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Memantine-Derived Schiff Bases as Transdermal Prodrug Candidates by Ana P. Araujo de Oliveira; Victoria C. Romero Colmenares; Renata Diniz; Jennifer T. J. Freitas; Clara M. da Cruz; Eduardo B. Lages; Lucas A. M. Ferreira; Rafael P. Vieira; Heloisa Beraldo is a Engineering article available to read on EtoBox.

What is Memantine-Derived Schiff Bases as Transdermal Prodrug Candidates about?

Condensation reactions of salicylaldehyde, 2-pyridinecarboxaldehyde, and pyridoxaldehyde with memantine (**Me**) produced novel memantine-derived Schiff bases (**1**–**3**). Speciation predictions and calculations of Log P, Log D, and of the percentage (%) of neutral species for (**1**–**3**) were carried out. In comparison with **Me**, the Schiff bases presented increased log P and log D in all cases and pH values, suggesting higher hydrophobicity. The determined solubilities in __n__-octanol were 34.7 mg/mL for memantine hydrochloride and 67.3 mg/mL for (**3**). According to the molecular weights and calculated logP, compounds (**1**–**3**) are suitable for transdermal administration, especially compound (**3**). In addition, hydrolysis of **3** with the release of pyridoxal, a daily cofactor in human metabolism, was observed. The results suggested that **3** is the most promising compound and that formation of the pyridoxal Schiff base with **Me** might be an effective strategy to obtain a prodrug candidate with increased lipophilicity, which would be able to passively cross biological barriers during transdermal delivery and might have applications in the treatment of Alzheimer

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Author

Ana P. Araujo de Oliveira; Victoria C. Romero Colmenares; Renata Diniz; Jennifer T. J. Freitas; Clara M. da Cruz; Eduardo B. Lages; Lucas A. M. Ferreira; Rafael P. Vieira; Heloisa Beraldo

Publisher

American Chemical Society

Published

2022

Language

EN

Field

Engineering (Physical Sciences)