Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis

Abstract

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/cm 2 . 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 steadystate 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/cm 2 /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.

5-Fluorouracil Nanoparticles Inhibit Hepatocellular Carcinoma via Activation of the p53 Pathway in the Orthotopic Transplant Mouse Model

“…Nanoparticles have been shown to be delivered to specific sites by size-dependant passive targeting [13] , [14] . Passive delivery occurs when nanoparticles are transported through leaky tumor capillary fenestrations into the tumor cells by diffusion or convection [15] . Active targeting involves the coupling the target-specific molecules, such as ligands, binding sites, or antibodies, to the surface of the nanoparticles to assist drug distribution to specific target tissues [16] .…”

Application of mathematical modelling to alginate chitosan polyelectrolyte complexes for the prediction of system behavior with Venlafaxine HCl as a model charged drug

“…This can be explained by a higher affinity between the positively charged drug and this negatively charged nanoparticles (zeta potential −55 mv). pKa value of venlafaxine HCl was found to be 9.6, which indicated that the drug was completely ionized at pH 7.4 ( Singh et al 2008 ). The release rate was not different between the prepared formulae.…”

Characterization of seven psychoactive pharmaceuticals as N‐nitrosodimethylamine precursors during free chlorine and chlorine dioxide chlorination processes

“…During the Table 1. Chemical structure and pKa of the selected seven drugs [21][22][23][24][25][26][27] wileyonlinelibrary.com/jctb course of the experiments, samples were collected at predefined time points and quenched by the addition of 1 mL ascorbic acid solution (10 mmol L -1 ). Samples were filtered through 0.45 μm nylon filers for NDMA analysis.…”

“…In the present study, seven widely used psychoactive drugs were selected containing a DMA functional group and detected in wastewater at concentrations from ng L −1 to µg L −1 . Their names and chemical structures are summarized in Table . The NDMA formation potentials of these psychoactive drugs were assessed during free chlorine (NaOCl) and chlorine dioxide (ClO 2 ) disinfection processes.…”

“…2,4,[18][19][20] Their names and chemical structures are summarized in Table 1. [21][22][23][24][25][26][27] The NDMA formation potentials of these psychoactive drugs were assessed during free chlorine (NaOCl) and chlorine dioxide (ClO 2 ) disinfection processes. The influence of several parameters (i.e.…”