformed to the Peppas equation. As the homogenizing times and pH increase, the drug release of sustained-release films was dominated by osmotic and swelling release into diffusion release which was driven by concentration difference, correspondingly, the drug release curves changed from being fitted by Higuchi equation to Peppas equation. The inhibition zone's diameters of standard staphylococcus aureus were in the range of 4.38-6.33mm around the sustained-release films, which indicated that the moxifloxacin/NFC had obvious antibacterial effect. The moxifloxacin/NFC film with the carboxyl content of 1.70 mmol/g and homogenizing time of 8 had the best antibacterial effect.

Key words: moxifloxacin, nanofibrillated cellulose, sustained-release films, drug release property, antibacterial effect

中图分类号:

TQ35
TB332

唐爱民, 闫长媛, 李德贵. 莫西沙星/纳米纤维素缓释膜的制备及其释药性能研究[J]. 生物质化学工程, 2018, 52(1): 1-9,28.

TANG Aimin, YAN Changyuan, LI Degui. Preparation of Moxifloxacin/Nanofibrillated Cellulose Sustained-release Films and Its Drug Releasing Property[J]. bce, 2018, 52(1): 1-9,28.

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