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In Vitro Evaluation Of Liposomes Containing Bio-enhancers For The Oral Delivery Of Macromolecules.

J. Parmentier, F. Hartmann, G. Fricker
Published 2010 · Chemistry, Medicine

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The aim of this work was to develop a new type of liposomes containing bio-enhancers for oral delivery of hydrophilic macromolecules. The study focused on EPC/cholesterol-based formulations combined with TPGS 1000 and 400, cholylsarcosine (CS), cetylpyridinium chloride (CpCl) and stearylamine (SA) covering a broad range of different types of enhancers. Most of the tested liposomal formulations and enhancers showed neither influence on cell viability in the Alamar Blue® assay nor an increase in lactate dehydrogenase LDH release. But, at a concentration of 1 mM, CpCl exhibited a strong toxicity after 2 h, TPGS 1000 reduced the cell viability at the same concentration after 8h significantly. Only one liposomal formulation with 25% CpCl led to a decrease in viability to 60.0% after 8h at a total lipid concentration of 5 mM. In the Caco-2 Transwell® model, one formulation with 5% TPGS 400 improved the permeation of FITC-dextran 70 kDa 3.34 ± 0.62-fold, one with 10% CpCl 3.69 ± 0.67 and one with 10% CS and 2.5% SA 3.41 ± 0.51-fold without influencing the TER. Liposomes with 10% SA or 25% CpCl increased the permeation of FITC-dextran 29.02 ± 5.84, respectively 39.28 ± 2.10-fold, but led also to a strong reduction in the TER. Especially, the three formulations which enhanced the permeation of FITC-dextran around 3.5-fold without showing any cell toxicity or decrease in TER should be safe and effective candidates for the development of an oral delivery system for hydrophilic macromolecules.
This paper references
An in vitro examination of the impact of polyethylene glycol 400, pluronic P85, and vitamin E d-a-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine
B. Johnson (2008)
Convenient Estimation for Counterion Dissociation of Cationic Micelles Using Chloride-Sensitive Fluorescence Probe
T. Asakawa (2001)
Use of liposomes to aid intestinal absorption of entrapped insulin in normal and diabetic dogs.
H. M. Patel (1982)
Induction of Apoptosis in WEHI 231 Cells by Cationic Liposomes
Y. Aramaki (2004)
Oral delivery of insulin with the eligen technology: mechanistic studies.
D. Malkov (2005)
Physicochemical and physiological properties of cholylsarcosine. A potential replacement detergent for bile acid deficiency states in the small intestine.
J. Lillienau (1992)
C) Means to enhance penetration
E. S. Swenson (1992)
Conjugated bile acid replacement therapy in short bowel syndrome patients with a residual colon.
C. Kapral (2004)
Intestinal absorption of peptides through the enterocytes
E. Ziv (2000)
Automated multi-well device to measure transepithelial electrical resistances under physiological conditions.
J. Wegener (2004)
Screening of cationic compounds as an absorption enhancer for nasal drug delivery.
H. Natsume (1999)
Potentiality of double liposomes containing salmon calcitonin as an oral dosage form.
Kenji Yamabe (2003)
Effect of replacement therapy with cholylsarcosine on fat malabsorption associated with severe bile acid malabsorption
S. Longmire-Cook (2005)
Influence of vitamin E TPGS poly(ethylene glycol) chain length on apical efflux transporters in Caco-2 cell monolayers.
E. Collnot (2006)
Biocompatibility index of antiseptic agents by parallel assessment of antimicrobial activity and cellular cytotoxicity.
G. Müller (2008)
Chitosan-N-acetyl cysteine conjugates: in vitro evaluation of permeation enhancing and P-glycoprotein inhibiting properties.
T. Schmitz (2008)
Absorption enhancement through intracellular regulation of tight junction permeability by medium chain fatty acids in Caco-2 cells.
T. Lindmark (1998)
Mechanistic analysis for drug permeation through intestinal membrane.
M. Hayashi (2007)
Caveolae: An Alternative Membrane Transport Compartment
M. Gumbleton (2004)
A mechanistic analysis of carrier-mediated oral delivery of protein therapeutics.
B. R. Stoll (2000)
D-alpha-tocopheryl polyethylene glycol 1000 succinate (tpgs) in use for food for particular nutritional purposes
E.F.S. Authority (2007)
The cationic lipid stearylamine reduces the permeability of the cationic drugs verapamil and prochlorperazine to lipid bilayers: implications for drug delivery.
M. Webb (1995)
Transport, metabolism, and effect of chronic feeding of cholylsarcosine, a conjugated bile acid resistant to deconjugation and dehydroxylation.
A. Schmassmann (1990)
Nanoparticles as potential oral delivery systems of proteins and vaccines: a mechanistic approach.
A. des Rieux (2006)
Intestinal drug absorption enhancement: an overview.
E. J. van Hoogdalem (1989)
Oral delivery of peptide drugs: barriers and developments.
J. Hamman (2005)
Enteric‐coated cholylsarcosine microgranules for the treatment of short bowel syndrome
T. Fürst (2005)
Dextran sulfate-dependent fusion of liposomes containing cationic stearylamine.
O. Zschörnig (1992)
Investigation of the micellar properties of the tocopheryl polyethylene glycol succinate surfactants TPGS 400 and TPGS 1000 by steady state fluorometry.
M. Sadoqi (2009)
Gastrointestinal uptake of liposomes
C. Chiang (1987)
Enhanced oral bioavailability of paclitaxel by D-alpha-tocopheryl polyethylene glycol 400 succinate in mice.
P. Ho (2008)
Surface charge effects upon membrane transport processes: the effects of surface charge on the monensin-mediated transport of lithium ions through phospholipid bilayers studied by 7Li-NMR spectroscopy.
F. Riddell (1988)
Application of surface-coated liposomes for oral delivery of peptide: effects of coating the liposome's surface on the GI transit of insulin.
K. Iwanaga (1999)
Intestinal permeability enhancement for proteins
E. Swenson (1992)
Caveolae, DIGs, and the dynamics of sphingolipid-cholesterol microdomains.
T. Harder (1997)
Gastrointestinal uptake of liposomes. II. In vivo studies
Chia-Ming Chiang (1987)
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.
C. Lipinski (2001)
Diffusion of univalent ions across the lamellae of swollen phospholipids.
A. Bangham (1965)
Enhanced intestinal absorption of salmon calcitonin (sCT) from proliposomes containing bile salts.
Keon-Hyoung Song (2005)
Clathrin-mediated endocytosis of FITC-albumin in alveolar type II epithelial cell line RLE-6TN.
R. Yumoto (2006)
Solubilization of negatively charged DPPC/DPPG liposomes by bile salts.
A. Hildebrand (2004)
Stearylamine-bearing cationic liposomes kill Leishmania parasites through surface exposed negatively charged phosphatidylserine.
Antara Banerjee (2008)
d-alpha-Tocopheryl poly(ethylene glycol) 1000 succinate. Acute toxicity, subchronic feeding, reproduction, and teratologic studies in the rat.
W. Krasavage (1977)
Current Concepts in Intestinal Peptide Absorption
G. Fricker (1996)
Effect of extrusion pressure and lipid properties on the size and polydispersity of lipid vesicles.
D. G. Hunter (1998)
Improvement of intestinal peptide absorption by a synthetic bile acid derivative, cholylsarcosine.
S. Michael (2000)
The effect of various liposome formulations on insulin penetration across Caco-2 cell monolayer.
Z. Değim (2004)
Functional dissociation of paracellular permeability and transepithelial electrical resistance and disruption of the apical- basolateral intramembrane diffusion barrier by expression of a mutant tight junction membrane protein
M. Balda (1996)
Toxicity of non-drug-containing liposomes for cultured human cells.
E. Mayhew (1987)
Intestinal permeation enhancers.
B. Aungst (2000)
Effect of permeation enhancers on buccal absorption.
S. Burgalassi (2006)
Caveolae--an alternative endocytotic pathway for targeted drug delivery.
G. Báthori (2004)
Cationic detergent/sterol mixtures can form fluid lamellar phases and stable unilamellar vesicles.
Thida Phoeung (2009)
T. Harder (1997)
Enhancement of the intestinal absorption of peptides and nonpeptides
B. Aungst (1996)
Absorption-Enhancing Effects of Sodium Caprate and Palmitoyl Carnitine in Rat and Human Colons
T. Shimazaki (2004)
Cytotoxicity of potential ocular permeation enhancers evaluated on rabbit and human corneal epithelial cell lines.
S. Burgalassi (2001)
Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers.
B. Rege (2002)
The chronic toxicity of octadecylamine in the rat--a supplemental report.
W. E. Macdonald (1962)
Bile acid malabsorption: mechanisms and treatment.
S. Eusufzai (1995)
E . F . S . Authority , D - alpha - tocopheryl polyethylene glycol 1000 succinate ( tpgs ) in use for food for particular nutritional purposes
O. Orwar Jesorka (2008)
Transcellular and paracellular contribution to transport processes in the colorectal route
M. Hayashi (1997)
Intestinal permeability enhancement for proteins , peptides and other polar drugs : mechanisms and potential toxicity
W. Curatolo Swenson (1992)
Safe and Effective Permeation Enhancers for Oral Drug Delivery
K. Whitehead (2007)
Cell cultures as models for drug absorption across the intestinal mucosa.
P. Artursson (1991)
Liposomes: technologies and analytical applications.
A. Jesorka (2008)
Investigating the uptake and intracellular fate of pH-sensitive liposomes by flow cytometry and spectral bio-imaging.
U. Huth (2006)
Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity.
E. Collnot (2007)

This paper is referenced by
Oral drug delivery research in Europe.
R. Mrsny (2012)
TPGS-chitosome as an effective oral delivery system for improving the bioavailability of Coenzyme Q10.
Yating Shao (2015)
Formulation and transport properties of tenofovir loaded liposomes through Caco-2 cell model
A. Zidan (2013)
The characterization, pharmacokinetic, and tissue distribution studies of TPGS-modified artesunate liposome in rats
C. Hu (2018)
Effect of the non-ionic surfactant Poloxamer 188 on passive permeability of poorly soluble drugs across Caco-2 cell monolayers.
S. M. Fischer (2011)
Oral nanocrystal formulations and their biopharmaceutical characterization
K. Anhalt (2012)
Carboxymethyl-chitosan-tethered lipid vesicles: hybrid nanoblanket for oral delivery of paclitaxel.
Nitin Joshi (2013)
University of Southern Denmark Effect of the non-ionic surfactant Poloxamer 188 on passive permeability of poorly soluble drugs across Caco-2 cell monolayers Fischer, Sarah; Brandl, Martin
S. M. Fischer (2011)
Lipophilic peptide character - What oral barriers fear the most.
O. Zupančič (2017)
Liposomes containing lipids from Sulfolobus islandicus withstand intestinal bile salts: An approach for oral drug delivery?
S. M. Jensen (2015)
Preparation and evaluation of a novel oral delivery system for low molecular weight heparin
N. Lavanya (2016)
Thiomer-coated liposomes harbor permeation enhancing and efflux pump inhibitory properties
K. Gradauer (2013)
Adapting liposomes for oral drug delivery
Haisheng He (2019)
Formulation and advantages of furazolidone in liposomal drug delivery systems.
Muhammad Irfan Alam (2016)
Strategies for the enhanced intracellular delivery of nanomaterials
Cláudia Azevedo (2018)
Improved oral bioavailability of breviscapine via a Pluronic P85‐modified liposomal delivery system
Y. Zhou (2014)
Microcontainers for oral insulin delivery - in vitro studies of permeation enhancement.
Jacob Rune Jørgensen (2019)
Microfluidic platform for impedance characterization of endothelial cells under fluid shear stress.
V. Velasco (2016)
Comparative study of Pluronic(®) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats.
Dan Chen (2013)
Syddansk Universitet Effect of the non-ionic surfactant Poloxamer 188 on passive permeability of poorly soluble drugs across Caco-2 cell monolayers
S. M. Fischer (2011)
Improved oral bioavailability of human growth hormone by a combination of liposomes containing bio-enhancers and tetraether lipids and omeprazole.
J. Parmentier (2014)
Theranostic liposomes of TPGS coating for targeted co-delivery of docetaxel and quantum dots.
M. Muthu (2012)
Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
K. Gradauer (2012)
Vitamin E TPGS as a molecular biomaterial for drug delivery.
Zhiping Zhang (2012)
Physicochemical characterization and in vitro permeation of an indirubin derivative.
Nasim Heshmati (2013)
Effects of polyphenols on vasomodulatory factors and associated cell signalling
M. Woodcock (2013)
Drug-permeability and transporter assays in Caco-2 and MDCK cell lines.
D. Volpe (2011)
Utilization of chitosan-caged liposomes to push the boundaries of therapeutic delivery.
Sonia Alavi (2017)
Vitamin E TPGS coated liposomes enhanced cellular uptake and cytotoxicity of docetaxel in brain cancer cells.
M. Muthu (2011)
Matrix liposomes: A solid liposomal formulation for oral administration
S. Pantze (2014)
Comparison of liposomal and NLC (nanostructured lipid carrier) formulations for improving the transdermal delivery of oxaprozin: Effect of cyclodextrin complexation.
N. Mennini (2016)
Lipid-based nanocarriers for the oral administration of biopharmaceutics.
T. Karamanidou (2016)
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