PASSIVE AND IONTOPHORETIC PERMEATION OF CAPTOPRIL  GEL: AN IN VITRO AND IN VIVO STUDY

Ashish Jain; Satish Nayak; Vandana Soni

doi:10.14499/indonesianjpharm23iss2pp121-129

PASSIVE AND IONTOPHORETIC PERMEATION OF CAPTOPRIL GEL: AN IN VITRO AND IN VIVO STUDY

Ashish Jain, Satish Nayak, Vandana Soni

Abstract

The Objective of this work was to formulate and evaluate captopril gel to assess its suitability for transdermal delivery by passive and iontophoresis. A polymer gel was prepared using hydroxypropyl methyl cellulose and in vitro skin permeability was assessed in full thickness skin of rabbits and pigs. For in vivo studies New Zealand rabbits were used. In vitro passive permeation was carried out in Franz diffusion cell but for iontophoresis, diffusion cell was modified according to Glikfield design. Iontophoresis was performed at a current density of 0.5 mA/cm²

via silver /silver chloride electrodes with passive controls but for in vivo study current density was

reduced to 0.1 mA/cm². Blood samples were analyzed for drug content by HPLC. Results of the in vitro study indicated that iontophoresis considerably increased the permeation rate of captopril compared to passive controls in both the skin types (P<0.01). The plasma concentration of captopril was significantly higher (P<0.001) than that obtained in the passive controls. Results showed that the target permeation rates for captopril could be achieved with the aid of iontophoresis by increasing the area in an appreciable range.

Key words: Captopril, iontophoresis, transdermal, Rabbit, Pigskin, in vitro, in vivo.

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References

Anigbogu A, Patil S, Singh P, Liu P, Dinh S, Maibach H. 2000; An in vivo investigation of the rabbit skin responses to transdermal iontophoresis. Int. J. Pharm 200:195-206.

Banga, A.K. 1998; Electrically Assisted Transdermal and Topical Drug Delivery. 1st ed.; Taylor & Francis Ltd: UK, pp. 1-32.

Bolton S. Pharmaceutical analysis practical and clinical application, ed 3, Marcel Dekker, New York, 1999; 250- 329p.

Dandagi PM, Mastiholimath VS, Patil MB, Gupta MK. 2006; Biodegradable microparti-culate system of captopril. Int. J. Pharm. 307(1): 83-88.

Doh, H.J., Cho, W.J., Yong, C.S., Choi, H.G., Kim, J.S., Lee, C.H., Kim, D.D., Synthesis and evaluation of ketorolac ester prodrugs for transdermal delivery, J. Pharm. Sci. 92 (2003) 1008–1017.

Faruk A, Ishar MPS. 2009;In- Vivo Passive and Iontophoresis Delivery of Lisinopril Using Wistar Rat Model. International J.Pharm. Clin. Res. 1(3): 131-135.

Ghosh B, Jain A, Ashok P, Patel B and Tarafdar K. 2009, Passive and Iontophoretic Permeation of Glipizide Gel: An In Vitro and In Vivo Study. Current Drug. Delivery, 6, 444-450.

Glikfield P, Cullander C, Hinz R, Guy R. 1988; A new system for in vitro studies of iontophoresis. Pharm Res 5: 443-446.

Hao W, Hui-Min H. 2000; Improvement of transdermal permeation of captopril by iontophoresis. Acta. Pharmacol. Sin. 21(7): 591-595.

Hirvonen J, Rytting JH, Paronen P, Urtti A, Dodecyl N. Ndimethylamino acetate and azone enhance drug penetration across human, snake, and rabbit skin. Pharm. Res. 1991; 8: 933-937.

Jain A, Nayak S, Soni V. 2011, A study of transdermal delivery of captopril using iontophoresis. J. Pharma. Bio Sci.,11(8).

Jarrott B, Drmmer O, Hooper R, Anderson AIE, Miach PJ. 1982; Pharmacokinetics properties of captopril after acute and chronic administration to hypertensive subjects. Am. J. Cardiol. 49: 1547-1552.

Jarrott B, Drummer O, Hooper R, Anderson AIE, Miach PJ, Louis WJ, 1982, Pharmacokinetic propertiesof captopril after acute and chronic administration to hypertensive subjects, Am J Cardiol, 49, , 1547.

Kalia YN, Naik A, Garrison J, Guy RH. 2004; Iontophoretic drug delivery. Adv. Drug. Deliv. Rev. 56(5): 619-58.

Levy M, Koren G, Klein J, McLorie G, Balfe JW, captopril pharmacokinetics, blood pressure response and plasma renin activity in normotensive children with renal scarring, Dev. Pharmacol. Ther, 4, 1991, 185-193.

Levy M, Koren G, Klein J, McLorie G, Balfe JW. 1990; Captopril pharmacokinetics, blood pressure response and plasma rennin activity in normotensive children with renal scarring. Dev Pharmacol Ther.94: 235-240.

McEvoy GK, 1996 American Hospital Formulary Service. USA Press, PP 864-871.

Mutalik S, Udapa N. 2006; Pharmacological evaluation of membrane-moderated transdermal system of glibenclamide. Clin. Exp. Pharmacol. Physiol. 33:17-26.

Nair VB, Panchagnula R. 2003; Effect of iontophoresis and fatty acids on permeation of arginine vasopressin through rat skin. Pharmacol. Res. 47(6): 563-569.

Ohman KP, Kagedal B, Larson R, Kalberg BE. 1985; Pharmacokinetics of captopril and its effect on blood pressure during acute and chronic administration in relation to food intake. J. Cardiovasc. Pharmacol. 7: S20-S24.

Pillai O, Nair V, Panchagnula R. 2004; Transdermal iontophoresis of insulin: IV. Influence of chemical enhancers. Int J Pharm. 269(1): 109-120.

Popovici RF, Alexa IF, Novac O, Vrinceanu N, Popovici E, Lupusoru CE, and Voicu VA. 2011; Pharmacokinetics Study on Mesoporous Silica-Captopril Controlled Release Systems. Digest J. Nano. Bios.6(3):1619-1630.

Raia JJ, Toseph J, Barone JA, Byerly WB, and Lacy CR, 1990, Angiotensin converting enzyme inhibitor: a comparative review, D1CP Ann Pharmacother, 24, 506-511.

Raia PC, Toseph J, Barone JA, Byerly WB, Lacy CR. 1990; Angiotensin converting enzyme inhibitor: a comparative review. DICP Ann Pharmacother. 24: 506-511.

Sung KC, Fang JY , Hu OYP. Delivery of nalbuphine and its prodrugs across skin by passive diffusion and iontophoresis. J Cont Rel 2000; 67:1–8.

Suwanpidokkul N, Thongnopnua P, Umprayn K. Transdermal delivery of zidovudine: The effects of vehicles, enhancers, and polymer membranes on permeation across cadaver pig skin. AAPS Pharm Sci Tech 2004; 5(3): 48.

Sweetman SC., 2005., Martindale: The Complete Drug Reference. 34th edition; Pharmaceutical press, Taro O, Tomona H, Masahiro Iwaki, and Tadatoshi T. 2001, Transdermal absorption of bupranolol in rabbit skin in vitro and in vivo. Biol. Pharm. Bull. 24, 588- 591.

Wang Y, Thakur R, Fan Q, Michniak B. 2005; Transdermal iontophoresis: combination strategies to improve transdermal iontophoretic drug delivery. Eur. J.Pharm. Biopharm. 60(2): 179-191.

Wu PC, Huang YB, Chang JJF, Chang JS, Tsai YH. Evaluation of pharmacokinetics and pharmacodynamics of captopril from transdermal hydrophilic gels in normotensive rabbits and spontaneously hypertensive rats. Int. J. Pharm. 2000; 209:87–94.

Wu PC, Huang YB, Fang JY, Tsai YH. 1997; In-vitro percutaneous absorption of captopril. Int. J. Pharm. 148: 41-46.

Wu PC, Huang YB, Lin HH, Tsai YH. 1996; Percutaneous absorption of captorpil from hydrophilic cellulose gel® through excised rabbit skin and human skin. Int. J. Pharmaceutics 145(2): 215-220

Zakzewski CA, Amory DW, Jasaitis DK, Li JK. 1992; Iontophoretically enhanced transdermal delivery of an ACE inhibitor in induced hypertensive rabbits: preliminary report. Cardiovasc Drugs Ther. 6(6):589-95.

Zhou XH, Li Wan Po A, 1994, Stability and in vitro absorption of captopril, enalapril, and lisinopril across the rat intestine, Biochem Pharmacol, 47, 1121-1126.

Zohu XH, Li Wan Po A. 1994; Stability and invitro absorption of Captopril, Enalapril and Lisinopril across the rat intestine. Biochem Pharmacol 47: 1121-1126.

DOI: http://dx.doi.org/10.14499/indonesianjpharm23iss2pp121-129