Tags

Type your tag names separated by a space and hit enter

In-vitro transfer of nitazoxanide across the intestinal epithelial barrier.
J Pharm Pharmacol 2002; 54(10):1413-7JP

Abstract

Nitazoxanide is a thiazolide compound that exhibits antimicrobial properties against helminths, protozoa, anaerobic bacteria and also Helicobacter pylori. The mucosal diffusion of this new drug has not been studied. The aim of this study was to examine the transport of radiolabelled nitazoxanide across the epithelial barrier according to the mode (mucosal or serosal) of drug administration. HT29-19A intestinal epithelial cells, grown as monolayers on microporous filters, were used as an epithelial model. In a short-term (100 min) transport study, the apical to basal and the basal to apical transport of nitazoxanide across the monolayers was studied in an Ussing chamber. In a long-term (24 h) study, the transport of the drug and its intracellular accumulation were studied in filter-grown epithelial monolayers kept in culture plates. In the short-term transport study, both the apical and basal fluxes achieved a steady state after 70 min and there was no significant difference between the apical to basal (3991+/-1001 ng h(-1) cm(-2)) and the basal to apical (4246+/-856 ng h(-1) cm(-2)) nitazoxanide fluxes. In the long-term transport study, after apical or basal drug application, a gradual increase in the drug concentration in the opposite compartment was noted, which reached similar values for apical and basal fluxes (2497+/-125 and 2309+/-81 ng mL(-1), respectively) after 24 h. Moreover, a rapid, although transitory, intracellular accumulation of nitazoxanide was observed at 10 min after apical (299+/-25 ng/10(6) cells) and basal (124+/-10 ng/10(6) cells) drug application, but decreased thereafter. There is an important transepithelial transport of nitazoxanide across the digestive epithelial monolayer with a rapid intracellular accumulation of the drug. No difference between the apical to basal and basal to apical fluxes of the drug was observed, suggesting that both topical and systemic modes of action of this antibiotic are successful.

Authors+Show Affiliations

INSERM EMI-0212, Faculté de Médecine Necker-Enfants Malades, 156 rue de Vaugirard, 75730 Paris, France. matsiak@necker.frNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

12396305

Citation

Matysiak-Budnik, Tamara, et al. "In-vitro Transfer of Nitazoxanide Across the Intestinal Epithelial Barrier." The Journal of Pharmacy and Pharmacology, vol. 54, no. 10, 2002, pp. 1413-7.
Matysiak-Budnik T, Mégraud F, Heyman M. In-vitro transfer of nitazoxanide across the intestinal epithelial barrier. J Pharm Pharmacol. 2002;54(10):1413-7.
Matysiak-Budnik, T., Mégraud, F., & Heyman, M. (2002). In-vitro transfer of nitazoxanide across the intestinal epithelial barrier. The Journal of Pharmacy and Pharmacology, 54(10), pp. 1413-7.
Matysiak-Budnik T, Mégraud F, Heyman M. In-vitro Transfer of Nitazoxanide Across the Intestinal Epithelial Barrier. J Pharm Pharmacol. 2002;54(10):1413-7. PubMed PMID: 12396305.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In-vitro transfer of nitazoxanide across the intestinal epithelial barrier. AU - Matysiak-Budnik,Tamara, AU - Mégraud,Francis, AU - Heyman,Martine, PY - 2002/10/25/pubmed PY - 2003/3/12/medline PY - 2002/10/25/entrez SP - 1413 EP - 7 JF - The Journal of pharmacy and pharmacology JO - J. Pharm. Pharmacol. VL - 54 IS - 10 N2 - Nitazoxanide is a thiazolide compound that exhibits antimicrobial properties against helminths, protozoa, anaerobic bacteria and also Helicobacter pylori. The mucosal diffusion of this new drug has not been studied. The aim of this study was to examine the transport of radiolabelled nitazoxanide across the epithelial barrier according to the mode (mucosal or serosal) of drug administration. HT29-19A intestinal epithelial cells, grown as monolayers on microporous filters, were used as an epithelial model. In a short-term (100 min) transport study, the apical to basal and the basal to apical transport of nitazoxanide across the monolayers was studied in an Ussing chamber. In a long-term (24 h) study, the transport of the drug and its intracellular accumulation were studied in filter-grown epithelial monolayers kept in culture plates. In the short-term transport study, both the apical and basal fluxes achieved a steady state after 70 min and there was no significant difference between the apical to basal (3991+/-1001 ng h(-1) cm(-2)) and the basal to apical (4246+/-856 ng h(-1) cm(-2)) nitazoxanide fluxes. In the long-term transport study, after apical or basal drug application, a gradual increase in the drug concentration in the opposite compartment was noted, which reached similar values for apical and basal fluxes (2497+/-125 and 2309+/-81 ng mL(-1), respectively) after 24 h. Moreover, a rapid, although transitory, intracellular accumulation of nitazoxanide was observed at 10 min after apical (299+/-25 ng/10(6) cells) and basal (124+/-10 ng/10(6) cells) drug application, but decreased thereafter. There is an important transepithelial transport of nitazoxanide across the digestive epithelial monolayer with a rapid intracellular accumulation of the drug. No difference between the apical to basal and basal to apical fluxes of the drug was observed, suggesting that both topical and systemic modes of action of this antibiotic are successful. SN - 0022-3573 UR - https://www.unboundmedicine.com/medline/citation/12396305/In_vitro_transfer_of_nitazoxanide_across_the_intestinal_epithelial_barrier_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0022-3573&date=2002&volume=54&issue=10&spage=1413 DB - PRIME DP - Unbound Medicine ER -