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一种将含-a二醇结构的药物制备成基于鸟嘌呤的超分子水凝胶用于药物输送的简单方法。

A simple method for fabricating drugs containing a -diol structure into guanosine-based supramolecular hydrogels for drug delivery.

机构信息

State Key Laboratory of Oral Diseases, National Clinical Research Center for Oral Diseases, Chinese Academy of Medical Sciences Research Unit of Oral Carcinogenesis and Management, Med-X Center for Materials, West China Hospital of Stomatology, Sichuan University, Chengdu, Sichuan, 610041, P. R. China.

Oral Biomedical Engineering Laboratory, Shanghai Stomatological Hospital, Fudan University, Shanghai, 200001, P. R. China.

出版信息

Biomater Sci. 2023 May 2;11(9):3092-3103. doi: 10.1039/d3bm00057e.

Abstract

Supramolecular hydrogels are attractive biomaterials for local drug delivery owing to their excellent self-healing, injectable, biodegradable, and biocompatible properties. However, traditional drug-loading approaches based on non-covalent encapsulation and covalent bonding have shown problems such as rapid or difficult drug release, complex reaction processes, low reaction efficiency, and decreased drug activity. Therefore, there is a need to find a simple and efficient method to load drugs into hydrogels, which possess stable drug release ability without impairing drug efficacy. In this study, we introduce dynamic borate ester bonds a simple one-pot method to load -diol-containing drugs into guanosine (G)-based supramolecular hydrogels. The experimental results confirm that the dynamic covalent borate ester bonds are formed based on the -diol groups of the drug and the G in these hydrogels. Meanwhile, the as-prepared G-based hydrogels not only possess self-healing properties and injectability but also have satisfactory biodegradability and biocompatibility. Additionally, the drug can be released from the G-based hydrogel according to the pH-responsive cleavage of the borate ester bonds without affecting drug activity. Overall, these results indicate that the simple one-pot method of utilizing the dynamic borate bond can provide a valuable reference for the design of hydrogel dosage forms.

摘要

超分子水凝胶由于其良好的自修复、可注射、可生物降解和生物相容性等特性,是一种很有吸引力的局部药物递送生物材料。然而,基于非共价包封和共价键合的传统药物加载方法存在药物释放过快或困难、反应过程复杂、反应效率低、药物活性降低等问题。因此,需要寻找一种简单有效的方法将药物载入水凝胶中,使其具有稳定的药物释放能力,而不影响药物疗效。在本研究中,我们引入了动态硼酸酯键,通过一种简单的一锅法将含有二醇的药物载入鸟苷(G)基超分子水凝胶中。实验结果证实,药物中的二醇基团和水凝胶中的 G 形成了动态共价硼酸酯键。同时,所制备的 G 基水凝胶不仅具有自修复性和可注射性,而且还具有令人满意的生物降解性和生物相容性。此外,药物可以根据硼酸酯键的 pH 响应性断裂从 G 基水凝胶中释放出来,而不会影响药物活性。总体而言,这些结果表明,利用动态硼酸酯键的简单一锅法为水凝胶剂型的设计提供了有价值的参考。

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