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Effects of sodium deoxycholate and sodium caprate on the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of rats.
Biochem Pharmacol. 2000 Mar 15; 59(6):665-72.BP

Abstract

The effects of sodium deoxycholate (Deo-Na), a bile salt, and sodium caprate (Cap-Na), a fatty acid, on the transport of epirubicin were investigated in both the human colon adenocarcinoma (Caco-2) cell line and the everted gut sacs of the rat jejunum and ileum. The possible use of these two potent absorption enhancers as multidrug resistance (MDR) reversing agents also was examined. Epirubicin uptake experiments using a flow cytometer showed that Deo-Na and Cap-Na significantly increased the accumulation of epirubicin in Caco-2 cells. These two enhancers significantly increased apical to basolateral absorption of epirubicin across Caco-2 monolayers and mucosal to serosal absorption of epirubicin in the rat jejunum and ileum. Moreover, the addition of Deo-Na or Cap-Na significantly reduced the basolateral to apical efflux of epirubicin across Caco-2 monolayers. The co-presence of verapamil, one typical P-glycoprotein (P-gp) substrate, and Deo-Na or Cap-Na demonstrated further reduction of epirubicin efflux. The study suggests that inhibition of P-gp or other transporter proteins located in the intestines may be involved, at least partially, in the reduction of epirubicin efflux. In conclusion, the therapeutic efficacy of epirubicin may be improved by the use of such low toxicity excipients as absorption enhancers and MDR modulators in formulations.

Authors+Show Affiliations

Department of Pharmacy, Chia-Nan College of Pharmacy and Science, Tainan Hsien, Taiwan. yulilo@ms17.hinet.netNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

10677583

Citation

Lo, Y L., and J D. Huang. "Effects of Sodium Deoxycholate and Sodium Caprate On the Transport of Epirubicin in Human Intestinal Epithelial Caco-2 Cell Layers and Everted Gut Sacs of Rats." Biochemical Pharmacology, vol. 59, no. 6, 2000, pp. 665-72.
Lo YL, Huang JD. Effects of sodium deoxycholate and sodium caprate on the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of rats. Biochem Pharmacol. 2000;59(6):665-72.
Lo, Y. L., & Huang, J. D. (2000). Effects of sodium deoxycholate and sodium caprate on the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of rats. Biochemical Pharmacology, 59(6), 665-72.
Lo YL, Huang JD. Effects of Sodium Deoxycholate and Sodium Caprate On the Transport of Epirubicin in Human Intestinal Epithelial Caco-2 Cell Layers and Everted Gut Sacs of Rats. Biochem Pharmacol. 2000 Mar 15;59(6):665-72. PubMed PMID: 10677583.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of sodium deoxycholate and sodium caprate on the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of rats. AU - Lo,Y L, AU - Huang,J D, PY - 2000/2/25/pubmed PY - 2000/3/11/medline PY - 2000/2/25/entrez SP - 665 EP - 72 JF - Biochemical pharmacology JO - Biochem Pharmacol VL - 59 IS - 6 N2 - The effects of sodium deoxycholate (Deo-Na), a bile salt, and sodium caprate (Cap-Na), a fatty acid, on the transport of epirubicin were investigated in both the human colon adenocarcinoma (Caco-2) cell line and the everted gut sacs of the rat jejunum and ileum. The possible use of these two potent absorption enhancers as multidrug resistance (MDR) reversing agents also was examined. Epirubicin uptake experiments using a flow cytometer showed that Deo-Na and Cap-Na significantly increased the accumulation of epirubicin in Caco-2 cells. These two enhancers significantly increased apical to basolateral absorption of epirubicin across Caco-2 monolayers and mucosal to serosal absorption of epirubicin in the rat jejunum and ileum. Moreover, the addition of Deo-Na or Cap-Na significantly reduced the basolateral to apical efflux of epirubicin across Caco-2 monolayers. The co-presence of verapamil, one typical P-glycoprotein (P-gp) substrate, and Deo-Na or Cap-Na demonstrated further reduction of epirubicin efflux. The study suggests that inhibition of P-gp or other transporter proteins located in the intestines may be involved, at least partially, in the reduction of epirubicin efflux. In conclusion, the therapeutic efficacy of epirubicin may be improved by the use of such low toxicity excipients as absorption enhancers and MDR modulators in formulations. SN - 0006-2952 UR - https://www.unboundmedicine.com/medline/citation/10677583/Effects_of_sodium_deoxycholate_and_sodium_caprate_on_the_transport_of_epirubicin_in_human_intestinal_epithelial_Caco_2_cell_layers_and_everted_gut_sacs_of_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0006-2952(99)00377-9 DB - PRIME DP - Unbound Medicine ER -