Abstract
In view of the variable oral absorption, short biological half-life and extensive first pass metabolism of the pineal hormone melatonin, an investigation of its solubilization profile in modified aqueous media is described. Four readily available surfactants were examined with respect to their ability to enhance the solubility of melatonin under simulated physiological conditions. The most effective surfactant was found to be the sodium salt of dioctyl sulfosuccinate (DSS), which augmented the aqueous solubility of the hormone by 23%. This is attributed to a favourable stereoelectronic interaction between DSS and the nucleus of melatonin, which seems to be independent of the pH of the dissolution medium. A noteworthy synergistic effect in the aqueous solubilization of the hormone occurs when a 1:2 DSS-sodium dodecyl sulphate mixture is used.
Keywords: Melatonin, Solubilization, Surfactants, Gastrointestinal pH
Current Drug Delivery
Title: Pineal Hormone Melatonin: Solubilization Studies in Model Aqueous Gastrointestinal Environments
Volume: 3 Issue: 3
Author(s): Marilena Vlachou, Aphrodite Eikosipentaki and Vassilios Xenogiorgis
Affiliation:
Keywords: Melatonin, Solubilization, Surfactants, Gastrointestinal pH
Abstract: In view of the variable oral absorption, short biological half-life and extensive first pass metabolism of the pineal hormone melatonin, an investigation of its solubilization profile in modified aqueous media is described. Four readily available surfactants were examined with respect to their ability to enhance the solubility of melatonin under simulated physiological conditions. The most effective surfactant was found to be the sodium salt of dioctyl sulfosuccinate (DSS), which augmented the aqueous solubility of the hormone by 23%. This is attributed to a favourable stereoelectronic interaction between DSS and the nucleus of melatonin, which seems to be independent of the pH of the dissolution medium. A noteworthy synergistic effect in the aqueous solubilization of the hormone occurs when a 1:2 DSS-sodium dodecyl sulphate mixture is used.
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Cite this article as:
Vlachou Marilena, Eikosipentaki Aphrodite and Xenogiorgis Vassilios, Pineal Hormone Melatonin: Solubilization Studies in Model Aqueous Gastrointestinal Environments, Current Drug Delivery 2006; 3 (3) . https://dx.doi.org/10.2174/156720106777731073
DOI https://dx.doi.org/10.2174/156720106777731073 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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