Abstract
To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on thein vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. Duro-Tak® 87-2100 and Duro-Tak® 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from 5.14 ± 3.31 to 0.31 ± 0.12 h as the PG increased from 40% to 60%.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Aungst, B. J., Blake, J. A., and Hussain, M. A., Contributions of drug solubilization, partitioning, barrier disruption, and solvent permeation to the enhancement of skin permeation of various compounds with fatty acids and amines.Pharm. Res., 7, 712–718 (1990).
Barry, B. W., Mode of action of penetration enhancers in human skin.J. Contr. Res., 6, 85–97 (1987).
Blackwell, C. P. and Harding, S. M., The clinical pharmacology of ondansetron.Eur. J. Cancer Clin. Oncol., 25 (Suppl 1), S21-S24 (1989).
Butcher, M. E., Global experience with ondansetron and future potential.Oncology, 50, 191–197 (1993).
Chien, Y. W. and Lambert, H. J., Controlled drug release from polymeric delivery devices II: differentiation between partition-controlled and matrix-controlled drug release mechanism.J. Pharm. Sci., 63, 515–519 (1974).
Cho, Y. J. and Choi, H. K., Enhancement of percutaneous absorption of ketoprofen: effect of vehicles and adhesive matrix.Int. J. Pharm., 169, 95–104 (1998).
Green, P. G., Guy, R. H., and Hadgraft, J.,In vitro an.in vivo enhancement of skin permeation with oleic and lauric acids.Int. J. Pharm., 48, 103–111 (1988).
Gwak, H. S. and Chun, I. K., Effect of vehicles and penetration enhancers on th.in vitro percutaneous absorption of tenoxicam through hairless mouse skin.Int. J. Pharm., 236, 57–64 (2002).
Gwak, H. S., Kim, S. U., and Chun, I. K., Effect of vehicles and enhancers on th.in vitro permeation of melatonin through hairless mouse skin.Arch. Pharm. Res., 25, 392–396 (2002).
Gwak, H. S., Oh, I. S., and Chun, I. K., Transdermal delivery of ondansetron hydrochloride: effect of vehicles and penetration enhancers.Drug Dev. Ind. Pharm., accepted (2003a).
Gwak, H. S., Oh, I. S., and Chun, I. K., Solubility and physicochemical stability of ondansetron hydrochloride in various vehicles.J. Kor. Pharm. Sci., 33, 45–49 (2003b).
Hesketh, P. J. and Gandara, D. R., Serotonin antagonists: a new class of antiemetic agents.J. Natl. Cancer Inst., 83, 613–620 (1991).
McKenzie, R., Kovac, A., O’Connor, T., Duncalf, D., Angel, J., Gratz, I., Tolpin, E., McLeskey, C., and Joslyn, A., Comparison of ondansetron versus placebo to prevent postoperative nausea and vomiting in women undergoing ambulatory gynecologic surgery.Anesthesiology, 78, 21–28 (1993).
Mollgard, B. and Hoelgaard, A., Vehicle effect in topical drug delivery I. Influence of glycols and drug concentration on skin transport.Acta. Pharm. Suec., 20, 433–442 (1983).
Nokhodchi, A., Shokri, J., Dashbolaghi, A., Hassan-Zadeh, D., Ghafourian, T., and Barzegar-Jalali, M., The enhancement effect of surfactants on the penetration of lorazepam through rat skin.Int. J. Pharm., 250, 359–369 (2003).
Roy, S. D., Gutierrez, M., Flynn, G. L., and Cleary, G. W., Controlled transdermal delivery of fentanyl: characterizations of pressure-sensitive adhesives for matrix patch design.J. Pharm. Sci., 85, 491–495 (1996).
Santoyo, S., Arellano, A., Ygartua, P., and Martin, C., Penetration enhancer effects on th.in vitro percutaneous absorption of piroxicam through rat skin.Int. J. Pharm., 117, 219–224 (1995).
Scuderi, P., Wetchler, B., Sung, Y. F., Mingus, M., DuPen, S., Claybon, L., Leslie, J., Talke, P., Apfelbaum, J., and Sharifi-Azad, S., Treatment of postoperative nausea and vomiting after outpatient surgery with the 5-HT3 antagonist ondansetron.Anesthesiology, 78, 15–20 (1993).
Yamada, M., Uda, Y., and Tanigawara, Y., Mechanism of enhancement of percutaneous absorption of molsidomine by oleic acid.Chem. Pharm. Bull., 35, 3399–3406 (1987).
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Gwak, H.S., Oh, I.S. & Chun, I.K. In vitro Percutaneous absorption of ondansetron hydrochloride from pressure-sensitive adhesive matrices through hairless mouse skin. Arch Pharm Res 26, 644–648 (2003). https://doi.org/10.1007/BF02976714
Received:
Issue Date:
DOI: https://doi.org/10.1007/BF02976714