In vitro iontophoretic transport of ketorolac: Synthetic membrane as a barrier

Sandip B. Tiwari, N. Udupa

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

The effect of different factors on the iontophoretic transport of ketorolac was analyzed. In vitro experiments were performed in a diffusion cell with a cellulose membrane as a barrier. The results indicated that an increase in current density or drug concentration enhanced the transmembrane permeation of the drug. The presence of extraneous ions (such as NaCl) or an increase in viscosity of the donor medium slowed down the iontophoretic transport of the drug. The pH does not seem to be an important factor determining iontophoretic transport of ketorolac as statistically insignificant difference was observed in flux at pH 5.6, 7.2, and 8. Also, the relative importance of the transport contributions involved in iontophoresis, namely diffusive iontophoretic and electro-osmotic fluxes, was investigated using glucose as a nonionizable drug. The results indicated that the total flux of ketorolac is a result of two contributions: passive diffusion and iontophoretic flux. The contribution of electro-osmosis appears to be negligible.

Original languageEnglish
Pages (from-to)161-168
Number of pages8
JournalDrug Delivery: Journal of Delivery and Targeting of Therapeutic Agents
Volume10
Issue number3
Publication statusPublished - 07-2003

Fingerprint

Ketorolac
Membranes
Pharmaceutical Preparations
Osmosis
Iontophoresis
Viscosity
Cellulose
Ions
Glucose
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

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title = "In vitro iontophoretic transport of ketorolac: Synthetic membrane as a barrier",
abstract = "The effect of different factors on the iontophoretic transport of ketorolac was analyzed. In vitro experiments were performed in a diffusion cell with a cellulose membrane as a barrier. The results indicated that an increase in current density or drug concentration enhanced the transmembrane permeation of the drug. The presence of extraneous ions (such as NaCl) or an increase in viscosity of the donor medium slowed down the iontophoretic transport of the drug. The pH does not seem to be an important factor determining iontophoretic transport of ketorolac as statistically insignificant difference was observed in flux at pH 5.6, 7.2, and 8. Also, the relative importance of the transport contributions involved in iontophoresis, namely diffusive iontophoretic and electro-osmotic fluxes, was investigated using glucose as a nonionizable drug. The results indicated that the total flux of ketorolac is a result of two contributions: passive diffusion and iontophoretic flux. The contribution of electro-osmosis appears to be negligible.",
author = "Tiwari, {Sandip B.} and N. Udupa",
note = "Cited By :2 Export Date: 10 November 2017 CODEN: DDELE Correspondence Address: Tiwari, S.B.; New Drug Delivery Systems Department, Zydus Research Centre, Sarkhej Bavala Natl. Highway No 8A, Moraiya, Ahmedabad 382 213, Gujarat, India; email: sandiptiwari@zyduscadila.com Chemicals/CAS: glucose, 50-99-7, 84778-64-3; ketorolac, 74103-06-3; Anti-Inflammatory Agents, Non-Steroidal; Cellulose, 9004-34-6; Glucose, 50-99-7; Ketorolac, 66635-83-4; Membranes, Artificial Manufacturers: Torrent, India References: Banga, A.K., Chien, Y.W., Iontophoretic delivery of drugs: Fundamental development and biomedical application (1988) J. Cont. Rel., 7, pp. 1-24; Behl, C.R., Char, H., Patel, S.B., (1993) Topical Drug Bioavailability, Bioequivalence and Penetration, pp. 225-260. , ed. V. P. Shah and H. I. Maibach, New York: Plenum Press; Bellantone, N.H., Rim, S., Franceuos, M.L., Rasadi, B., Enhanced percutaneous absorption via iontophoresis I: Evaluation of an in vitro system and transport of model compounds (1986) Int. J. Pharm., 30, pp. 63-72; Burnette, R.R., Ongpipattanakul, B., Characterization of the pore transport properties and tissue alteration of excised human skin during iontophoresis (1988) J. Pharm. Sci., 77 (2), pp. 132-137; Cleary, G.W., (1993) Topical Drug Bioavailability, Bioequivalance and Penetration, pp. 17-68. , ed. V. P. Shah and H. I. Maibach, New York: Plenum Press; Fang, J.-Y., Huang, Y.-B., Wu, P.-C., Tsai, Y.-H., Transdermal iontophoresis of sodium nonivamide acetate I: Consideration of electrical and chemical factors (1996) Int. J. Pharm., 143, pp. 47-58; Fang, J.-Y., Hsu, L.-R., Huang, Y.-B., Tsai, Y.-H., Evaluation of transdermal iontophoresis of enoxacin from polymer formulations: In vitro skin permeation and in vivo microdialysis using Wistar rat as an animal model (1999) Int. J. Pharm., 180, pp. 137-149; Fang, J.-Y., Sung, K.C., Lin, H.-H., Fang, C.-L., Transdermal iontophoretic delivery of diclofenac sodium from, various polymer formulations: In vitro and in vivo studies (1999) Int. J. Pharm., 178, pp. 83-92; Glikfeld, P., Cullander, C., Hinz, R.S., Guy, R.H., A new system for in vitro studies of iontophoresis (1988) Pharm. Res., 5, pp. 443-446; Guy, R.H., Current status and future prospects of transdermal drug delivery (1996) Pharm. Res., 13 (12), pp. 1765-1769; Haigh, J.M., Smith, E.W., The selection and use of natural and synthetic membranes for in vitro diffusion experiments (1994) Eur. J. Pharm. Sci., 2, pp. 311-320; Li, K.S., Ghanem, A.-H., Peck, K.D., Higuchi, W.I., Characterization of the transport pathways induced during low to moderate voltage iontophoresis in human epidermal membrane (1998) J. Pharm. Sci., 87 (1), pp. 40-47; Litvak, K.M., McEvoy, G.K., Ketorolac, an injectable nonnarcotic analgesic (1990) Clin. Pharm., 9, pp. 921-935; Moll, F., Knoblauch, P., Iontophoretic in vitro release of antimycotics from hydrogels (1993) Drug Dev. Ind. Pharm., 19 (10), pp. 1143-1158; Morimoto, Y., Numajiri, S., Sugibayashi, K., Effect of ion species and their concentration on the iontophoretic transport of benzoic acid through poly(vinyl acetate) membrane (1991) Chem. Pharm. Bull., 39 (9), pp. 2412-2416; Sanderson, J.E., Riel, S.D., Dixon, R., Iontophoretic delivery of nonpeptide drugs: Formulation optimization for maximum skin permeability (1989) J. Pharm. Sci., 78 (5), pp. 361-364; Santi, P., Catellani, P.L., Massimo, G., Zanardi, G., Colombo, P., Iontophoretic transport of verapamil and melatonin I. Cellophane membrane as a barrier (1993) Int. J. Pharm., 92, pp. 23-28; Schultz, S.G., (1980) Basic Principles of Membrane Transport, 21, p. 42. , New York: Cambridge University Press; Sims, S.M., Higuchi, W.I., Srinivasan, V., Interaction of electric field and electroosmotic effects in determining iontophoretic enhancement of anions and cations (1991) Int. J. Pharm., 77, pp. 107-118; Srinivasan, V., Higuchi, W.I., A model for iontophoresis incorporating the effect of convective solvent flow (1990) Int. J. Pharm., 60, pp. 133-138; Thysman, S., Preat, V., Roland, M., Factors affecting iontophoretic mobility of metoprolol (1992) J. Pharm. Sci., 81 (7), pp. 670-675; Tiwari, S.B., Udupa, N., Low cost mini magnetic stirrers for application in pharmacy (1999) Ind. J. Pharm. Edu., 33 (4), pp. 223-224; Tu, Y.-H., Allen, L.V., In vitro iontophoretic studies using a synthetic membrane (1989) J. Pharm. Sci., 78 (3), pp. 211-213; Tyle, P., Iontophoreitc devices for drug delivery (1986) Pharm. Res., 3 (6), pp. 318-326; Zhang, I., Shung, K.K., Edwards, D.A., Hydrogels with enhanced mass transfer for transdermal drug delivery (1996) J. Pharm. Sci., 85 (12), pp. 1312-1316",
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In vitro iontophoretic transport of ketorolac: Synthetic membrane as a barrier. / Tiwari, Sandip B.; Udupa, N.

In: Drug Delivery: Journal of Delivery and Targeting of Therapeutic Agents, Vol. 10, No. 3, 07.2003, p. 161-168.

Research output: Contribution to journalArticle

TY - JOUR

T1 - In vitro iontophoretic transport of ketorolac: Synthetic membrane as a barrier

AU - Tiwari, Sandip B.

AU - Udupa, N.

N1 - Cited By :2 Export Date: 10 November 2017 CODEN: DDELE Correspondence Address: Tiwari, S.B.; New Drug Delivery Systems Department, Zydus Research Centre, Sarkhej Bavala Natl. Highway No 8A, Moraiya, Ahmedabad 382 213, Gujarat, India; email: sandiptiwari@zyduscadila.com Chemicals/CAS: glucose, 50-99-7, 84778-64-3; ketorolac, 74103-06-3; Anti-Inflammatory Agents, Non-Steroidal; Cellulose, 9004-34-6; Glucose, 50-99-7; Ketorolac, 66635-83-4; Membranes, Artificial Manufacturers: Torrent, India References: Banga, A.K., Chien, Y.W., Iontophoretic delivery of drugs: Fundamental development and biomedical application (1988) J. Cont. Rel., 7, pp. 1-24; Behl, C.R., Char, H., Patel, S.B., (1993) Topical Drug Bioavailability, Bioequivalence and Penetration, pp. 225-260. , ed. V. P. Shah and H. I. Maibach, New York: Plenum Press; Bellantone, N.H., Rim, S., Franceuos, M.L., Rasadi, B., Enhanced percutaneous absorption via iontophoresis I: Evaluation of an in vitro system and transport of model compounds (1986) Int. J. Pharm., 30, pp. 63-72; Burnette, R.R., Ongpipattanakul, B., Characterization of the pore transport properties and tissue alteration of excised human skin during iontophoresis (1988) J. Pharm. Sci., 77 (2), pp. 132-137; Cleary, G.W., (1993) Topical Drug Bioavailability, Bioequivalance and Penetration, pp. 17-68. , ed. V. P. Shah and H. I. Maibach, New York: Plenum Press; Fang, J.-Y., Huang, Y.-B., Wu, P.-C., Tsai, Y.-H., Transdermal iontophoresis of sodium nonivamide acetate I: Consideration of electrical and chemical factors (1996) Int. J. Pharm., 143, pp. 47-58; Fang, J.-Y., Hsu, L.-R., Huang, Y.-B., Tsai, Y.-H., Evaluation of transdermal iontophoresis of enoxacin from polymer formulations: In vitro skin permeation and in vivo microdialysis using Wistar rat as an animal model (1999) Int. J. Pharm., 180, pp. 137-149; Fang, J.-Y., Sung, K.C., Lin, H.-H., Fang, C.-L., Transdermal iontophoretic delivery of diclofenac sodium from, various polymer formulations: In vitro and in vivo studies (1999) Int. J. Pharm., 178, pp. 83-92; Glikfeld, P., Cullander, C., Hinz, R.S., Guy, R.H., A new system for in vitro studies of iontophoresis (1988) Pharm. Res., 5, pp. 443-446; Guy, R.H., Current status and future prospects of transdermal drug delivery (1996) Pharm. Res., 13 (12), pp. 1765-1769; Haigh, J.M., Smith, E.W., The selection and use of natural and synthetic membranes for in vitro diffusion experiments (1994) Eur. J. Pharm. Sci., 2, pp. 311-320; Li, K.S., Ghanem, A.-H., Peck, K.D., Higuchi, W.I., Characterization of the transport pathways induced during low to moderate voltage iontophoresis in human epidermal membrane (1998) J. Pharm. Sci., 87 (1), pp. 40-47; Litvak, K.M., McEvoy, G.K., Ketorolac, an injectable nonnarcotic analgesic (1990) Clin. Pharm., 9, pp. 921-935; Moll, F., Knoblauch, P., Iontophoretic in vitro release of antimycotics from hydrogels (1993) Drug Dev. Ind. Pharm., 19 (10), pp. 1143-1158; Morimoto, Y., Numajiri, S., Sugibayashi, K., Effect of ion species and their concentration on the iontophoretic transport of benzoic acid through poly(vinyl acetate) membrane (1991) Chem. Pharm. Bull., 39 (9), pp. 2412-2416; Sanderson, J.E., Riel, S.D., Dixon, R., Iontophoretic delivery of nonpeptide drugs: Formulation optimization for maximum skin permeability (1989) J. Pharm. Sci., 78 (5), pp. 361-364; Santi, P., Catellani, P.L., Massimo, G., Zanardi, G., Colombo, P., Iontophoretic transport of verapamil and melatonin I. Cellophane membrane as a barrier (1993) Int. J. Pharm., 92, pp. 23-28; Schultz, S.G., (1980) Basic Principles of Membrane Transport, 21, p. 42. , New York: Cambridge University Press; Sims, S.M., Higuchi, W.I., Srinivasan, V., Interaction of electric field and electroosmotic effects in determining iontophoretic enhancement of anions and cations (1991) Int. J. Pharm., 77, pp. 107-118; Srinivasan, V., Higuchi, W.I., A model for iontophoresis incorporating the effect of convective solvent flow (1990) Int. J. Pharm., 60, pp. 133-138; Thysman, S., Preat, V., Roland, M., Factors affecting iontophoretic mobility of metoprolol (1992) J. Pharm. Sci., 81 (7), pp. 670-675; Tiwari, S.B., Udupa, N., Low cost mini magnetic stirrers for application in pharmacy (1999) Ind. J. Pharm. Edu., 33 (4), pp. 223-224; Tu, Y.-H., Allen, L.V., In vitro iontophoretic studies using a synthetic membrane (1989) J. Pharm. Sci., 78 (3), pp. 211-213; Tyle, P., Iontophoreitc devices for drug delivery (1986) Pharm. Res., 3 (6), pp. 318-326; Zhang, I., Shung, K.K., Edwards, D.A., Hydrogels with enhanced mass transfer for transdermal drug delivery (1996) J. Pharm. Sci., 85 (12), pp. 1312-1316

PY - 2003/7

Y1 - 2003/7

N2 - The effect of different factors on the iontophoretic transport of ketorolac was analyzed. In vitro experiments were performed in a diffusion cell with a cellulose membrane as a barrier. The results indicated that an increase in current density or drug concentration enhanced the transmembrane permeation of the drug. The presence of extraneous ions (such as NaCl) or an increase in viscosity of the donor medium slowed down the iontophoretic transport of the drug. The pH does not seem to be an important factor determining iontophoretic transport of ketorolac as statistically insignificant difference was observed in flux at pH 5.6, 7.2, and 8. Also, the relative importance of the transport contributions involved in iontophoresis, namely diffusive iontophoretic and electro-osmotic fluxes, was investigated using glucose as a nonionizable drug. The results indicated that the total flux of ketorolac is a result of two contributions: passive diffusion and iontophoretic flux. The contribution of electro-osmosis appears to be negligible.

AB - The effect of different factors on the iontophoretic transport of ketorolac was analyzed. In vitro experiments were performed in a diffusion cell with a cellulose membrane as a barrier. The results indicated that an increase in current density or drug concentration enhanced the transmembrane permeation of the drug. The presence of extraneous ions (such as NaCl) or an increase in viscosity of the donor medium slowed down the iontophoretic transport of the drug. The pH does not seem to be an important factor determining iontophoretic transport of ketorolac as statistically insignificant difference was observed in flux at pH 5.6, 7.2, and 8. Also, the relative importance of the transport contributions involved in iontophoresis, namely diffusive iontophoretic and electro-osmotic fluxes, was investigated using glucose as a nonionizable drug. The results indicated that the total flux of ketorolac is a result of two contributions: passive diffusion and iontophoretic flux. The contribution of electro-osmosis appears to be negligible.

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