Physicochemical and structure-activity properties of piroxicam—a mini review

Abstract

The neutral bidentate ligand coordinated to the metal ion through pyridyl-N and carbonyl of the amide moiety causes protonation/deprotonation equilibria (tautomerism) of piroxicam. The penetration of piroxicam through blood–brain barrier (BBB) may be by redox chemical delivery system linking it to the lipophilic dihydropyridine carrier creating a complex with carboxylic acid that transverses the BBB. The complex is enzymatically oxidized to the conic pyridinium salt. Subsequent cleavage of the drug from the pyridinium carrier leads to sustained drug delivery in the brain parenchyma. Brain uptake of piroxicam may be positively correlated with lipid solubility at high doses or negatively correlated with hydrogen bonding or due to damage to meninges.

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