Department of Biomedical Engineering, Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, College of Life Science and Technology, Jinan University, Guangzhou 510632, China.
Department of Biomedical Engineering, Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, College of Life Science and Technology, Jinan University, Guangzhou 510632, China.
Mater Sci Eng C Mater Biol Appl. 2019 Jun;99:159-170. doi: 10.1016/j.msec.2019.01.078. Epub 2019 Jan 25.
A magnetic-pH dual responsive drug delivery system was prepared for antibacterial therapy to reduce the side effects on nonpathological cells or tissues. Iron oxide (FeO) core was surface-functionalized with silane coupling agents to link β‑cyclodextrin (β-CD) (CDMNP), and a polypseudorotaxanes shell where polyethyleneglycol chains threaded much CD molecules was further prepared on the magnetic FeO core (CDMNP-PEG-CD) to enhance loading capacity of roxithromycin (ROX). CDMNP-PEG-CD with a hydrodynamic diameter of ~168 nm was cytocompatible, superparamagnetic, magnetic-responsive and stable for 180 min of storage. No significant interaction with serum albumin was shown for the nanocomposites. The in vitro release from ROX-loaded CDMNP-PEG-CD nanocomposites was about 76% of total drug within 30 min at pH 1.0, 1.6-fold of that at pH 7.4 and 2-fold of that at pH 8.0, presenting pH-responsive drug release behaviors. The nanocomposites showed positive antibacterial activity against both E. coli and S. aureus based on an agar diffusion method. The antibacterial activity of the nanocomposites was more sensitive against E. coli than S. aureus, and the inhibition halo against E. coli was 85% more than that of FeO. CDMNP-PEG-CD nanocomposites allowed for the localization and fast concentration of hydrophobic drugs, providing a broad potential range of therapeutic applications.
一种磁- pH 双重响应药物递送系统被制备用于抗菌治疗，以减少对非病变细胞或组织的副作用。氧化铁（FeO）核表面用硅烷偶联剂官能化以连接β-环糊精（β-CD）（CDMNP），并进一步在磁性 FeO 核上制备其中聚乙二醇链穿过许多 CD 分子的聚伪轮烷壳（CDMNP-PEG-CD）以增强罗红霉素（ROX）的载药量。具有约 168nm 水动力直径的 CDMNP-PEG-CD 具有细胞相容性、超顺磁性、磁响应性和在 180min 的储存时间内稳定。纳米复合材料与血清白蛋白没有显示出明显的相互作用。ROX 负载的 CDMNP-PEG-CD 纳米复合材料在 pH 1.0 下 30min 内的总药物释放约为 76%，在 pH 7.4 下为 1.6 倍，在 pH 8.0 下为 2 倍，呈现 pH 响应性药物释放行为。纳米复合材料基于琼脂扩散法对大肠杆菌和金黄色葡萄球菌均表现出阳性抗菌活性。纳米复合材料对大肠杆菌的抗菌活性比对金黄色葡萄球菌更敏感，对大肠杆菌的抑制晕圈比 FeO 高 85%。CDMNP-PEG-CD 纳米复合材料允许疏水性药物的定位和快速浓缩，提供了广泛的治疗应用潜力。
