The objective of the study was to investigate in vitro transdermal delivery of venlafaxine hydrochloride across the pigskin by passive diffusion and iontophoresis. For passive diffusion, experiments were carried out in Franz diffusion cell whereas for iontophoretic permeation, the diffusion cell was modified to contain both the donor and return electrode on the same side of skin. Anodal iontophoresis was carried out using a current density of 0.5 mA/cm2. Donor concentrations used were 585.5 mg/ml (saturated solution) and 100 mg/ml. Experiments initially performed to determine the transport efficiency of venlafaxine ions showed promising results. Iontophoresis increased the permeation rate at both concentration levels over their passive counterparts (P < 0.01), but surprisingly higher steady-state flux was obtained from lower donor drug load (P < 0.01). The favorable pH of the unsaturated solutions is suggested to be the cause for this effect. Mild synergistic effect was observed when iontophoresis was carried out incorporating peppermint oil in the donor but the same was not found in passive diffusion. Highest steady-state flux obtained in the experiment was 3.279 μmol/cm2/h when peppermint oil (0.1%) was included in the donor. As the maintenance requirement of venlafaxine hydrochloride is approximately 9.956 μmol/h, the results suggested that the drug is a promising candidate for iontophoretic delivery.
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机译：该研究的目的是通过被动扩散和离子电渗疗法研究盐酸文拉法辛跨猪皮的体外透皮递送。对于被动扩散，在Franz扩散池中进行了实验，而对于离子电渗渗透，则对扩散池进行了修改，使其在皮肤的同一侧同时包含供体电极和返回电极。阳极离子电渗疗法使用的电流密度为0.5mA / cm 2 。供体使用的浓度为585.5 mg / ml（饱和溶液）和100 mg / ml。最初进行的确定文拉法辛离子传输效率的实验显示出令人鼓舞的结果。离子电渗疗法在两个浓度水平上均比其被动对应物增加了渗透率（P <0.01），但是出人意料的是，较低的供体载药量获得了更高的稳态通量（P <0.01）。建议不饱和溶液的有利pH值是造成这种效果的原因。当在供体中加入薄荷油进行离子电渗疗法时，观察到轻微的协同作用，但在被动扩散中未发现相同的效果。当供体中包括薄荷油（0.1％）时，实验中获得的最高稳态通量为3.279μmol/ cm 2 / h。由于盐酸文拉法辛的维护需求约为9.956μmol/ h，因此结果表明该药物是离子电渗疗法的有希望的候选者。
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