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The sleep cycle, an integral part of human health, consists of several stages with distinct characteristics and functions. It begins with a transition from wakefulness to sleep, known as the light sleep phase, followed by the restorative deep sleep phase, essential for physical recovery and growth. The cycle concludes with the Rapid Eye Movement (REM) phase, characterized by high brain activity and vivid dreaming. Insomnia, a prevalent sleep disorder, involves difficulty falling asleep, staying...
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Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
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Melatonin/Cyclodextrin Inclusion Complexes: A Review.

Aikaterini Sakellaropoulou1, Angeliki Siamidi2, Marilena Vlachou2

  • 1Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece.

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Melatonin (MLT) solubility and absorption are improved by cyclodextrin (CD) complexation. This review highlights key findings on MLT/CD complexes, showing enhanced drug uptake for therapeutic applications.

Keywords:
cyclodextrinsinclusion complexesmelatonin

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Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Supramolecular Chemistry

Background:

  • Melatonin (MLT) is a hormone with diverse physiological roles, including sleep regulation and antioxidant effects.
  • MLT is implicated in various conditions such as seasonal affective disorder (SAD), neurological disorders, and cancers.
  • Poor water solubility of MLT limits its bioavailability and therapeutic efficacy.

Purpose of the Study:

  • To review and consolidate key findings on the complexation of melatonin with cyclodextrins (CDs).
  • To evaluate the impact of CD complexation on MLT's physicochemical properties and in vivo performance.

Main Methods:

  • Literature appraisal of studies investigating MLT/CD complexes.
  • Analysis of characterization techniques including NMR, FT-IR, XRD, and DCS.
  • Review of in vivo experimental data on MLT/CD complex uptake.

Main Results:

  • MLT forms predominantly 1:1 inclusion complexes with various CDs.
  • Complexation significantly enhances the aqueous solubility of melatonin.
  • Characterization techniques confirm the formation and interaction within MLT/CD complexes.
  • In vivo studies demonstrate increased MLT uptake when complexed with CDs.

Conclusions:

  • Cyclodextrin complexation is an effective strategy to improve melatonin's solubility and bioavailability.
  • MLT/CD complexes show promise for enhanced therapeutic delivery of melatonin.
  • Further research into MLT/CD complexes can optimize drug delivery for various medical conditions.