Intestinal drug absorption enhancement: An overview

Hoogdalem, Ewoud J. van; Boer, Albertus G. de; Breimer, D. D.

doi:10.1016/0163-7258(89)90009-0

Cited by 115 publications

(37 citation statements)

References 273 publications

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“…Nevertheless, Odle et al (1991), studying the metabolism of even-and odd-C MCFA as Na salts (1 mmol/l) in isolated piglet hepatocytes, did not mention any alterations. However several authors warned of epithelial cell damage and disorders in phospholipid bilayers and membranes by MCFA and related compounds (Wargovich et al 1984;Van Hoogdalem et al 1989;Bergner & Sommer, 1994;Shima et al 1998Shima et al , 1999Kimura et al 2001). Kanai & Kondo (1979) concluded that, because MCFA and their acylglycerols are anionic surface-active compounds, in vitro cytotoxicity and membrane disorders and perturbations in tissue culture cells can occur.…”

Section: Effects On the Gastrointestinal Mucosa And Physiologymentioning

confidence: 99%

The combined use of triacylglycerols containing medium-chain fatty acids and exogenous lipolytic enzymes as an alternative to in-feed antibiotics in piglets: concept, possibilities and limitations. An overview

Decuypere

Dierick²

2003

Nutr. Res. Rev.

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In the search for alternatives to banned in-feed antibiotics, a concept was developed based on studies with medium-chain fatty acid-containing triacylglycerols (MCTAG) and selected lipases for in situ generation of diacylglycerols, monoacylglycerols and medium-chain fatty acids (MCFA) in the stomach and proximal gut of piglets. MCFA are known to have strong antibacterial properties but can hardly be used as such because of their repellent odour and taste. Those problems could be overcome by the generation of MCFA in situ. The concept was tested in vitro and validated in vivo with gastric-cannulated piglets and under field conditions, including effects on zootechnical performance, with classical antibacterial growth promoters or organic acids acting as positive controls. Furthermore, the metabolic and dietary constraints on the nutritional and nutritive use of MCTAG and/or MCFA (for example, the effects on digestive physiology, gut flora, feed intake, performance, carcass composition) are reviewed. The role of natural preduodenal lipase activity, the presence of endogenous plant lipase activity in raw materials and the feasibility for exogenous lipase addition to the feed are discussed, in order to optimize the concept. The present review illustrates the similarity of the action of MCFA and commonly used antimicrobials on the flora (total flora, Gram-positive flora, Gram-negative flora, potential pathogens) and epithelial morphology and histology in the foregut. These observations are believed to be the basis for obtaining optimal growth performances. In addition, these naturally occurring antimicrobial agents have little or no human or animal toxicity and induce no problems of residues and cross-resistance induction. They are proposed as a valuable alternative to in-feed antibiotics, used for growth promotion, and even for the preventive and curative treatment of gastrointestinal diseases.

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Section: Effects On the Gastrointestinal Mucosa And Physiologymentioning

confidence: 99%

The combined use of triacylglycerols containing medium-chain fatty acids and exogenous lipolytic enzymes as an alternative to in-feed antibiotics in piglets: concept, possibilities and limitations. An overview

Decuypere

Dierick²

2003

Nutr. Res. Rev.

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“…The effects of surfactants on intestinal permeability are usually studied either in situ or in excised intestinal segments [8]. These models provide important information on the interaction between surfactants and the intestinal epithelial barrier.…”

Section: Introductionmentioning

confidence: 99%

Surfactants Enhance the Tight-Junction Permeability of Food Allergens in Human Intestinal Epithelial Caco-2 Cells

Mine

Zhang²

2003

Int Arch Allergy Immunol

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Background: Food additives are responsible for certain allergic types of symptoms. Here Caco-2 cell monolayers were used as a model of the intestinal epithelium for the study of the effect of a food grade surfactant. We determined whether or not the presence of a surfactant enhances the transportation of food allergens across human intestinal epithelial Caco-2 cells. Methods: This study investigated sucrose monoester fatty acids, which are a food grade surfactant. As an in vitro model of human epithelial cells, Caco-2 cells were grown in monolayers and exposed to different doses of the surfactant in conjunction with ovomucoid, a major egg white allergen. The integrity of the monolayer was assessed by measuring transepithelial electrical resistance (TEER). The permeability of tight junctions and transport of the antigen were studied. Results: TEER correlated with the permeability of tight junctions. TEER significantly decreased upon exposure to a surfactant, indicating anincrease in ovomucoid permeability without degradation. The surfactant induced shortening in microvilli, actin disbandmentand structural separation of tight junctions. The results indicate that food grade surfactants can increase the paracellular uptake of food allergens.

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“…If such peptides were absorbed, and a number of factors are now recognized to enhance intestinal 'permeability' to small and medium-sized molecules (e.g. van Hoogdalem, de Boer & Breimer, 1989), they might exert activity in peripheral tissues (e.g. Gardner, 1985).…”

Section: Introductionmentioning

confidence: 99%

Intestinal absorption of the intact peptide carnosine in man, and comparison with intestinal permeability to lactulose.

Gardner

Illingworth

Kelleher

et al. 1991

The Journal of Physiology

139

107

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SUMMARY Healthy humans ingested the dipeptide carnosine (L-/I-alanyl-L-histidine).Their plasma levels and urinary outputs of carnosine and ,8-alanine were monitored over the following 5 h.2. Large amounts of intact carnosine (up to 14 % of the ingested dose) were recovered in the urine over the 5 h after ingestion. However, carnosine was undetectable in the plasma unless precautions were taken to inhibit blood carnosinase activity ex vivo during and after blood collection.3. The amount of carnosine recovered in urine varied substantially between subjects. It correlated negatively with carnosinase enzymic activity in the plasma. Highest carnosinase activities were observed in those subjects who regularly underwent physical training.4. Urinary recovery of the disaccharide lactulose also varied considerably between subjects, but was substantially lower than that of carnosine. There was no significant correlation between the recoveries of carnosine and lactulose. 5. When lactulose was ingested with a hypertonic solution, the urinary recovery of lactulose was generally increased. When carnosine was ingested with a hypertonic solution, the urinary recovery of carnosine was reduced: hence the paracellular route probably is not dominant for absorption of intact carnosine.6. Intact carnosine must have crossed the intestine to an extent much greater than hitherto recognized. Rapid post-absorptive hydrolysis is a severe obstacle to quantification of intact peptide absorption.

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Intestinal drug absorption enhancement: An overview

Cited by 115 publications

References 273 publications

The combined use of triacylglycerols containing medium-chain fatty acids and exogenous lipolytic enzymes as an alternative to in-feed antibiotics in piglets: concept, possibilities and limitations. An overview

The combined use of triacylglycerols containing medium-chain fatty acids and exogenous lipolytic enzymes as an alternative to in-feed antibiotics in piglets: concept, possibilities and limitations. An overview

Surfactants Enhance the Tight-Junction Permeability of Food Allergens in Human Intestinal Epithelial Caco-2 Cells

Intestinal absorption of the intact peptide carnosine in man, and comparison with intestinal permeability to lactulose.

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