离子levothyroxine配方:合成,生物可用性和细胞毒性研究
António Barreira1, Andreia F M Santos1, Madalena Dionísio1
1LAQV-REQUIMTE, Department of Chemistry, NOVA School of Science and Technology, NOVA University of Lisbon, Campus de Caparica, 2829-516 Caparica, Portugal.
International journal of molecular sciences
|May 27, 2023
概括
研究人员合成了基于levothyroxine (T4) 的新型离子液体 (IL),以提高药物的溶解性. T4-ILs证明了提高溶解度和生物可用性,为甲状腺功能低下症治疗提供了一个有前途的替代方案.
科学领域:
- 制药化学 制药化学 制药化学
- 材料科学 材料科学 材料科学
- 内分泌学 在内分泌学.
背景情况:
- 甲状腺疾病,特别是甲状腺功能低下,很普遍,需要有效的治疗.
- 利沃甲状腺素 (T4) 是甲状腺功能低下症的标准治疗方法,但面临着溶解性挑战.
- 离子液体 (ILs) 具有改善药物性能的潜力.
研究的目的:
- 合成含有levothyroxine (T4) 的新型离子液体,以提高其可溶性.
- 描述合成的基于T4的离子液体 (T4-ILs).
- 评估T4-ILs的可溶性,透性和细胞毒性.
主要方法:
- 合成T4-ILs通过结合利沃西 ([Na][T4]) 与胆[Ch]+和1-(2-基乙烯) -3-甲基利米达[C2OHMiM]+.
- 使用NMR,ATR-FTIR,元素分析和差分扫描热量计 (DSC) 的表征.
- 在血清,水和PBS中的溶解性研究;透性测定;以及对L929细胞的细胞毒性评估.
主要成果:
- 成功合成和表征T4-ILs,证实它们的化学结构和热特性.
- 与[Na][T4]相比,T4-ILs在血清,水和PBS中的溶解度显著提高.
- 对T4-ILs没有观察到显著的细胞毒性,[C2OHMiM][T4]显示有希望的透性.
结论:
- 利沃西 (T4) 的离子液体配方有效地提高了药物的溶解性和生物可用性.
- 合成的[C2OHMiM][T4]离子液体代表了潜在的优越替代商业甲酸盐.
- 这种方法对开发改善的药物输送系统来治疗甲状腺功能低下症有希望.
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