Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Kraków, Poland.
Molecules. 2020 Jul 31;25(15):3501. doi: 10.3390/molecules25153501.
The present studies were conducted to show the potential of 2D zeolites as effective and non-toxic carriers of drugs. Layered zeolites exhibit adjustable interlayer porosity which can be exploited for controlled drug delivery allowing detailed investigation of the drug release because the structure of the carrier is known exactly. This study was conducted with model drugs ciprofloxacin and piracetam, and ZSM-55 with ca 1 nm thick layers, in detemplated and pillared forms. The release profiles differed from the commercial, crystalline forms of drugs-the release rate increased for ciprofloxacin and decreased for piracetam. To understand the dissolution mechanisms the release data were fitted to Korsmeyer-Peppas equation, showing Fickian (for pillared) and anomalous (for detemplated sample) transport. FT-IR studies showed that strong interaction carrier-drug may be responsible for the modified, slowed down release of piracetam while better solubility and faster release of ciprofloxacin was attributed to formation of the protonated form resulting in weaker interaction with the zeolite than in the pure crystalline form. Two independent tests on L929 mice fibroblasts (ToxiLight and PrestoBlue) showed that ZSM-55, in moderate concentrations may be safely used as a carrier of drug molecules, not having negative effect on the cells viability or proliferation rate.
本研究旨在展示二维沸石作为有效且无毒的药物载体的潜力。层状沸石具有可调节的层间孔隙度，可用于控制药物释放，从而可以详细研究药物释放情况，因为载体的结构完全已知。这项研究使用模型药物环丙沙星和吡拉西坦以及具有约 1nm 厚层的 ZSM-55 进行，采用脱模板和支柱化形式。释放曲线与药物的商业结晶形式不同-环丙沙星的释放速率增加，吡拉西坦的释放速率降低。为了理解溶解机制，将释放数据拟合到 Korsmeyer-Peppas 方程中，表明存在菲克型（对于支柱化）和异常型（对于脱模板样品）传输。FT-IR 研究表明，载体-药物之间的强相互作用可能是导致吡拉西坦释放速度减慢的原因，而环丙沙星的溶解度更高且释放速度更快，则归因于质子化形式的形成，这导致与沸石的相互作用比在纯结晶形式中弱。对 L929 小鼠成纤维细胞（ToxiLight 和 PrestoBlue）进行的两项独立测试表明，ZSM-55 在适度浓度下可安全用作药物分子的载体，对细胞活力或增殖率没有负面影响。
