Inhibition of P-glycoprotein, multidrug resistance-associated protein 2 and cytochrome P450 3A4 improves the oral absorption of octreotide in rats with portal hypertension

Corrigendum in: /10.3892/etm.2022.11281

  • Authors:
    • Xiao‑Yu Sun
    • Zhi‑Jun Duan
    • Zhen Liu
    • Shun‑Xiong Tang
    • Yang Li
    • Shou‑Cheng He
    • Qiu‑Ming Wang
    • Qing‑Yong Chang
  • View Affiliations

  • Published online on: October 14, 2016     https://doi.org/10.3892/etm.2016.3808
  • Pages: 3716-3722
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Abstract

The aim of the present study was to increase the intestinal transport of octreotide (OCT) by targeting the first‑pass impact to identify a potential method for decreasing portal vein pressure (PVP) using oral OCT. Thus, the bioavailability of intestinally absorbed OCT was evaluated in normal rats and rats with portal hypertension (PH) that had been administered P‑glycoprotein/multidrug resistance‑associated protein 2/cytochrome P450 3A4 (P‑gp/MRP2/CYP3A4) inhibitors. The mRNA and protein expression levels of P‑gp, MRP2 and CYP3A4 were evaluated in normal and PH rats with or without OCT and the inhibitors using RT‑PCR, western blot and immunohistochemical analyses. The potential effects of the inhibitor administration on PVP were also examined. The results suggest that P‑gp, MRP2 and CYP3A4 play important roles in prohibiting the enteral absorption of OCT, particularly under a PH environment. Moreover, inhibitors of P‑gp, MRP2 and CYP3A4 decrease the first‑pass effects of OCT and effectively reduce PVP under PH conditions. Therefore, the present results suggest P‑gp, MRP2 and CYP3A4 are key factors in the intestinal absorption of OCT. The inhibition of P‑gp, MRP2 and CYP3A4 can markedly decrease the first‑pass effects of OCT, and their use may facilitate the use of orally administered OCT.
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December-2016
Volume 12 Issue 6

Print ISSN: 1792-0981
Online ISSN:1792-1015

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Spandidos Publications style
Sun XY, Duan ZJ, Liu Z, Tang SX, Li Y, He SC, Wang QM and Chang QY: Inhibition of P-glycoprotein, multidrug resistance-associated protein 2 and cytochrome P450 3A4 improves the oral absorption of octreotide in rats with portal hypertension Corrigendum in /10.3892/etm.2022.11281. Exp Ther Med 12: 3716-3722, 2016
APA
Sun, X., Duan, Z., Liu, Z., Tang, S., Li, Y., He, S. ... Chang, Q. (2016). Inhibition of P-glycoprotein, multidrug resistance-associated protein 2 and cytochrome P450 3A4 improves the oral absorption of octreotide in rats with portal hypertension Corrigendum in /10.3892/etm.2022.11281. Experimental and Therapeutic Medicine, 12, 3716-3722. https://doi.org/10.3892/etm.2016.3808
MLA
Sun, X., Duan, Z., Liu, Z., Tang, S., Li, Y., He, S., Wang, Q., Chang, Q."Inhibition of P-glycoprotein, multidrug resistance-associated protein 2 and cytochrome P450 3A4 improves the oral absorption of octreotide in rats with portal hypertension Corrigendum in /10.3892/etm.2022.11281". Experimental and Therapeutic Medicine 12.6 (2016): 3716-3722.
Chicago
Sun, X., Duan, Z., Liu, Z., Tang, S., Li, Y., He, S., Wang, Q., Chang, Q."Inhibition of P-glycoprotein, multidrug resistance-associated protein 2 and cytochrome P450 3A4 improves the oral absorption of octreotide in rats with portal hypertension Corrigendum in /10.3892/etm.2022.11281". Experimental and Therapeutic Medicine 12, no. 6 (2016): 3716-3722. https://doi.org/10.3892/etm.2016.3808