The intestinal uptake of phenol from micellar systems does not conform to the aqueous transfer model

Prajakti A. Kothare; Cheryl L. Zimmerman

doi:10.1023/A:1007560309582

The intestinal uptake of phenol from micellar systems does not conform to the aqueous transfer model

Prajakti A. Kothare, Cheryl L. Zimmerman

Pharmaceutics

Research output: Contribution to journal › Article › peer-review

Abstract

Purpose. To evaluate the aqueous transfer model as the mechanism for the micelle-mediated uptake of phenol in the rat in situ intestinal perfusion model. Methods. Phenol in isotonic HEPES buffer was perfused through the jejunal segment at two flow rates and at various concentrations. Phenol was then dispersed in two, distinct mixed micelle systems composed of 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 uptake studied in each case. Equilibrium dialysis was done to determine the aqueous fraction of phenol in each system. Results. The P(eff) of phenol in isotonic HEPES buffer at a low flow rate (n = 6) was 1.7 ± 0.4 x 10^-4 cm/s and at a high flow rate (n = 13) was 1.8 ± 0.5 x 10^-4 cm/s. The P(eff) for the 10:2.5 system at the high flow rate (n = 3) was 1.5 ± 0.4 x 10^-4 cm/s and at the low flow rate (n = 3) was 1.4 ± 0.3 x 10^-4 cm/s. Uptake was membrane rate-limited in both the non-micellar and 10:2.5 systems. P(eff) at a high flow rate (n = 3) in the 10:10 system was 1.3 ± 0.1 x 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 the aqueous transfer model of uptake.

Original language	English (US)
Pages (from-to)	839-843
Number of pages	5
Journal	Pharmaceutical research
Volume	17
Issue number	7
DOIs	https://doi.org/10.1023/A:1007560309582
State	Published - 2000

Bibliographical note

Funding Information:
The partial financial support from ISWOP, University of Minnesota, is acknowledged. We thank Dr. Timothy S. Wied-mann for useful scientific discussions through the course of the study. The authors would also like to thank Dr. Roland Gunther, Department of Veterinary Medicine, University of Minnesota, for the analysis of the histological samples.

Copyright:
Copyright 2017 Elsevier B.V., All rights reserved.

Keywords

Aqueous transfer model
Equilibrium dialysis
Micelle-mediated uptake
Phenol

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10.1023/A:1007560309582

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@article{4586d1ee31864c95aab7f5db9fab2346,

title = "The intestinal uptake of phenol from micellar systems does not conform to the aqueous transfer model",

abstract = "Purpose. To evaluate the aqueous transfer model as the mechanism for the micelle-mediated uptake of phenol in the rat in situ intestinal perfusion model. Methods. Phenol in isotonic HEPES buffer was perfused through the jejunal segment at two flow rates and at various concentrations. Phenol was then dispersed in two, distinct mixed micelle systems composed of 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 uptake studied in each case. Equilibrium dialysis was done to determine the aqueous fraction of phenol in each system. Results. The P(eff) of phenol in isotonic HEPES buffer at a low flow rate (n = 6) was 1.7 ± 0.4 x 10-4 cm/s and at a high flow rate (n = 13) was 1.8 ± 0.5 x 10-4 cm/s. The P(eff) for the 10:2.5 system at the high flow rate (n = 3) was 1.5 ± 0.4 x 10-4 cm/s and at the low flow rate (n = 3) was 1.4 ± 0.3 x 10-4 cm/s. Uptake was membrane rate-limited in both the non-micellar and 10:2.5 systems. P(eff) at a high flow rate (n = 3) in the 10:10 system was 1.3 ± 0.1 x 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 the aqueous transfer model of uptake.",

keywords = "Aqueous transfer model, Equilibrium dialysis, Micelle-mediated uptake, Phenol",

author = "Kothare, {Prajakti A.} and Zimmerman, {Cheryl L.}",

note = "Funding Information: The partial financial support from ISWOP, University of Minnesota, is acknowledged. We thank Dr. Timothy S. Wied-mann for useful scientific discussions through the course of the study. The authors would also like to thank Dr. Roland Gunther, Department of Veterinary Medicine, University of Minnesota, for the analysis of the histological samples. Copyright: Copyright 2017 Elsevier B.V., All rights reserved.",

year = "2000",

doi = "10.1023/A:1007560309582",

language = "English (US)",

volume = "17",

pages = "839--843",

journal = "Pharmaceutical Research",

issn = "0724-8741",

publisher = "Springer New York",

number = "7",

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TY - JOUR

T1 - The intestinal uptake of phenol from micellar systems does not conform to the aqueous transfer model

AU - Kothare, Prajakti A.

AU - Zimmerman, Cheryl L.

N1 - Funding Information: The partial financial support from ISWOP, University of Minnesota, is acknowledged. We thank Dr. Timothy S. Wied-mann for useful scientific discussions through the course of the study. The authors would also like to thank Dr. Roland Gunther, Department of Veterinary Medicine, University of Minnesota, for the analysis of the histological samples. Copyright: Copyright 2017 Elsevier B.V., All rights reserved.

PY - 2000

Y1 - 2000

N2 - Purpose. To evaluate the aqueous transfer model as the mechanism for the micelle-mediated uptake of phenol in the rat in situ intestinal perfusion model. Methods. Phenol in isotonic HEPES buffer was perfused through the jejunal segment at two flow rates and at various concentrations. Phenol was then dispersed in two, distinct mixed micelle systems composed of 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 uptake studied in each case. Equilibrium dialysis was done to determine the aqueous fraction of phenol in each system. Results. The P(eff) of phenol in isotonic HEPES buffer at a low flow rate (n = 6) was 1.7 ± 0.4 x 10-4 cm/s and at a high flow rate (n = 13) was 1.8 ± 0.5 x 10-4 cm/s. The P(eff) for the 10:2.5 system at the high flow rate (n = 3) was 1.5 ± 0.4 x 10-4 cm/s and at the low flow rate (n = 3) was 1.4 ± 0.3 x 10-4 cm/s. Uptake was membrane rate-limited in both the non-micellar and 10:2.5 systems. P(eff) at a high flow rate (n = 3) in the 10:10 system was 1.3 ± 0.1 x 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 the aqueous transfer model of uptake.

AB - Purpose. To evaluate the aqueous transfer model as the mechanism for the micelle-mediated uptake of phenol in the rat in situ intestinal perfusion model. Methods. Phenol in isotonic HEPES buffer was perfused through the jejunal segment at two flow rates and at various concentrations. Phenol was then dispersed in two, distinct mixed micelle systems composed of 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 uptake studied in each case. Equilibrium dialysis was done to determine the aqueous fraction of phenol in each system. Results. The P(eff) of phenol in isotonic HEPES buffer at a low flow rate (n = 6) was 1.7 ± 0.4 x 10-4 cm/s and at a high flow rate (n = 13) was 1.8 ± 0.5 x 10-4 cm/s. The P(eff) for the 10:2.5 system at the high flow rate (n = 3) was 1.5 ± 0.4 x 10-4 cm/s and at the low flow rate (n = 3) was 1.4 ± 0.3 x 10-4 cm/s. Uptake was membrane rate-limited in both the non-micellar and 10:2.5 systems. P(eff) at a high flow rate (n = 3) in the 10:10 system was 1.3 ± 0.1 x 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 the aqueous transfer model of uptake.

KW - Aqueous transfer model

KW - Equilibrium dialysis

KW - Micelle-mediated uptake

KW - Phenol

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U2 - 10.1023/A:1007560309582

DO - 10.1023/A:1007560309582

M3 - Article

C2 - 10990203

AN - SCOPUS:0033843182

VL - 17

SP - 839

EP - 843

JO - Pharmaceutical Research

JF - Pharmaceutical Research

SN - 0724-8741

IS - 7

ER -

The intestinal uptake of phenol from micellar systems does not conform to the aqueous transfer model

Abstract

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