Skin permeation of gemcitabine hydrochloride by passive diffusion, iontophoresis and sonophoresis: In vitro and in vivo evaluations

Shaik Baji, Aswathi R. Hegde, Mrugank Kulkarni, Sushil Yadaorao Raut, Jyothsna Manikkath, Meka Sreenivasa Reddy, Srinivas Mutalik

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Abstract

The present study was undertaken to assess skin permeation of gemcitabine hydrochloride (GEM) following passive diffusion, iontophoresis and sonophoresis. In vitro passive diffusion were carried out in HEPES solution of pH 4.5, 5.8, 7.4 and 9.2 which revealed a pH-dependent permeation of GEM. Further, cathodic and anodic iontophoresis were carried out and the results indicated that anodic iontophoresis exhibited highest amount of GEM permeated at the end of 6 h (Q6h = 2203.74 ± 128.75 μg/cm2). Subsequently, effect of varying drug concentration on the permeation of GEM with iontophoresis was studied. The results demonstrated that GEM exhibited a concentration-dependent permeation profile with the highest permeation observed at 50 mg/mL (Q6h = 3334.94 ± 133.38 μg/cm2). In sonophoresis, among the different amplitudes tested, highest skin permeation of GEM was observed at 40 W amplitude. Also, effect of sonophoresis on varying drug concentrations revealed that highest permeation of GEM was observed at 50 mg/mL (Q30min = 950.24 ± 38.61 μg/cm2). In vivo permeation studies carried out using passive diffusion, anodic iontophoresis or sonophoresis indicated that anodic iontophoresis of GEM showed a higher plasma concentration (2472.83 ± 90.91 ng/mL) as compared to sonophoresis (2198.27 ± 109.91 ng/mL) and passive diffusion (845.21 ± 52.70 ng/mL). This study illustrates the application of iontophoresis or sonophoresis as a non-invasive drug delivery modality for GEM.

Original languageEnglish
Pages (from-to)49-54
Number of pages6
JournalJournal of Drug Delivery Science and Technology
Volume47
DOIs
Publication statusPublished - 01-10-2018

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gemcitabine
Iontophoresis
Skin
Pharmaceutical Preparations
HEPES
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

@article{749b37f13d2049c8a97ee7c80cbf52bd,
title = "Skin permeation of gemcitabine hydrochloride by passive diffusion, iontophoresis and sonophoresis: In vitro and in vivo evaluations",
abstract = "The present study was undertaken to assess skin permeation of gemcitabine hydrochloride (GEM) following passive diffusion, iontophoresis and sonophoresis. In vitro passive diffusion were carried out in HEPES solution of pH 4.5, 5.8, 7.4 and 9.2 which revealed a pH-dependent permeation of GEM. Further, cathodic and anodic iontophoresis were carried out and the results indicated that anodic iontophoresis exhibited highest amount of GEM permeated at the end of 6 h (Q6h = 2203.74 ± 128.75 μg/cm2). Subsequently, effect of varying drug concentration on the permeation of GEM with iontophoresis was studied. The results demonstrated that GEM exhibited a concentration-dependent permeation profile with the highest permeation observed at 50 mg/mL (Q6h = 3334.94 ± 133.38 μg/cm2). In sonophoresis, among the different amplitudes tested, highest skin permeation of GEM was observed at 40 W amplitude. Also, effect of sonophoresis on varying drug concentrations revealed that highest permeation of GEM was observed at 50 mg/mL (Q30min = 950.24 ± 38.61 μg/cm2). In vivo permeation studies carried out using passive diffusion, anodic iontophoresis or sonophoresis indicated that anodic iontophoresis of GEM showed a higher plasma concentration (2472.83 ± 90.91 ng/mL) as compared to sonophoresis (2198.27 ± 109.91 ng/mL) and passive diffusion (845.21 ± 52.70 ng/mL). This study illustrates the application of iontophoresis or sonophoresis as a non-invasive drug delivery modality for GEM.",
author = "Shaik Baji and Hegde, {Aswathi R.} and Mrugank Kulkarni and Raut, {Sushil Yadaorao} and Jyothsna Manikkath and Reddy, {Meka Sreenivasa} and Srinivas Mutalik",
year = "2018",
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TY - JOUR

T1 - Skin permeation of gemcitabine hydrochloride by passive diffusion, iontophoresis and sonophoresis

T2 - In vitro and in vivo evaluations

AU - Baji, Shaik

AU - Hegde, Aswathi R.

AU - Kulkarni, Mrugank

AU - Raut, Sushil Yadaorao

AU - Manikkath, Jyothsna

AU - Reddy, Meka Sreenivasa

AU - Mutalik, Srinivas

PY - 2018/10/1

Y1 - 2018/10/1

N2 - The present study was undertaken to assess skin permeation of gemcitabine hydrochloride (GEM) following passive diffusion, iontophoresis and sonophoresis. In vitro passive diffusion were carried out in HEPES solution of pH 4.5, 5.8, 7.4 and 9.2 which revealed a pH-dependent permeation of GEM. Further, cathodic and anodic iontophoresis were carried out and the results indicated that anodic iontophoresis exhibited highest amount of GEM permeated at the end of 6 h (Q6h = 2203.74 ± 128.75 μg/cm2). Subsequently, effect of varying drug concentration on the permeation of GEM with iontophoresis was studied. The results demonstrated that GEM exhibited a concentration-dependent permeation profile with the highest permeation observed at 50 mg/mL (Q6h = 3334.94 ± 133.38 μg/cm2). In sonophoresis, among the different amplitudes tested, highest skin permeation of GEM was observed at 40 W amplitude. Also, effect of sonophoresis on varying drug concentrations revealed that highest permeation of GEM was observed at 50 mg/mL (Q30min = 950.24 ± 38.61 μg/cm2). In vivo permeation studies carried out using passive diffusion, anodic iontophoresis or sonophoresis indicated that anodic iontophoresis of GEM showed a higher plasma concentration (2472.83 ± 90.91 ng/mL) as compared to sonophoresis (2198.27 ± 109.91 ng/mL) and passive diffusion (845.21 ± 52.70 ng/mL). This study illustrates the application of iontophoresis or sonophoresis as a non-invasive drug delivery modality for GEM.

AB - The present study was undertaken to assess skin permeation of gemcitabine hydrochloride (GEM) following passive diffusion, iontophoresis and sonophoresis. In vitro passive diffusion were carried out in HEPES solution of pH 4.5, 5.8, 7.4 and 9.2 which revealed a pH-dependent permeation of GEM. Further, cathodic and anodic iontophoresis were carried out and the results indicated that anodic iontophoresis exhibited highest amount of GEM permeated at the end of 6 h (Q6h = 2203.74 ± 128.75 μg/cm2). Subsequently, effect of varying drug concentration on the permeation of GEM with iontophoresis was studied. The results demonstrated that GEM exhibited a concentration-dependent permeation profile with the highest permeation observed at 50 mg/mL (Q6h = 3334.94 ± 133.38 μg/cm2). In sonophoresis, among the different amplitudes tested, highest skin permeation of GEM was observed at 40 W amplitude. Also, effect of sonophoresis on varying drug concentrations revealed that highest permeation of GEM was observed at 50 mg/mL (Q30min = 950.24 ± 38.61 μg/cm2). In vivo permeation studies carried out using passive diffusion, anodic iontophoresis or sonophoresis indicated that anodic iontophoresis of GEM showed a higher plasma concentration (2472.83 ± 90.91 ng/mL) as compared to sonophoresis (2198.27 ± 109.91 ng/mL) and passive diffusion (845.21 ± 52.70 ng/mL). This study illustrates the application of iontophoresis or sonophoresis as a non-invasive drug delivery modality for GEM.

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U2 - 10.1016/j.jddst.2018.06.019

DO - 10.1016/j.jddst.2018.06.019

M3 - Article

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JO - Journal of Drug Delivery Science and Technology

JF - Journal of Drug Delivery Science and Technology

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