ABSTRACT

A simple and cost-effective synthesis method for zeolitic imidazolate framework-8 (ZIF-8) was developed and loaded with metformin (MET@ZIF-8) for pH sensitive-release behaviour for the treatment of lung cancer. ZIF-8 and MET@ZIF-8 were subjected to particle size, zeta potential analysis and HR-TEM through which it shows evidence that the particles had spherical morphology and nanosize. Percentage of metformin (MET) loading in the ZIF-8 was found to be 63.39 ± 1.32%. Dissociation of ZIF-8 into its coordination ions at acidic conditions (pH 5–6) thereby leads to the release of MET at a higher drug release rate (98%) compared to physiological conditions (pH 7.4) the drug release rate at 35%. Pore volume and pore size of ZIF-8 (1242 m²/g) gets reduced to 1042.00 m²/g after incorporation of MET in ZIF-8. In-vitro cytotoxicity assay results showed the enhanced cytotoxicity for MET @ZIF-8 compared to free MET in a dose dependent manner in human lung adenocarcinoma cells A549.

摘要

开发了一种简单且具有成本效益的沸石咪唑酯骨架 8 (ZIF-8) 合成方法，并负载二甲双胍 (MET@ZIF-8)，用于治疗肺癌的 pH 敏感释放行为。对 ZIF-8 和 MET@ZIF-8 进行粒度、zeta 电位分析和 HR-TEM 分析，结果表明颗粒具有球形形态和纳米尺寸。发现 ZIF-8 中二甲双胍 (MET) 负载的百分比为 63.39 ± 1.32%。ZIF-8 在酸性条件（pH 5-6）下解离成其配位离子，从而导致 MET 以更高的药物释放率（98%）释放，而生理条件下（pH 7.4）的药物释放率为 35% . ^{ZIF-8 (1242 m 2} /g) 的孔容和孔径减小到 1042.00 m ²/g 在 MET 并入 ZIF-8 后。体外细胞毒性测定结果显示，与游离 MET 相比，MET @ZIF-8 在人肺腺癌细胞 A549 中以剂量依赖性方式增强了细胞毒性。