Iontophoresis of dexamethasone phosphate: competition with chloride ions.

Iontophoresis of dexamethasone phosphate: competition with chloride ions.
复制标题

磷酸地塞米松的离子电渗疗法:与氯离子的竞争。

DOI:
10.1016/j.jconrel.2008.07.002
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发表时间:
2008
期刊:
Journal of controlled release : official journal of the Controlled Release Society
影响因子:
--
通讯作者:
Guy,RH
Guy,RH
中科院分区:
--
文献类型:
--
作者:
Sylvestre,J-P;Díaz-Marín,C;Delgado-Charro,MB;Guy,RH

文献摘要

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The objective was to study the competition of chloride released from a Ag/AgCl cathode on the iontophoretic delivery of dexamethasone phosphate (Dex-Phos). Iontophoresis of Dex-Phos was performed in side-by-side diffusion cells (0.78 cm2) using pig skin. A 0.3 mA constant current was applied via Ag/AgCl electrodes. The amounts of Dex-Phos and dexamethasone (Dex) were also quantified in the stratum corneum (SC), using tape-stripping, after passive and iontophoretic delivery. The profiles of Dex-Phos and Dex, as a function of position in the SC, were deduced. The iontophoretic delivery of Dex-Phos from pure water was unaffected by the accumulation of Cl−released by the donor cathode when the drug's concentration was 4.25 mM to 17 mM. At 0.85 mM, however, Cl−competition was significant and the drug flux was significantly reduced. Formulation of the drug in the presence of Cl−resulted in a non-linear dependence of flux on the molar fraction of the drug. Tape-stripping experiments confirmed the enhanced delivery of Dex-Phos by iontophoresis relative to passive diffusion, with Dex-Phos concentration greater inside the barrier post-iontophoresis than that in the donor. The latter observation could explain the robustness of Dex-Phos delivery to the presence of Cl−in the donor solution.