Energetically favorable interactions between diclofenac sodium and cyclodextrin molecules in aqueous media

Potential interaction between zinc ions and a cyclodextrin-based diclofenac formulation

“…A likely explanation would be that the enhanced dissociation of DF improved the solubility of the chelate complex itself. Addition of cyclodextrin, in the absence of zinc ions, resulted in a linear increase in equilibrium solubility of DF-Na with an estimated binding constants in the range 117-574 M À1 , which goes in line with the reported generally low, and variable binding constants of DF to cyclodextrins 3,13,14,17 . Even in the presence of zinc ions, which decreased the solubility of DF-Na five folds at pH 4.5, addition of HPbCD improved the equilibrium solubility of DF-Na, yet with a higher binding constant.…”

“…Comparing the profiles of DF-Na and its HPbCD complex in the absence of zinc, the mean values of AUC (0-1) and Cp/AUC (0-1) of free DF-Na were higher, than those obtained from DF-HPbCD, but not to a statistically significant level, indicating that inclusion complexation to HPbCD did not improve the rate or extent of DF-Na absorption (p40.05). In spite of many literature reports that studied the binding of diclofenac to cyclodextrins, with some of them demonstrating potential enhancement of solubility through inclusion complex formation 3,7,13 , no studies (to the best of our knowledge) have been reported demonstrating the in vivo effect of cyclodextrin complexes which would reflect the oral bioavailability of the drug. Using silicone membranes, it has been demonstrated that cyclodextrins enhanced the flux of diclofenac through the artificial membrane in vitro 6 .…”

“…The use of cyclodextrins as solubilizers that improve dissolution, consequently bioavailability and onset of action, is a particularly attractive approach [6][7][8][9][10] . Several previous studies have discussed the inclusion complexes of DF and DF-Na with cyclodextrins 3,6,7,[11][12][13][14][15][16][17] , which were found to improve the in vitro dissolution of diclofenac. However, to the best of our knowledge, there have been no studies that assessed the in vivo bioavailability of DF from its cyclodextrin complexes.…”

Cyclodextrin-functionalized polyethylene and polypropylene as biocompatible materials for diclofenac delivery

“…The incidence of having pendant CDs on the wettability, the thermal stability and the friction coefficient of the novel materials, as well as on the biocompatibility and the performance as carriers of diclofenac was evaluated in detail. Diclofenac is a widely used non-steroidal antinflammatory drug (NSAID) that can form inclusion complexes with CDs (Dias et al, 2003;Mehta et al, 2008). Thus, a high local proportion of CDs can create a favorable microenvironment for the uptake of the drug and for sustaining its release.…”

A Comparative Study of Molecular Interactions of Three Tetracycline Derivatives with Aqueous β-Cyclodextrin Solution at Different Temperatures

“…4) for all three tetracycline derivatives at 298 K, it is seen that in the presence of β-CD, the system shows lower conductivity values as compared to pure drug/water system. This can be accounted by the fact that the mobility of associated drug is comparatively less than that of free drug which points towards the interaction of drug molecule with cyclodextrin moiety [14]. The energetics of these interactions is estimated in terms of change in free energy according to the following equation [15].…”