Absorption-Enhancing Effects of Sodium Caprate and Palmitoyl Carnitine in Rat and Human Colons

doi:10.1023/A:1018835829643

Paper

Absorption-Enhancing Effects of Sodium Caprate and Palmitoyl Carnitine in Rat and Human Colons

Published Mar 1, 1998 · T. Shimazaki, M. Tomita, S. Sadahiro

Digestive Diseases and Sciences

Q1 SJR score

42

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1

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Abstract

We examined the enhancing action of sodiumcaprate and palmitoylcarnitine on the permeability offluorescein isothiocyanate dextran 4000 as aparacellular permeant compound in isolated rat and humancolon samples using the Ussing-type chamber method.In the absence of an enhancer, the permeation clearanceof fluorescein isothiocyanate dextran 4000 was notsignificantly different in the rat and human colons, but the electric membrane resistance wassmaller in the rat colon than in the human colon. Sodiumcaprate and palmitoylcarnitine increased permeationclearance and decreased electric membrane resistance in both types of colonic membrane, showing thatthe rat colon can be used as a model of the human colonfor studies of enhancer effects. A calmodulin antagonistsignificantly inhibited the action of sodium caprate in both colonic membranes. However, ittended to promote the effects of palmitoylcarnitine onpermeation clearance and electric membrane resistance.These results suggest that sodium caprate induces the contraction of the perijunctionalactomyosin ring to widen the tight junction and that themechanism of palmitoylcarnitine is different from thatof sodium caprate in the human colon, as reportedpreviously for Caco-2 cell monolayers.

In Vitro Study

Study Snapshot

Sodium caprate and palmitoylcarnitine enhance permeation clearance and decrease electric membrane resistance in both rat and human colons, with palmitoylcarnitine having a different mechanism in the human colon.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

Absorption-Enhancing Effects of Sodium Caprate and Palmitoyl Carnitine in Rat and Human Colons

References

Absorption-enhancing mechanism of EDTA, caprate, and decanoylcarnitine in Caco-2 cells.

EDTA activates PKC by depleting extracellular calcium, caprate increases intracellular calcium levels, and decanoylcarnitine interacts with the apical membrane to increase intracellular calcium levels in Caco-2 cells.

Absorption-enhancing mechanism of sodium caprate and decanoylcarnitine in Caco-2 cells.

Sodium caprate enhances absorption in Caco-2 cells by activating phospholipase C, while decanoylcarnitine enhances absorption through different mechanisms.

In vitro and in vivo analysis of the mechanism of absorption enhancement by palmitoylcarnitine.

Palmitoylcarnitine enhances drug absorption across intestinal mucosa by loosening tight junctions without disrupting actin filament distribution.

Sodium Caprate Elicits Dilatations in Human Intestinal Tight Junctions and Enhances Drug Absorption by the Paracellular Route

Sodium caprate increases drug absorption mainly by the paracellular route, causing dilatations in human intestinal tight junctions.

In vitro effects of long-chain acylcarnitines on the permeability, transepithelial electrical resistance and morphology of rat colonic mucosa.

Long-chain acylcarnitines enhance drug absorption through two different concentration-dependent pathways in rat colonic mucosa, with palmitoyl and lauroyl carnitine showing the best recovery of transepithelial electrical resistance.

Citations

Comparison of the effects of the intestinal permeation enhancers, SNAC and sodium caprate (C10): isolated rat intestinal mucosae and sacs.

SNAC and C10 are both effective intestinal permeation enhancers with low potency and toxic potential, in agreement with clinical trial data.

Investigations of Piperazine Derivatives as Intestinal Permeation Enhancers in Isolated Rat Intestinal Tissue Mucosae

1-4-MPPZ shows the most promise as an intestinal permeation enhancer, but multiple mechanisms of action may impact intestinal physiology.

Regulation of the intestinal barrier by nutrients: The role of tight junctions

Dietary factors may regulate the intestinal tight junction barrier, potentially preventing and reducing inflammation in various disorders.

The Leak Pathway: A Pathway in Flux

The Leak Pathway mediates the movement of large solutes in epithelial cells, but its molecular mechanism, regulation, and potential size limit remain in flux.

Intestinal Permeation Enhancers for Oral Delivery of Macromolecules: A Comparison between Salcaprozate Sodium (SNAC) and Sodium Caprate (C10)

There is no clear scientific advantage between SNAC and C10 for oral delivery of poorly permeable macromolecules, and formulation, manufacturing, and commercial considerations should drive decision-making.