Online citations, reference lists, and bibliographies.
← Back to Search

Evaluation Of The In‐vitro Digestion Profiles Of Long And Medium Chain Glycerides And The Phase Behaviour Of Their Lipolytic Products

L. Sek, C. H. Porter, A. Kaukonen, W. Charman
Published 2002 · Chemistry, Medicine

Cite This
Download PDF
Analyze on Scholarcy
An evaluation of the in‐vitro digestion profile and phase behaviour of the common formulation lipids Miglyol 812 (medium chain triglyceride, MCT), Capmul MCM (C8/C10 monoglyceride/diglyceride mixture), soybean oil (long chain triglyceride, LCT) and Maisine 35‐1 (C18 monoglyceride/diglyceride mixture), is described. Experiments were conducted using titrimetric, high‐performance thin‐layer chromatographic (HPTLC) and ultracentrifugational techniques under model fasted and post‐prandial intestinal conditions. The rate and extent of digestion of the medium chain lipids was greater than the corresponding long chain lipids, and independent of bile salt concentration, with complete conversion to monoglyceride and fatty acid occurring after 30 min digestion. The long chain lipid digests separated into an oily phase (containing undigested triglyceride and diglyceride), an aqueous phase (containing bile salt, fatty acid and monoglyceride) and a pellet phase (containing approximately 5 mM of fatty acid, presumably as an insoluble soap) after ultracentrifugation. Higher proportions of long chain fatty acid and monoglyceride were dispersed into the aqueous phase with increasing bile salt concentrations. In contrast, medium chain lipolytic products separated only into an aqueous phase and a pellet fraction in a bile‐salt‐independent manner. The digestion of both the C8/C10 and C18 monoglyceride/diglyceride lipid mixtures was more rapid than the corresponding triglyceride, especially at early time points. This investigation provides insight into the relative digestion kinetics of medium chain and long chain lipids and provides information regarding the phase behaviour of their lipolytic products under conditions modelled on those expected after oral administration. The data also provide a background for improved understanding of the potential utility of long chain and medium chain lipid‐based formulations.
This paper references
Lipid digestion and absorption.
M. Carey (1983)
Formation of lithogenic bile in man.
T. Scherstén (1973)
Combined eŒect of a
A. Lykidis (1997)
The ionic behavior of fatty acids solubilized by bile salts.
W. Shankland (1970)
Coassimilation of dietary fat and benzo(a)pyrene in the small intestine: an absorption model using the killifish.
R. Vetter (1985)
Solubilities of normal aliphatic acids, alcohols and alkanes in water
G. H. Bell (1973)
Physicochemical properties of bile
A. F. Hofmann (1984)
On the mechanism of pancreatic lipolysis of glycerides
B. Borgström (1954)
Study of the oil and micellar phases during fat digestion in the normal child.
C. Ricour (1970)
Competitive inhibitory effect exerted by bile salt micelles on the hydrolysis of tributyrin by pancreatic lipase.
A. Vandermeers (1976)
Binding of bile salts to pancreatic colipase and lipase
B. Borgstrom (2002)
1994)Pancreatic lipase assays
A. Lykidis (1994)
Inhibition of human pancreatic
J. S. Patton (1981)
Characterisation and quantification of medium chain and long chain triglycerides and their in vitro digestion products, by HPTLC coupled with in situ densitometric analysis.
L. Sek (2001)
Lipid digestion
M. C. Carey (1983)
Physical-chemical behavior of dietary and biliary lipids during intestinal digestion and absorption. 2. Phase analysis and aggregation states of luminal lipids during duodenal fat digestion in healthy adult human beings.
O. Hernell (1990)
Binding of bile salts to pancreatic colipase and lipase.
B. Borgström (1975)
Pancreatic Lipase and Co-Lipase
B. Borgström (1973)
Polycyclic hydrocarbon and
J. M. Laher (1983)
Lipid-based vehicles for the oral delivery of poorly water soluble drugs
A. Humberstone (1997)
F. Mattson (1964)
Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine
Shui-Mei Khoo (1998)
1995)Lipid microemulsions for improving drug
P. P. Constantinides (1995)
Intestinal lipid absorption and transport.
Phan Ct (2001)
Lipid Microemulsions for Improving Drug Dissolution and Oral Absorption: Physical and Biopharmaceutical Aspects
P. Constantinides (2004)
Formulation design and bioavailability
W. N. Charman (1998)
Ionization and phase behavior of fatty acids in water: application of the Gibbs phase rule.
D. Cistola (1988)
The behavior and solubility of monoglycerides in dilute, micellar bile-salt solution
A. Hofmann (1963)
Lipid-based vehicles
A. J. Humberstone (1997)
Hydrolysis of long-chain
B. m (1963)
Physicochemical characteristics of emulsions during fat digestion in human stomach and duodenum.
M. Armand (1996)
On the mechanism of pancreatic lipolysis of glycerides.
B. Borgstrom (1954)
Physical-chemical behavior of dietary and biliary lipids during intestinal digestion and absorption. 1. Phase behavior and aggregation states of model lipid systems patterned after aqueous duodenal contents of healthy adult human beings.
J. Staggers (1990)
Influence of lipolysis on drug absorption from the gastro-intestinal tract
Karen J. MacGregor (1997)
Physicochemical properties of bile acids and their relationship to biological properties: an overview of the problem.
A. Hofmann (1984)
EOE ect of phosphatidylcholine and free fatty acids on the activity of pancreatic lipasecolipase
A Larsson (1986)
Effect of phosphatidylcholine and free fatty acids on the activity of pancreatic lipase-colipase.
A. Larsson (1986)
Pancreatic lipase and co-lipase. Interactions and effects of bile salts and other detergents.
B. Borgström (1973)
Digestion and Absorption
O. Koldovský (1978)
EŒect of phosphatidyl
A. Larsson (1986)
Inhibition of human pancreatic lipase-colipase activity by mixed bile salt-phospholipid micelles.
J. Patton (1981)
The Role of Calcium Ions and Bile Salts on the Pancreatic Lipase-Catalyzed Hydrolysis of Triglyceride Emulsions Stabilized with Lecithin
F. J. Álvarez (2004)
Physiochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH.
W. Charman (1997)
Isolation of the aqueous phase of human intestinal contents during the digestion of a fatty meal.
H. P. Porter (1971)
Duodenal bile acids after a test meal.
O. Fausa (1974)
Intestinal lipid absorption and transport.
Cam T Phan (2001)
Arzoglou,P. (1995)Kinetics of the two-step
A. Lykidis (1995)
Pancreatic lipase assays with triglycerides as substrate: contribution of each sequential reaction to product formation.
A. Lykidis (1994)
Hydrolysis of long-chain monoglycerides in micellar solution by pancreatic lipase.
A. Hofmann (1963)
Combined effect of a lecithin and a bile salt on pancreatic lipase activity.
A. Lykidis (1997)
Watching fat digestion.
J. Patton (1979)
Kinetics of the two-step hydrolysis of triacylglycerol by pancreatic lipases.
A. Lykidis (1995)

This paper is referenced by
A comparison of the effect of medium- vs. long-chain triglycerides on the in vitro solubilization of cholesterol and/or phytosterol into mixed micelles
A. Bonsdorff-Nikander (2005)
The effect of different lipid based formulations on the oral absorption of lipophilic drugs: the ability of in vitro lipolysis and consecutive ex vivo intestinal permeability data to predict in vivo bioavailability in rats.
A. Dahan (2007)
Silica-Lipid Hybrid (SLH) Versus Non-lipid Formulations for Optimising the Dose-Dependent Oral Absorption of Celecoxib
A. Tan (2011)
How relevant are assembled equilibrium samples in understanding structure formation during lipid digestion?
Stephanie Phan (2015)
In vitro lipolysis models as a tool for the characterization of oral lipid and surfactant based drug delivery systems.
A. T. Larsen (2011)
Increasing the fat content of pancakes augments the digestibility of starch in-vitro
M. Clegg (2011)
Stable drug encapsulation in micelles and microemulsions.
A. Narang (2007)
Design of functional beverage emulsion systems for improved citral stability and coenzyme Q10 bioavailability
Qin Zhao (2016)
Fabrication of edible biocompatible carbohydrate particle-based Pickering emulsions
Xuanxuan Lu (2017)
Microemulsions as drug delivery systems to improve the solubility and the bioavailability of poorly water-soluble drugs
Cai-Xia He (2010)
Development of a food-grade organogel with high bioaccessibility and loading of curcuminoids
H. Yu (2012)
Tableting lipid-based formulations for oral drug delivery: a case study with silica nanoparticle-lipid-mannitol hybrid microparticles.
K. Bremmell (2013)
Effect of Ingested Lipids on Drug Dissolution and Release with Concurrent Digestion: A Modeling Approach
Fulden Buyukozturk (2013)
Self-nanoemulsifying systems for oral bioavailability enhancement
B. Singh (2015)
Potential applications of lipid nanoparticles in edible packaging and nutraceutical delivery
Annie D'Souza Palaparthi (2016)
Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development
N. Thomas (2012)
Toward the Establishment of Standardized In Vitro Tests for Lipid-Based Formulations, Part 3: Understanding Supersaturation Versus Precipitation Potential During the In Vitro Digestion of Type I, II, IIIA, IIIB and IV Lipid-Based Formulations
H. Williams (2013)
Is there an effect of food on the biliary secretion of cyclosporine and three in vivo formed metabolites in a porcine model
E. M. Persson (2007)
Edible oil nanoemulsion: An organic nanoantibiotic as a potential biomolecule delivery vehicle
Varun Saxena (2018)
Nanoemulsion delivery systems for oil-soluble vitamins: Influence of carrier oil type on lipid digestion and vitamin D3 bioaccessibility.
Bengu Ozturk (2015)
Nanostructuring Biomaterials with Specific Activities towards Digestive Enzymes for Controlled Gastrointestinal Absorption of Lipophilic Bioactive Molecules.
P. Joyce (2016)
Comparison of lipases for in vitro models of gastric digestion: lipolysis using two infant formulas as model substrates.
P. Sassene (2016)
Drug Solubilization Behavior During in Vitro Digestion of Suspension Formulations of Poorly Water-Soluble Drugs in Triglyceride Lipids
A. Kaukonen (2004)
Toward the establishment of standardized in vitro tests for lipid-based formulations. 2. The effect of bile salt concentration and drug loading on the performance of type I, II, IIIA, IIIB, and IV formulations during in vitro digestion.
H. Williams (2012)
Lyophilized silica lipid hybrid (SLH) carriers for poorly water-soluble drugs: physicochemical and in vitro pharmaceutical investigations.
Rokhsana Yasmin (2014)
Colloidal aspects of dispersion and digestion of self-dispersing lipid-based formulations for poorly water-soluble drugs.
K. Vithani (2019)
Slowing down lipolysis significantly enhances the oral absorption of intact solid lipid nanoparticles.
Z. Yu (2019)
A novel excipient, 1-perfluorohexyloctane shows limited utility for the oral delivery of poorly water-soluble drugs.
R. Holm (2011)
Biocatalytic synthesis of ultra-long-chain fatty acid sugar alcohol monoesters
W. Wei (2015)
Nanostructured reverse hexagonal liquid crystals sustain plasma concentrations for a poorly water-soluble drug after oral administration
T. Nguyen (2011)
Functionalized Lipid Particulates in Targeted Drug Delivery
M. Nagarsenker (2015)
Immobilised lipase for in vitro lipolysis experiments.
Stephanie Phan (2015)
See more
Semantic Scholar Logo Some data provided by SemanticScholar