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Comparison of effects of surfactants with other MDR reversing agents on intracellular uptake of epirubicin in Caco-2 cell line.
Anticancer Res. 1998 Jul-Aug; 18(4C):3005-9.AR

Abstract

P-glycoprotein (P-gp) actively pumps out a number of anticancer drugs, such as epirubicin, from tumor cells. P-gp is also expressed in the small intestine under normal physiological conditions. Inhibition of intestinal P-gp function using MDR reversing agents may enhance the oral bioavailability of some chemotherapeutic agents. Human colon adenocarcinoma (Caco-2) cell line expresses many characteristics of differentiated cells of the normal small intestine. Using Caco-2 as an in vitro intestinal model, the overall goal of the present study was to evaluate the MDR-reversing effects of some commonly used nonabsorptive pharmaceutical surfactants, such as Tween 20, Tween 80 and acacia on the intracellular accumulation of epirubicin by flow cytometry. Tween 20, Tween 80 or acacia all significantly increased intracellular accumulation of epirubicin with the highest enhancing effect for acacia and the lowest for Tween 20. Apart from progesterone, the enhancing effects of surfactants were better than those of non-surfactant MDR reversing agents such as verapamil, trifluoperazine and reserpine. In conclusion, our results demonstrate that progesterone, acacia, Tween 20 and Tween 80 are potent MDR modifiers of epirubicin in Caco-2 at concentrations that could be achieved in vivo. Use of surfactants in excipients may increase the intestinal absorption of some drugs through P-gp inhibition and thus improve drug bioavailability for P-gp substrate.

Authors+Show Affiliations

Department of Pharmacy, Chia Nan College of Pharmacy and Science, Hsien, Taiwan, R.O.C. yulilo@mail.ncku.edu.twNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

9713500

Citation

Lo, Y L., et al. "Comparison of Effects of Surfactants With Other MDR Reversing Agents On Intracellular Uptake of Epirubicin in Caco-2 Cell Line." Anticancer Research, vol. 18, no. 4C, 1998, pp. 3005-9.
Lo YL, Hsu CY, Huang JD. Comparison of effects of surfactants with other MDR reversing agents on intracellular uptake of epirubicin in Caco-2 cell line. Anticancer Res. 1998;18(4C):3005-9.
Lo, Y. L., Hsu, C. Y., & Huang, J. D. (1998). Comparison of effects of surfactants with other MDR reversing agents on intracellular uptake of epirubicin in Caco-2 cell line. Anticancer Research, 18(4C), 3005-9.
Lo YL, Hsu CY, Huang JD. Comparison of Effects of Surfactants With Other MDR Reversing Agents On Intracellular Uptake of Epirubicin in Caco-2 Cell Line. Anticancer Res. 1998 Jul-Aug;18(4C):3005-9. PubMed PMID: 9713500.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparison of effects of surfactants with other MDR reversing agents on intracellular uptake of epirubicin in Caco-2 cell line. AU - Lo,Y L, AU - Hsu,C Y, AU - Huang,J D, PY - 1998/8/26/pubmed PY - 1998/8/26/medline PY - 1998/8/26/entrez SP - 3005 EP - 9 JF - Anticancer research JO - Anticancer Res VL - 18 IS - 4C N2 - P-glycoprotein (P-gp) actively pumps out a number of anticancer drugs, such as epirubicin, from tumor cells. P-gp is also expressed in the small intestine under normal physiological conditions. Inhibition of intestinal P-gp function using MDR reversing agents may enhance the oral bioavailability of some chemotherapeutic agents. Human colon adenocarcinoma (Caco-2) cell line expresses many characteristics of differentiated cells of the normal small intestine. Using Caco-2 as an in vitro intestinal model, the overall goal of the present study was to evaluate the MDR-reversing effects of some commonly used nonabsorptive pharmaceutical surfactants, such as Tween 20, Tween 80 and acacia on the intracellular accumulation of epirubicin by flow cytometry. Tween 20, Tween 80 or acacia all significantly increased intracellular accumulation of epirubicin with the highest enhancing effect for acacia and the lowest for Tween 20. Apart from progesterone, the enhancing effects of surfactants were better than those of non-surfactant MDR reversing agents such as verapamil, trifluoperazine and reserpine. In conclusion, our results demonstrate that progesterone, acacia, Tween 20 and Tween 80 are potent MDR modifiers of epirubicin in Caco-2 at concentrations that could be achieved in vivo. Use of surfactants in excipients may increase the intestinal absorption of some drugs through P-gp inhibition and thus improve drug bioavailability for P-gp substrate. SN - 0250-7005 UR - https://www.unboundmedicine.com/medline/citation/9713500/Comparison_of_effects_of_surfactants_with_other_MDR_reversing_agents_on_intracellular_uptake_of_epirubicin_in_Caco_2_cell_line_ L2 - https://antibodies.cancer.gov/detail/CPTC-ABCB1-4 DB - PRIME DP - Unbound Medicine ER -