pH响应性可降解聚(醚酯-氨酯)的制备及在药物缓释领域的应用
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Preparation of pH-Responsive Degradable Poly (ether-ester-urethane) and Potential Application for Controlled Drug Release
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    摘要:

    设计和制备了一类具有高pH响应性的可降解聚氨酯材料,旨在作为一种智能给药载体。首先通过“硫醇-烯”点击反应合成了一种吡啶基二醇(PyDH);然后,以PyDH、聚醚酯二醇和二异氰酸酯为原料,通过缩聚反应制备了侧链含吡啶基团的聚(醚酯-氨酯)(PEEU-Py),并经溶剂挥发得到相应的薄膜材料。通过核磁共振、红外光谱、凝胶渗透色谱等对PyDH 和PEEU-Py 的化学结构进行了表征,并对PEEU-Py 膜的力学、溶胀、降解、药物缓释等性能进行了研究。PEEU-Py 膜展示出高的pH溶胀性,其在pH=1.5 介质中的平衡吸水率分别为pH=7.0 和pH=11.5 的2 倍和8 倍以上;体外药物缓释研究表明,膜材料的药物释放速率随pH值的降低而提高,其药物释放能力与材料的溶胀性能相一致。此外,细胞毒性评价表明该材料具有良好的细胞相容性。研究结果表明,PEEU-Py 作为一种受外界pH变化触发的智能开关在药物载体上有好的应用前景。

    Abstract:

    This paper presented the design and preparation of a new kind of degradable polyurethane with highly pH- sensitivity, which was hoped to apply in the field of intelligent drug delivery. The diol contained pyridinyl(PyDH) was first synthesized via “click” reaction, then the poly(ether-ester-urethane) with pendent pyridinyls (PEEUPy) was prepared from PyDH, poly(ether- ester) diol and diisocyanate via condensation polymerization, and the corresponding films were obtained by solvent evaporation. The chemical structures of PyDH and PEEU- Py were characterized by 1H-NMR, IR and GPC, and the tensile properties, swellabilities, degradability and drug release properties of the PEEU-Py films were researched. The films exhibit highly pH-sensitive equilibrium water absorption(EWA), the EWA at pH of 1.5 is twofold and eightfold of that at pH of 7.0 and 11.5, respectively. The drug release efficiency increases with the decreasing of pH value, which is consistent with the EWA, indicating a pH-dependent release efficiency. The cytotoxicity evaluation indicates that the materials possess good cytocompatibility. All the results manifest that the materials have promising applications as intelligent drug carriers controlled by pH value.

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张冬梅, 张娜,纪晨旭, 赵海云, 张丹丹, 刘文坤. pH响应性可降解聚(醚酯-氨酯)的制备及在药物缓释领域的应用[J].高分子材料科学与工程,2022,38(9):23-30.

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  • 在线发布日期: 2022-11-23
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