Characterízatíon and pharmacologícal actívíty of zínc(Il)-díclofenac and zínc(Il)-díclofenac-hydroxypropylbeta-cyclodextrín ínclusíon complex
Keywords:
Non-steroidal anti inflammatory, Diclofenac, Cyclodextrins, Metal complex, lnclusion complexAbstract
This study aimed to present the synthesis, the physical!chemical characterization and the pharmacologica/ evaluation of the metal comp!ex zinc(/1)-diclofenac and its inc!usion in hydroxypropy/-/3-cyclodextrin, with both of these being compared to potassium-diclofenac. The metal complex zinc(ll)-diclofenac was synthesized via the direct mixture of aqueous solutions of zinc(ll)-su/fate and potassium diclofenac (molar ratio 1:2) and was subsequently included in hydroxypropyl-/3- cyclodextrin (molar ratio 1:1). The triais to determine solubility and melting point showed changes characteristic of the complexation of the drug with meta/fie ians. On the other hand, the interaction with cyclodextrins was determined by morphologica/ changes in the drug crystals and the enhanced zinc(ll)-diclofenac aqueous so/ubility, after inclusion in the hydroxypropyl-/3-cyclodextrin hydrophobic cavity (association constant Ks=623. 6 M'). Pharmaco!ogical eva/uation showed that treatment with zinc(ll)-diclofenac or zinc(ll)-diclofenac-hydroxypropy/-/3- cyclodextrin brought a significant reduction in the volume of abdominal writhing and u/cers, when compared to potassium-diclofenac (p<0.001), enhancing the anti-inflammatory activity and reducing the adverse effects.
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