Purpose: The anionic form of the drug mefenamic acid intercalated into the nanocarrier layered double hydroxide (LDH-Mef) was evaluated by anti-inflammatory and antinociceptive assays.
Methods: The LDH-Mef material was characterized by a set of physicochemical techniques, which was supported by Density Functional Theory calculations. The pharmacological effects of LDH-Mef (40 wt% of drug) were evaluated by hemolytic, anti-inflammatory activity and antinociceptive assays.
Results: In vivo assays were conducted for the first time in order to assess the LDH-Mef potential. The hemolytic effects decreased for the intercalated Mef as demonstrated by the higher tolerated hemolytic concentration (1.83 mM) compared to mefenamic acid (MefH), 0.48 mM. Pretreatment of animals with MefH or LDH-Mef reduced carrageenan-, dextran sulfate- and PGE2-induced paw edema. MefH or LDH-Mef also decrease total leucocytes and neutrophil counts of the peritoneal cavity after inflammation induction with carrageenan. In the nociception model, oral pretreatment with LDH-Mef reduced mechanical hypernociception carrageenan-induced after 3-4h and also the number of writhings induced by acetic acid.
Conclusions: This work shows the increase of the anti-inflammatory and antinociceptive potential of the drug confined into the LDH, as well as, its hemolytic effect.
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Article Synopsis
- - Mefenamic acid, a non-steroidal anti-inflammatory drug, can both enhance and inhibit cardiac ion currents formed by KCNQ1 and KCNE1 channels, revealing its dual effect on these channels, especially in patients with long and short QT syndromes.
- - The study used whole cell patch clamp techniques and molecular dynamics simulations to investigate how mefenamic acid interacts with these channels, particularly noting its inhibition at high concentrations and its potential to preserve some current potentiation effects.
- - Findings emphasize the importance of specific structural regions in the KCNQ1/KCNE1 channels that influence how drugs like mefenamic acid affect ion current, which has significant implications for developing treatments for certain genetic long QT syndrome mutations.*
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