Please confirm you are human (Sign Up for free to never see this)
← Back to Search
In Vitro Lipolysis Models As A Tool For The Characterization Of Oral Lipid And Surfactant Based Drug Delivery Systems.
A. T. Larsen, P. Sassene, A. Müllertz
Published 2011 · Chemistry, Medicine
Save to my Library
Download PDFAnalyze on Scholarcy
With the increasing interest in lipid and surfactant based drug delivery systems (LSBDDS) for oral delivery of poorly soluble drugs, the need for efficient development tools is emerging. In vitro lipolysis models, simulating the digestion in the small intestine, is a promising tool in this regard. Several different in vitro lipolysis models have been used for characterization of LSBDDS, all using porcine pancreatin as lipase source, and primarily differing in the addition scheme of calcium and the kind of bile acids employed. Both calcium and bile influence the lipolysis. Calcium have been used both as fixed addition at the beginning of the experiment and with a continuous addition during lipolysis. Both pure bile acids and crude porcine bile extract have been used. Lipolysis of LSBDDS will generate mixed micelles, as well as lamellar and hexagonal phases. These have been characterized by dynamic light scattering, cryogenic transmission electron microscopy and small angle X-ray scattering. The faith of drug during in vitro digestion of a LSBDDS is often studied by ultracentrifugation and quantification of drug in the different phases formed. Further, drug precipitated during in vitro lipolysis has been characterized by X-ray powder diffraction and polarized light microscopy.
This paper references
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)
A Clinical Single-Pass Perfusion Investigation of the Dynamic in Vivo Secretory Response to a Dietary Meal in Human Proximal Small Intestine
E. Persson (2006)
Secretion and contribution to lipolysis of gastric and pancreatic lipases during a test meal in humans.
F. Carrière (1993)
Effects of droplet size, triacylglycerol composition, and calcium on the hydrolysis of complex emulsions by pancreatic lipase : an in vitro study
M. Armand (1992)
Automated approach to couple solubility with final pH and crystallinity for pharmaceutical discovery compounds.
Christopher Seadeek (2007)
Cryo-electron microscopy of vitrified specimens.
J. Dubochet (1988)
Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols.
J. Christensen (2004)
The Role of Calcium Ions and Bile Salts on the Pancreatic Lipase-Catalyzed Hydrolysis of Triglyceride Emulsions Stabilized with Lecithin
F. J. Álvarez (2004)
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)
Probing drug solubilization patterns in the gastrointestinal tract after administration of lipid-based delivery systems: a phase diagram approach.
Greg A Kossena (2004)
Drug delivery strategies for poorly water-soluble drugs
A. Fahr (2007)
Structure and function of gastro-intestinal lipases
Jonathan Kenneth Embleton (1997)
In vitro-in vivo correlations of self-emulsifying drug delivery systems combining the dynamic lipolysis model and neuro-fuzzy networks.
D. Fatouros (2008)
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)
Quantitation of amorphicity by microcalorimetry
D. Giron (1997)
Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs.
R. N. Gursoy (2004)
Relationships between bile salts hydrophilicity and phospholipid composition in bile of various animal species.
D. Alvaro (1986)
In Vitro Gastrointestinal Lipolysis of Four Formulations of Piroxicam and Cinnarizine with the Self Emulsifying Excipients Labrasol® and Gelucire® 44/14
S. Fernandez (2009)
Characterization of fasted‐state human intestinal fluids collected from duodenum and jejunum
Mariangeles Perez de la Cruz Moreno (2006)
Separation and characterization of the colloidal phases produced on digestion of common formulation lipids and assessment of their impact on the apparent solubility of selected poorly water-soluble drugs.
Greg A Kossena (2003)
What is the True Solubility Advantage for Amorphous Pharmaceuticals?
Bruno C. Hancock (2004)
Simulating fasted human intestinal fluids: understanding the roles of lecithin and bile acids.
E. Soederlind (2010)
Precipitation of a poorly soluble model drug during in vitro lipolysis: characterization and dissolution of the precipitate.
P. Sassene (2010)
Inhibition of human pancreatic lipase-colipase activity by mixed bile salt-phospholipid micelles.
J. Patton (1981)
Watching fat digestion.
J. Patton (1979)
Evaluation of drug precipitation of solubility-enhancing liquid formulations using milligram quantities of a new molecular entity (NME).
Wei-guo Dai (2007)
Evaluation of the in‐vitro digestion profiles of long and medium chain glycerides and the phase behaviour of their lipolytic products
L. Sek (2002)
Biorelevant media simulating fed state intestinal fluids: colloid phase characterization and impact on solubilization capacity.
Karen Kleberg (2010)
Influence of the intermediate digestion phases of common formulation lipids on the absorption of a poorly water-soluble drug.
Greg A Kossena (2005)
Modification of a phospholipid stabilized emulsion interface by bile salt: effect on pancreatic lipase activity.
M. Wickham (1998)
Design of lipid-based formulations for oral administration of poorly water-soluble drugs: precipitation of drug after dispersion of formulations in aqueous solution.
K. Mohsin (2009)
Nano-emulsions and Micro-emulsions: Clarifications of the Critical Differences
N. Anton (2010)
Effect of degree, type, and position of unsaturation on the pKa of long-chain fatty acids.
J. R. Kanicky (2002)
Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems.
C. Pouton (2000)
Biliary secretion of rosuvastatin and bile acids in humans during the absorption phase.
E. Bergman (2006)
Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system.
C. Pouton (2006)
Lipid-based Formulations for Danazol Containing a Digestible Surfactant, Labrafil M2125CS: In Vivo Bioavailability and Dynamic In Vitro Lipolysis
A. Larsen (2008)
Use of a Dynamic in Vitro Lipolysis Model to Rationalize Oral Formulation Development for Poor Water Soluble Drugs: Correlation with in Vivo Data and the Relationship to Intra-Enterocyte Processes in Rats
A. Dahan (2006)
Characterization of the Human Upper Gastrointestinal Contents Under Conditions Simulating Bioavailability/Bioequivalence Studies
L. Kalantzi (2005)
The complete digestion of human milk triacylglycerol in vitro requires gastric lipase, pancreatic colipase-dependent lipase, and bile salt-stimulated lipase.
S. Bernbäck (1990)
Characterising the behaviour of poorly water soluble drugs in the intestine: application of biorelevant media for solubility, dissolution and transport studies
Karen Kleberg (2010)
Colipase-induced reorganization of interfaces as a regulator of lipolysis
H. Brockman (2002)
In Vivo Model for Ciclosporin Intestinal Absorption in Lipid Vehicles
J. Reymond (2004)
Drug Solubilization Behavior During in Vitro Digestion of Simple Triglyceride Lipid Solution Formulations
A. Kaukonen (2004)
Giardia lamblia: the roles of bile, lactic acid, and pH in the completion of the life cycle in vitro.
F. Gillin (1989)
Intraluminal drug and formulation behavior and integration in in vitro permeability estimation: a case study with amprenavir.
J. Brouwers (2006)
Analysis of conjugated and unconjugated bile acids in serum and jejunal fluid of normal subjects.
A. Tangerman (1986)
Structural Development of Self Nano Emulsifying Drug Delivery Systems (SNEDDS) During In Vitro Lipid Digestion Monitored by Small-angle X-ray Scattering
Dimitrios G. Fatouros (2007)
Controlled environment vitrification system: an improved sample preparation technique.
J. Bellare (1988)
Hydrolysis of emulsions with different triglycerides and droplet sizes by gastric lipase in vitro. Effect on pancreatic lipase activity
P. Borel (1994)
Evaluation of the impact of surfactant digestion on the bioavailability of danazol after oral administration of lipidic self-emulsifying formulations to dogs.
Jean F Cuiné (2008)
Characterization of Fluids from the Stomach and Proximal Jejunum in Men and Women
A. Lindahl (2004)
Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: studies with halofantrine.
C. H. Porter (2004)
In vitro assessment of oral lipid based formulations.
C. J. Porter (2001)
The Effects of Food on the Dissolution of Poorly Soluble Drugs in Human and in Model Small Intestinal Fluids
E. M. Persson (2005)
Susceptibility to Lipase-Mediated Digestion Reduces the Oral Bioavailability of Danazol After Administration as a Medium-Chain Lipid-Based Microemulsion Formulation
C. H. Porter (2004)
Colipase enhances hydrolysis of dietary triglycerides in the absence of bile salts.
L. Bläckberg (1979)
New perspectives on lipid and surfactant based drug delivery systems for oral delivery of poorly soluble drugs
A. Müllertz (2010)
Comparative study on digestive lipase activities on the self emulsifying excipient Labrasol, medium chain glycerides and PEG esters.
S. Fernandez (2007)
Influence of lipolysis on drug absorption from the gastro-intestinal tract
Karen J. MacGregor (1997)
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)
A dynamic in vitro lipolysis model. II: Evaluation of the model.
N. H. Zangenberg (2001)
Morphological observations on a lipid-based drug delivery system during in vitro digestion.
D. Fatouros (2007)
Drug Solubilization Behavior During in Vitro Digestion of Suspension Formulations of Poorly Water-Soluble Drugs in Triglyceride Lipids
A. Kaukonen (2004)
Miniaturized Assay for Solubility and Residual Solid Screening (SORESOS) in Early Drug Development
Nicole Wyttenbach (2006)
Lipid digestion and absorption.
M. Carey (1983)
A dynamic in vitro lipolysis model. I. Controlling the rate of lipolysis by continuous addition of calcium.
N. H. Zangenberg (2001)
This paper is referenced by
In vitro digestion testing of lipid-based delivery systems: calcium ions combine with fatty acids liberated from triglyceride rich lipid solutions to form soaps and reduce the solubilization capacity of colloidal digestion products.
R. Devraj (2013)
Comparisons of in vitro Fick’s first law, lipolysis, and in vivo rat models for oral absorption on BCS II drugs in SNEDDS
Jingyi Ye (2019)
Solution or suspension – Does it matter for lipid based systems? In vivo studies of chase dosing lipid vehicles with aqueous suspensions of a poorly soluble drug
A. T. Larsen (2017)
Does the commonly used pH-stat method with back titration really quantify the enzymatic digestibility of lipid drug delivery systems? A case study on solid lipid nanoparticles (SLN).
M. Heider (2016)
Evaluation of gastrointestinal drug supersaturation and precipitation: strategies and issues.
Jan Bevernage (2013)
Biopolymer-coated liposomes by electrostatic adsorption of chitosan (chitosomes) as novel delivery systems for carotenoids
Chen Tan (2016)
Nanostructured lipid carriers versus microemulsions for delivery of the poorly water-soluble drug luteolin.
Ying Liu (2014)
Effect of Lipolysis on Drug Release from Self-microemulsifying Drug Delivery Systems (SMEDDS) with Different Core/Shell Drug Location
J. Zhang (2014)
Biorelevant in‐vitro performance testing of orally administered dosage forms
C. Reppas (2012)
Oral bioavailability of cinnarizine in dogs: relation to SNEDDS droplet size, drug solubility and in vitro precipitation.
A. T. Larsen (2013)
Orally Bioavailable and Effective Buparvaquone Lipid-Based Nanomedicines for Visceral Leishmaniasis.
L. Smith (2018)
An in vitro digestion test that reflects rat intestinal conditions to probe the importance of formulation digestion vs first pass metabolism in Danazol bioavailability from lipid based formulations.
M. U. Anby (2014)
In Vitro Model Simulating Gastro-Intestinal Digestion in the Pediatric Population (Neonates and Young Infants)
Danna Kamstrup (2016)
Successful oral delivery of poorly water-soluble drugs both depends on the intraluminal behavior of drugs and of appropriate advanced drug delivery systems.
B. Boyd (2019)
DESIGN, DEVELOPMENT AND EVALUATION OF FENOFIBRATE AND ROSUVASTATIN NANODROPLETS
R. S. Kumar (2014)
Self‐microemulsifying tablets prepared by direct compression for improved resveratrol delivery
Katarina Bolko Seljak (2018)
Lipid-based formulations for oral administration of poorly water-soluble drugs.
H. Mu (2013)
Recent developments in oral lipid-based drug delivery
Nicky Thomas (2013)
Drug Delivery Using Oral Vehicles: Controlled Release in the GI-tract
Maren Sæther (2012)
In Vitro Lipolysis and Intestinal Transport of β-Arteether-Loaded Lipid-Based Drug Delivery Systems
P. Memvanga (2013)
The gut in the beaker: Missing the surfactants?
C. Wilson (2016)
Quantitative Prediction of Oral Bioavailability of a Lipophilic Antineoplastic Drug Bexarotene Administered in Lipidic Formulation Using a Combined In Vitro Lipolysis/Microsomal Metabolism Approach.
J. B. Lee (2019)
Elucidating the Molecular Interactions Occurring during Drug Precipitation of Weak Bases from Lipid-Based Formulations: A Case Study with Cinnarizine and a Long Chain Self-Nanoemulsifying Drug Delivery System.
P. Sassene (2015)
Nanomedicine: From Concept to Reality
K. R. Rakhimol (2016)
Supersaturated Lipid-Based Formulations to Enhance the Oral Bioavailability of Venetoclax
N. Koehl (2020)
Preparation and characterization of nanoemulsions for the controlled delivery of hydrophobic compounds
Miguel Wulff Pérez (2012)
Solid lipid matrix mediated nanoarchitectonics for improved oral bioavailability of drugs
S. Banerjee (2019)
Nano lipid based carriers for lymphatic voyage of anti-cancer drugs: An insight into the in-vitro, ex-vivo, in-situ and in-vivo study models
Shashank Chaturvedi (2020)
Control of colloidal stability and bioavailability of lipid nanoparticles for oral delivery of food bioactives
Lipid-Based Formulations Can Enable the Model Poorly Water-Soluble Weakly Basic Drug Cinnarizine To Precipitate in an Amorphous-Salt Form During In Vitro Digestion.
J. Khan (2016)
Strategies to Address Low Drug Solubility in Discovery and Development
H. Williams (2013)
A Proof of Concept for 3D Printing of Solid Lipid-Based Formulations of Poorly Water-Soluble Drugs to Control Formulation Dispersion Kinetics
K. Vithani (2019)See more