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Int J Mol Sci. 2017 Jul 28;18(8). pii: E1641. doi: 10.3390/ijms18081641.

Comparative In Vitro Controlled Release Studies on the Chronobiotic Hormone Melatonin from Cyclodextrins-Containing Matrices and Cyclodextrin: Melatonin Complexes.

Author information

1
School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Technology, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece. vlachou@pharm.uoa.gr.
2
School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Technology, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece. mpapami1983@gmail.com.
3
School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Technology, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece. asiamidi@pharm.uoa.gr.
4
School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Technology, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece. esfragouli@gmail.com.
5
School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece. pafroudakischem@yahoo.gr.
6
School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece. Kompogennitaki@hotmail.com.
7
School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece. idotsik@pharm.uoa.gr.

Abstract

A series of hydrophilic matrix tablets was prepared and tested with respect to their ability to release the hormone melatonin in a controlled manner, in order to alleviate sleep onset and sleep maintenance dysfunctions. Besides the active ingredient, the tablets were comprised of combinations of the following: HPMC K 15M, low viscosity sodium alginate, microcrystalline cellulose (Avicel PH 102), magnesium stearate, and the cyclodextrins, α-CD, β-CD, γ-CD, HP-β-CD, sulfated β-CD, HP-α-CD and HP-γ-CD, and MLT (guest):CD (host) complexes of the above cyclodextrins, in 1:1 ratio. The controlled release studies were conducted in two aqueous dissolution media at pH 1.2 and 7.4. The stoichiometry of the formed complexes was examined by applying the continuous variation method (Job plot), while the stability constants were calculated by monitoring the spectrophotometric properties of free and CD-encapsulated melatonin (UV-Vis). Host-guest interactions were studied by Nuclear Magnetic Resonance (NMR) spectroscopy. The dissolution data suggest that melatonin is released faster from the MLT:CD complexes than from the rest matrix systems. This enhancement in the dissolution rate and the % release of melatonin from the complexes is due to the increased solubility of the MLT:CD complexes.

KEYWORDS:

NMR studies; cyclodextrins; in vitro controlled release; melatonin

PMID:
28788064
PMCID:
PMC5578031
DOI:
10.3390/ijms18081641
[Indexed for MEDLINE]
Free PMC Article

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