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Current Pharmaceutical Design

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ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

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Research Article

In vitro Modified Release Studies on Melatoninergic Fluorinated Phenylalkylamides: Circumventing their Lipophilicity for Oral Administration

Author(s): Marilena Vlachou*, Angeliki Siamidi, Chrystalla Protopapa, Michalis Vlachos, Sophia Kloutsou, Chrysoula-Christina Dreliozi and Ioannis P. Papanastasiou

Volume 30, Issue 18, 2024

Published on: 09 April, 2024

Page: [1433 - 1441] Pages: 9

DOI: 10.2174/0113816128304967240328065809

Price: $65

Abstract

Introduction: In an attempt to circumvent the lipophilicity burden for the oral administration of new potent synthetic melatoninergic fluorine-substituted methoxyphenylalkyl amides, we conducted in vitro modified release studies using carefully selected matrix tablets’ biopolymeric materials in different ratios.

Methods: In particular, we sought to attain release profiles of these analogues similar to that of the parent compound, the chronobiotic hormone Melatonin (MLT), and also of the commercially available drug, Circadin®.

Results: It was found that some of these systems, albeit being more lipophilic than MLT, mimic the in vitro release patterns of melatonin and Circadin®.

Conclusion: Moreover, a number of these derivatives were proven suitable for dealing with sleep onset problems, whilst others for dealing with combined sleep onset/sleep maintenance dysfunctions.

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