Faculty of Biological Science and Technology, Institute of Science and Engineering, Kanazawa University, Kakuma-machi, Kanazawa, 920-1192, Japan.
Division of Tumor Cell Biology and Bioimaging, Cancer Research Institute of Kanazawa University, Kakuma-machi, Kanazawa, 920-1192, Japan.
Sci Rep. 2021 May 7;11(1):9770. doi: 10.1038/s41598-021-89144-0.
Trimethylglycine (TMG) is a cheap, natural, and highly biocompatible compound. Therefore, it has been used in the fields of food and life sciences, but the application of solid TMG is limited to utilisation as an "additive". In the present study, we focussed on the high solubility of TMG in water, derived from the aprotic zwitterionic structure, and proposed TMG as the chemical accounting for a major portion of the aqueous solution (e.g., 50 wt%). High loading of TMG shifted the properties of water and enabled the dissolution of poorly water-soluble cisplatin, an anticancer agent, at high concentration (solubility of cisplatin: 0.15 wt% in water vs 1.7 wt% in TMG aqueous solution). For hepatic arterial infusion, this can reduce the amount of cisplatin administered from 40 to 4 mL. It enables simple injection using a syringe, without the need for catheters and automatic pumps, leading to critical alleviation of the risk to patients. Furthermore, we produced a dry powder from a cisplatin-containing TMG aqueous solution via freeze-drying. Powders can be conveniently stored and transported. Furthermore, cisplatin is often used as a mixture with other drugs, and cisplatin aqueous solutions are not preferred as they dilute the other drugs.
三甲基甘氨酸（TMG）是一种廉价、天然且高度生物相容的化合物。因此，它已被应用于食品和生命科学领域，但固态 TMG 的应用仅限于作为“添加剂”。在本研究中，我们关注 TMG 在水中的高溶解度，这源于非质子两性离子结构，并提出 TMG 是构成大部分水溶液（例如 50wt%）的主要成分。高浓度 TMG 负载会改变水的性质，使水中难溶的顺铂（一种抗癌药物）能够高浓度溶解（顺铂在水中的溶解度为 0.15wt%，而在 TMG 水溶液中的溶解度为 1.7wt%）。对于肝动脉灌注，这可以将给药量从 40 毫升减少到 4 毫升。它可以通过注射器进行简单注射，无需使用导管和自动泵，从而极大地降低了患者的风险。此外，我们通过冷冻干燥从含有顺铂的 TMG 水溶液中制备了干燥粉末。粉末便于储存和运输。此外，顺铂通常与其他药物混合使用，而不优选使用顺铂水溶液，因为它们会稀释其他药物。
