壳聚糖修饰的金属有机框架作为口服给药的有前途的载体,RSC Advances

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壳聚糖修饰的金属有机框架作为口服给药的有前途的载体
RSC Advances ( IF 3.9 ) Pub Date : 2020-12-22 , DOI: 10.1039/d0ra08459j
Li Li _{1,

2} , Shasha Han ₁ , Sengqun Zhao ₁ , Xurui Li ₁ , Bingmi Liu _{1,

2} , Yu Liu _{1,

2}

Affiliation

金属-有机框架（MOFs）由有机连接体和金属离子组成，已成为治疗癌症和其他疾病的优秀药物递送剂。目前，MOF的研究主要集中在静脉给药，而专门针对口服给药的研究相对较少。本研究合成了 5 种 MOF，即 UiO-66、UiO-66-NH ₂、UiO-66-COOH、UiO-67 和 Zr-NDC，其中 Zr-NDC 的载药量最大为 5-傅。接下来，开发了壳聚糖 (CS) 修饰的 Zr-NDC，为 5-FU 的口服给药提供了强大的动力。体外异硫氰酸荧光素（FITC）标记壳聚糖的释放实验表明，FITC标记壳聚糖在人工胃液和人工肠液中的累积释放率分别约为20%和90%。体外的药物释放曲线显示，在CS-MOF保护下，5-FU在酸性环境中的释放率仅为20%，但在人工肠液中的释放率达到70%。药代动力学分析表明，壳聚糖包覆在 MOFs 表面发挥了控释作用，进一步提高了 5-FU 的口服生物利用度。这些发现表明，CS涂层可以突破MOF不耐酸的限制。预计 CS-MOF@5-FU 可以作为一种潜在的 5-FU 口服给药系统。

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Chitosan modified metal–organic frameworks as a promising carrier for oral drug delivery

Metal–organic frameworks (MOFs) are composed of both organic linkers and metallic ions, which have emerged as excellent drug delivery agents for the treatment of cancer and other diseases. Currently, MOF studies are mainly focused on intravenous administration, while studies dedicated to oral administration are relatively scarce. In this study, five MOFs, namely UiO-66, UiO-66-NH₂, UiO-66-COOH, UiO-67 and Zr-NDC, were synthesized, of which Zr-NDC had the largest drug loading capacity for 5-FU. Next, a chitosan (CS) modified Zr-NDC was developed to provide a strong impetus for the oral administration of 5-FU. In vitro release experiments of fluorescein isothiocyanate (FITC)-labeled chitosan demonstrated that the cumulative release rates of FITC-labeled chitosan in artificial gastric juice and artificial intestinal fluid were about 20% and 90%, respectively. The in vitro drug release profiles showed that under the protection of CS-MOF, the release of 5-FU into an acidic environment was only 20%, but the release in artificial intestinal fluid reached 70%. Pharmacokinetic analysis revealed that the coating of chitosan on the surface of MOFs exerted a controlled drug release effect, and further improved the oral bioavailability of 5-FU. These findings suggest that CS coating can break through the limitation of MOF intolerance to acid. It is expected that CS-MOF@5-FU can serve as a potential drug delivery system for the oral administration of 5-FU.

更新日期：2020-12-22

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