← Back to Search
In Vitro Lipolysis Tests On Lipid Nanoparticles: Comparison Between Lipase/co-lipase And Pancreatic Extract
V. Jannin, E. Dellera, S. Chevrier, Yann Chavant, C. Voutsinas, Cristina Bonferoni, F. Demarne
Published 2015 · Medicine, Chemistry
Download PDFAnalyze on Scholarcy
Abstract Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLC) are lipid nanocarriers aimed to the delivery of drugs characterized by a low bioavailability, such as poorly water-soluble drugs and peptides or proteins. The oral administration of these lipid nanocarriers implies the study of their lipolysis in presence of enzymes that are commonly involved in dietary lipid digestion in the gastrointestinal tract. In this study, a comparison between two methods was performed: on one hand, the lipase/co-lipase assay, commonly described in the literature to study the digestion of lipid nanocarriers, and on the other hand, the lipolysis test using porcine pancreatic extract and the pH-stat apparatus. This pancreatic extract contains both the pancreatic lipase and carboxyl ester hydrolase (CEH) that permit to mimic in a biorelevant manner the duodenal digestive lipolysis. The test was performed by means of a pH-stat apparatus to work at constant pH, 5.5 or 6.25, representing respectively the fasted or fed state pH conditions. The evolution of all acylglycerol entities was monitored during the digestion by sampling the reaction vessel at different time points, until 60 min, and the lipid composition of the digest was analyzed by gas chromatography. SLN and NLC systems obtained with long-chain saturated acylglycerols were rapidly and completely digested by pancreatic enzymes. The pH-stat titration method appears to be a powerful technique to follow the digestibility of these solid lipid-based nanoparticles.
This paper references
Nanostructured lipid carriers (NLCs) versus solid lipid nanoparticles (SLNs) for topical delivery of meloxicam
R. Khalil (2014)
Toward the Establishment of Standardized In Vitro Tests for Lipid-Based Formulations. 5. Lipolysis of Representative Formulations by Gastric Lipase
Jean-Claude Bakala-N’Goma (2014)
Toward the establishment of standardized in vitro tests for lipid-based formulations, part 4: proposing a new lipid formulation performance classification system.
Hywel D Williams (2014)
Chitosan-associated SLN: in vitro and ex vivo characterization of cyclosporine A loaded ophthalmic systems
G. Sandri (2010)
Secretion and contribution to lipolysis of gastric and pancreatic lipases during a test meal in humans.
F. Carrière (1993)
Chitosan-coated solid lipid nanoparticles for insulin delivery.
P. Fonte (2012)
Lipid-based colloidal carriers for peptide and protein delivery – liposomes versus lipid nanoparticles
S. Martins (2007)
Lipid Nanoparticles with a Solid Matrix (SLN®, NLC®, LDC®) for Oral Drug Delivery
M. Muchow (2008)
Influence of lipid physical state on the in vitro digestibility of emulsified lipids.
Lucile Bonnaire (2008)
Further biochemical characterization of human pancreatic lipase-related protein 2 expressed in yeast cells Published, JLR Papers in Press, March 30, 2007.
C. Eydoux (2007)
Bile salt‐stimulated lipase in human milk
L. Bläckberg (1993)
Specific assay of carboxyl ester hydrolase using PEG esters as substrate
Sylvie Fernandez (2010)
Comparative study on digestive lipase activities on the self emulsifying excipient Labrasol, medium chain glycerides and PEG esters.
S. Fernandez (2007)
A retinyl palmitate-loaded solid lipid nanoparticle system: effect of surface modification with dicetyl phosphate on skin permeation in vitro and anti-wrinkle effect in vivo.
H. S. Jeon (2013)
A sensitive method for the determination of free fatty acids in plasma.
W. T. Hron (1981)
Lipase degradation of Dynasan 114 and 116 solid lipid nanoparticles (SLN)--effect of surfactants, storage time and crystallinity.
C. Olbrich (2002)
Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: method parameterization and comparison of in vitro digestion profiles across a range of representative formulations.
H. Williams (2012)
Understanding the lipid-digestion processes in the GI tract before designing lipid-based drug-delivery systems.
J. Bakala N'Goma (2012)
New approach to improve encapsulation and antitumor activity of doxorubicin loaded in solid lipid nanoparticles.
S. V. Mussi (2013)
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)
2-Hydroxypropyl-beta-cyclodextrin-modified SLN of paclitaxel for overcoming p-glycoprotein function in multidrug-resistant breast cancer cells
JS Baek (2013)
Influence of particle size on the in vitro digestibility of protein-coated lipid nanoparticles.
E. Troncoso (2012)
Two novel human pancreatic lipase related proteins, hPLRP1 and hPLRP2. Differences in colipase dependence and in lipase activity.
T. Giller (1992)
Physiology of Gastrointestinal Lipolysis and Therapeutical Use of Lipases and Digestive Lipase Inhibitors
H. Lengsfeld (2005)
Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations.
R. Mueller (2002)
Characterization of pancreatic lipase-related protein 2 isolated from human pancreatic juice.
J. De Caro (2004)
Physicochemical techniques for solid lipid nanoparticles: principles and limitations. Drug Dev Indus Pharm
N Kathe (2014)
Physicochemical techniques for solid lipid nanoparticles: principles and limitations
N Kathe (2014)
Lipolysis of the semi-solid self-emulsifying excipient Gelucire 44/14 by digestive lipases.
S. Fernandez (2008)
Lipid nanoparticles with a solid matrix (SLN, NLC, LDC) for oral drug delivery.
M. Muchow (2008)
Importance of human gastric lipase for intestinal lipolysis: an in vitro study.
Y. Gargouri (1986)
Physicochemical characterization techniques for solid lipid nanoparticles: principles and limitations
N. Kathe (2014)
Anew approach to improve encapsulation and antitumor activity of doxorubicin loaded in solid lipid nanoparticles
SV Mussi (2013)
In vitro digestion of curcuminoid-loaded lipid nanoparticles
Andreas Noack (2012)
Resveratrol-loaded solid lipid nanoparticles versus nanostructured lipid carriers: evaluation of antioxidant potential for dermal applications
E. Gokce (2012)
'Stealth' lipid-based formulations: poly(ethylene glycol)-mediated digestion inhibition improves oral bioavailability of a model poorly water soluble drug.
O. Feeney (2014)
In Vitro Gastrointestinal Lipolysis of Four Formulations of Piroxicam and Cinnarizine with the Self Emulsifying Excipients Labrasol® and Gelucire® 44/14
S. Fernandez (2009)
Pancreatic lipase-related protein 1 (PLRP1) is present in the pancreatic juice of several species.
J. De Caro (1998)
In Vitro Digestion of the Self-Emulsifying Lipid Excipient Labrasol® by Gastrointestinal Lipases and Influence of its Colloidal Structure on Lipolysis Rate
S. Fernandez (2013)
Stealth’ lipidbased formulations: poly(ethylene glycol)-mediated digestion inhibition improves oral bioavailability of a model poorly water soluble drug
OM Feeney (2014)
2‐Hydroxypropyl‐β‐cyclodextrin‐modified SLN of paclitaxel for overcoming p‐glycoprotein function in multidrug‐resistant breast cancer cells
J. Baek (2013)
Studies on the substrate specificity of a carboxyl ester hydrolase from human pancreatic juice. I. Action on carboxyl esters, glycerides and phospholipids.
D. Lombardo (1980)
Fatty acids generated by gastric lipase promote human milk triacylglycerol digestion by pancreatic colipase-dependent lipase.
S. Bernbäck (1989)
This paper is referenced by
Evaluation of the digestibility of solid lipid nanoparticles of glyceryl dibehenate produced by two techniques: Ultrasonication and spray‐flash evaporation
Vincent Jannin (2018)
Novel strategies in the oral delivery of antidiabetic peptide drugs – Insulin, GLP 1 and its analogs
R. Ismail (2017)
Mammalian gastrointestinal tract parameters modulating the integrity, surface properties, and absorption of food‐relevant nanomaterials
Susann Bellmann (2015)
Advances on the formulation of proteins using nanotechnologies
Irene Santalices (2017)
Lipid-based nanocarriers for oral peptide delivery.
Zhigao Niu (2016)
Solid lipid nanoparticles for oral drug delivery
S. K. Basha (2020)
Solid lipid nanoparticles modified with amphipathic chitosan derivatives for improved stability in the gastrointestinal tract
Suping Qiu (2018)
Observation of chitosan coated lipid nanoparticles with different lipid compositions under simulated in vitro digestion system
G. H. Shin (2018)
In Vitro Study for Lipolysis of Soybean Oil, Pomegranate Oil, and Their Blended and Interesterified Oils under a pH-Stat Model and a Simulated Model of Small Intestinal Digestion
Chenming Ji (2019)
Lipid-based nanosuspensions for oral delivery of peptides, a critical review.
Camille Dumont (2018)
Spray congealed lipid microparticles for the local delivery of &bgr;‐galactosidase to the small intestine
Serena Bertoni (2018)
Factors affecting the bioaccessibility of β-carotene in lipid-based microcapsules: Digestive conditions, the composition, structure and physical state of microcapsules
Quanquan Lin (2017)
Development of a New Ex Vivo Lipolysis-Absorption Model for Nanoemulsions
L. Xiao (2019)