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The Intestinal Uptake of Phenol from Micellar Systems Does Not Conform to the Aqueous Transfer Model

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Abstract

Purpose. To evaluate the aqueous transfer model as the mechanismfor the micelle-mediated uptake of phenol in the rat in situ intestinalperfusion model.

Methods. Phenol in isotonic HEPES buffer was perfused through thejejunal segment at two flow rates and at various concentrations. Phenolwas then dispersed in two, distinct mixed micelle systems composedof sodium taurocholate and phosphatidylcholine at 10 mM:2.5 mM(10:2.5 system) and at 10 mM: 10 mM (10:10 system) and its uptakestudied in each case. Equilibrium dialysis was done to determine theaqueous fraction of phenol in each system.

Results. The Peff of phenol in isotonic HEPES buffer at a low flowrate (n = 6) was 1.7 ± 0.4 × 10−4 cm/s and at a high flow rate(n = 13) was 1.8 ± 0.5 × 10−4 cm/s. The Peff for the 10:2.5 systemat the high flow rate (n = 3) was 1.5 ± 0.4 × 10−4 cm/s and at thelow flow rate (n = 3) was 1.4 ± 0.3 × 10−4 cm/s. Uptake wasmembrane rate-limited in both the non-micellar and 10:2.5 systems.Peff at a high flow rate (n = 3) in the 10:10 system was 1.3 ± 0.1 ×10−4 cm/s. Equilibrium dialysis (n = 4) revealed free fractions of 0.60± 0.05 and 0.50 ± 0.03 for the 10:2.5 and 10:10 systems.

Conclusions. The uptake of micellized phenol did not follow theaqueous transfer model of uptake.

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Authors and Affiliations

  1. Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota, 55455

    Prajakti A. Kothare

  2. Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota, 55455

    Cheryl L. Zimmerman

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  1. Prajakti A. Kothare
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  2. Cheryl L. Zimmerman
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Kothare, P.A., Zimmerman, C.L. The Intestinal Uptake of Phenol from Micellar Systems Does Not Conform to the Aqueous Transfer Model. Pharm Res 17, 839–843 (2000). https://doi.org/10.1023/A:1007560309582

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