Melatonin/Cyclodextrin Inclusion Complexes: A Review

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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. 

The tendency toward usage of β-CD analogues is probably due to the fact that the size of the cavity in these CDs is ideal for hosting MLT. Studies conducted with other CDs proved that for the purpose of hosting MLT, α-CD had a relatively small cavity, whereas that of γ-CD was considerably larger.

Sakellaropoulou, A.; Siamidi, A.; Vlachou, M. Melatonin/Cyclodextrin Inclusion Complexes: A Review. Molecules 2022, 27, 445. https://doi.org/10.3390/molecules27020445

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