Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece.
Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, 15784 Athens, Greece.
Molecules. 2022 Jan 10;27(2):445. doi: 10.3390/molecules27020445.
Melatonin (MLT) is involved in many functions of the human body, mainly in sleeping-related disorders. It also has anti-oxidant potential and has been proven very effective in the treatment of seasonal affective disorders (SAD), which afflict some people during short winter days. Melatonin has been implicated in a range of other conditions, including Parkinson's disease, Alzheimer's and other neurological conditions, and in certain cancers. Its poor solubility in water leads to an insufficient absorption that led scientists to investigate MLT inclusion in cyclodextrins (CDs), as inclusion of drugs in CDs is a way of increasing the solubility of many lipophilic moieties with poor water solubility. The aim of this review is to gather all the key findings on MLT/CD complexes. The literature appraisal concluded that MLT inclusion leads to a 1:1 complex with the majority of CDs and increases the solubility of the hormone. The interactions of MLT with CDs can be studied by a variety of techniques, such as NMR, FT-IR, XRD and DCS. More importantly, the in vivo experiments showed an increase in the uptake of MLT when included in a CD.
褪黑素（MLT）参与人体的许多功能，主要与睡眠相关的疾病有关。它还具有抗氧化潜力，已被证明对治疗季节性情感障碍（SAD）非常有效，这种疾病在冬季白天较短时会影响一些人。褪黑素还与其他一些疾病有关，包括帕金森病、阿尔茨海默病和其他神经疾病，以及某些癌症。它在水中的溶解度差导致吸收不足，这促使科学家研究将 MLT 纳入环糊精（CDs）中，因为将药物纳入 CDs 是增加许多疏水性较差的亲脂性部分的溶解度的一种方法。本综述的目的是收集所有关于 MLT/CD 配合物的关键发现。文献评估得出结论，MLT 与大多数 CDs 形成 1:1 配合物，并提高激素的溶解度。可以通过各种技术，如 NMR、FT-IR、XRD 和 DCS，来研究 MLT 与 CDs 的相互作用。更重要的是，体内实验表明，当 MLT 被包含在 CD 中时，它的摄取量会增加。
