Evaluation of creatine transport using Caco-2 monolayers as an in vitro model for intestinal absorption

Alekha K. Dash, Donald W. Miller, Han Huai-Yan, Joe Carnazzo, Jeffrey R. Stout

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

Creatine is a nutraceutical that has gained popularity in both well-trained and casual athletes for its performance-enhancing or ergogenic properties. The major disadvantages of creatine monohydrate formulations are poor solubility and oral bioavailability. In the present study, creatine transport was examined using Caco-2 monolayers as an in vitro model for intestinal absorption. Confluent monolayers of Caco-2 cells (passage 25-35) were used for the permeability studies. Monolayers were placed in side-by-side diffusion chambers. 14C-Creatine (0.1-0.5 μCi/mL) was added to either the apical or basolateral side, and the transport of the creatine across the Caco-2 monolayer was measured over a 90-min period. The apical to basolateral transport of 14C-creatine was small, ranging from 0.2-3% of the original amount appearing on the receiver side in a 90-min period. Interestingly, the basolateral to apical permeability of radiolabeled creatine was substantially greater than that observed in the apical to basolateral direction. Studies with drug efflux transport inhibitors indicate that neither the P-glycoprotein nor multidrug resistance-associated protein is involved in the enhanced basolateral to apical transport of creatine.

Original languageEnglish
Pages (from-to)1593-1598
Number of pages6
JournalJournal of Pharmaceutical Sciences
Volume90
Issue number10
DOIs
StatePublished - 2001

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Creatine
Intestinal Absorption
Monolayers
Permeability
Multidrug Resistance-Associated Proteins
Caco-2 Cells
In Vitro Techniques
P-Glycoprotein
Dietary Supplements
Athletes
Solubility
Biological Availability
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science

Cite this

Evaluation of creatine transport using Caco-2 monolayers as an in vitro model for intestinal absorption. / Dash, Alekha K.; Miller, Donald W.; Huai-Yan, Han; Carnazzo, Joe; Stout, Jeffrey R.

In: Journal of Pharmaceutical Sciences, Vol. 90, No. 10, 2001, p. 1593-1598.

Research output: Contribution to journalArticle

Dash, Alekha K. ; Miller, Donald W. ; Huai-Yan, Han ; Carnazzo, Joe ; Stout, Jeffrey R. / Evaluation of creatine transport using Caco-2 monolayers as an in vitro model for intestinal absorption. In: Journal of Pharmaceutical Sciences. 2001 ; Vol. 90, No. 10. pp. 1593-1598.
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