Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis |
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Authors: | Gursharanjit Singh Bijaya Ghosh Dave Kaushalkumar Vanita Somsekhar |
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Institution: | (1) Research associate, Formulation and Development, Cadila Pharmaceuticals Ltd., Ahmedabad, India;(2) Department of Pharmaceutical Technology, K.L.E Society’s College of Pharmacy, IInd Block, Rajajinagar, Bangalore, 560010, Karnataka, India |
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Abstract: | 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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Keywords: | iontophoresis menthol peppermint oil transdermal venlafaxine hydrochloride |
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