Ion-exchange fibers and drugs: an equilibrium study.

The purpose of this study was to investigate the mechanisms of drug binding into and drug release from cation-exchange fibers in vitro under equilibrium conditions. Ion-exchange groups of the fibers were weakly drug binding carboxylic acid groups (-COOH), strongly drug binding sulphonic acid groups (-SO(3)H), or combinations thereof. Parameters determining the drug absorption and drug release properties of the fibers were: (i) the lipophilicity of the drug (tacrine and propranolol are lipophilic compounds, nadolol is a relatively hydrophilic molecule), (ii) the ion-exchange capacity of the fibers, which was increased by activating the cation-exchange groups with NaOH, (iii) the ionic strength of the extracting salt (NaCl), which was studied in a range of 1.5 mM to 1.5 M, and finally (iv) the effect of divalent calcium ions (CaCl(2)) on the release of the model drugs, which was tested and compared to monovalent sodium ions (NaCl), and combinations thereof. It was found that the lipophilic drugs, tacrine and propranolol, were retained in the fibers more strongly and for longer than the more hydrophilic nadolol. The more hydrophilic nadolol was released to a greater extent from the fibers containing strong ion-exchange groups (-SO(3)H), whereas the lipophilic drugs were attached more strongly to strong ion-exchange groups and released more easily from the weak (-COOH) ion-exchange groups. The salt concentration and the choice of the salt also had an effect: at lower NaCl concentrations more drug was released as a result of the influence of both electrostatic and volume effects (equimolar drug:salt ratio). Incorporation of CaCl(2) in the bathing solution increased drug release considerably as compared to NaCl alone. The equilibrium distribution of the drug species between the fiber and external solution phases was also simulated and it was found that the theoretical modelling proposed describes adequately the basic trends of the behavior of these systems.

Controlled transdermal iontophoresis by ion-exchange fiber.

The objective of this study was to assess the transdermal delivery of drugs using iontophoresis with cation- and anion-exchange fibers as controlled drug delivery vehicles. Complexation of charged model drugs with the ion-exchange fibers was studied as a method to achieve controlled transdermal drug delivery. Drug release from the cation-exchange fiber into a physiological saline was dependent on the lipophilicity of the drug. The release rates of lipophilic tacrine and propranolol were significantly slower than that of hydrophilic nadolol. Permeation of tacrine across the skin was directly related to the iontophoretic current density and drug concentration used. Anion-exchange fiber was tested with anionic sodium salicylate. The iontophoretic flux enhancement of sodium salicylate from the fiber was substantial. As the drug has to be released from the ion-exchange fiber before permeating across the skin, a clear reduction in the drug fluxes from the cationic and anionic fibers were observed compared to the respective fluxes of the drugs in solution. Overall, the ion-exchange fibers act as a drug reservoir, controlling the release and iontophoretic transdermal delivery of the drug.