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In-vitro Evaluation Of Solid Lipid Nanoparticles: Ability To Encapsulate, Release And Ensure Effective Protection Of Peptides In The Gastrointestinal Tract.

Camille Dumont, S. Bourgeois, H. Fessi, Pierre-Yves Dugas, V. Jannin
Published 2019 · Chemistry, Medicine

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Peptides are rarely orally administrated due to rapid degradation in the gastrointestinal tract and low absorption at the epithelial border. The objective of this study was to encapsulate a model water-soluble peptide in biodegradable and biocompatible solid lipid-based nanoparticles, i.e. Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) in order to protect it from metabolic degradation. Leuprolide (LEU) and a LEU-docusate Hydrophobic Ion Pair (HIP) were encapsulated in SLN and NLC by High Pressure Homogenization. The particles were characterized regarding their Encapsulation Efficiency (EE), size, morphology, peptide release in FaSSIF-V2, and protective effect towards proteases. Nanoparticles of 120 nm with platelet structures were obtained. Formation of HIP led to a significant increase in LEU EE. Particle size was moderately affected by the presence of simulated fluids. Nonetheless, an important burst release was observed upon dispersion in FaSSIF-V2. NLC were able to improve LEU-HIP resistance to enzymatic degradation induced by trypsin but presented no advantages in presence of α-chymotrypsin. SLN provided no protection regarding both proteases. Despite an increased amount of encapsulated peptide in solid lipid-based nanoparticles following HIP formation, the important specific surface area linked to their platelet structures resulted in an important peptide release upon dispersion in FaSSIF-V2 and limited protection towards enzymatic degradation.
This paper references
10.1016/j.colsurfb.2014.02.045
Ion pairing with linoleic acid simultaneously enhances encapsulation efficiency and antibacterial activity of vancomycin in solid lipid nanoparticles.
Rahul S. Kalhapure (2014)
10.1016/S1461-5347(98)00075-3
Novel oral drug delivery gateways for biotechnology products: polypeptides and vaccines
D. Brayden (1998)
10.1016/S1872-2067(16)62528-7
Recent advances in immobilized enzymes on nanocarriers
S. Cao (2016)
10.1016/J.IJPHARM.2004.10.014
Solid lipid micro-particles carrying insulin formed by solvent-in-water emulsion-diffusion technique.
M. Trotta (2005)
10.1002/JPS.20243
Effect of the covalent modification with poly(ethylene glycol) on alpha-chymotrypsin stability upon encapsulation in poly(lactic-co-glycolic) microspheres.
I. J. Castellanos (2005)
10.1034/J.1399-3011.1999.00069.X
Characterization and comparison of leuprolide degradation profiles in water and dimethyl sulfoxide.
S. Hall (1999)
10.1016/j.ijpharm.2017.02.019
Hydrophobic ion pairing: Key to highly payloaded self-emulsifying peptide drug delivery systems.
J. Griesser (2017)
10.1016/S0169-409X(01)00105-3
Solid lipid nanoparticles: production, characterization and applications.
W. Mehnert (2001)
10.1016/j.nano.2015.09.004
Nanostructured lipid carriers: Promising drug delivery systems for future clinics.
A. Beloqui (2016)
10.1002/JPS.10413
Influence of emulsifiers on the crystallization of solid lipid nanoparticles.
H. Bunjes (2003)
10.4067/S0717-97072013000400033
POLYETHYLENE GLYCOL EFFECT ON THE TRANSIENT AND STEADY STATE PHASES OF P-NITROPHENYLTRIMETHYL ACETATE HYDROLYSIS CATALYZED BY α-CHYMOTRYPSIN
C. Calderón (2013)
10.1021/BC00022A007
Enzymatic activity of chymotrypsin and its poly(ethylene glycol) conjugates toward low and high molecular weight substrates.
Hsin-Cheng Chiu (1993)
10.1021/AC970634X
Identification of the degradation products of gonadorelin and three analogues in aqueous solution
M. A. Hoitink (1997)
10.3109/10717544.2016.1143056
Development and in vitro evaluation of an oral SEDDS for desmopressin
O. Zupančič (2016)
10.2134/JEQ2009.0462
Nanoparticle aggregation: challenges to understanding transport and reactivity in the environment.
E. M. Hotze (2010)
10.1016/J.IJPHARM.2003.12.016
Preparation and characterization of solid lipid nanoparticles containing peptide.
F. Hu (2004)
10.1016/J.JCONREL.2003.11.012
Investigations on the structure of solid lipid nanoparticles (SLN) and oil-loaded solid lipid nanoparticles by photon correlation spectroscopy, field-flow fractionation and transmission electron microscopy.
K. Jores (2004)
10.1517/17425247.2015.1068287
Self-emulsifying drug delivery systems in oral (poly)peptide drug delivery
G. Leonavičiūtė (2015)
10.1016/j.ejpb.2015.04.013
Effective incorporation of insulin in mucus permeating self-nanoemulsifying drug delivery systems.
T. Karamanidou (2015)
10.1016/j.ijpharm.2017.03.027
Comparison of the protective effect of self-emulsifying peptide drug delivery systems towards intestinal proteases and glutathione.
G. Hetényi (2017)
10.1016/j.colsurfb.2008.12.031
Strategic approaches for improving entrapment of hydrophilic peptide drugs by lipid nanoparticles.
Hong Yuan (2009)
10.1016/S0939-6411(00)00087-4
Solid lipid nanoparticles (SLN) for controlled drug delivery - a review of the state of the art.
R. Mueller (2000)
10.1016/J.IJPHARM.2004.12.030
New surface-modified lipid nanoparticles as delivery vehicles for salmon calcitonin.
M. Garcia-Fuentes (2005)
10.1016/j.ijpharm.2018.01.018
Self-emulsifying peptide drug delivery systems: How to make them highly mucus permeating.
J. Griesser (2018)
10.1039/c5sm02958a
Nanoemulsions: formation, properties and applications.
A. Gupta (2016)
10.1016/j.ijpharm.2018.06.025
Visual validation of the measurement of entrapment efficiency of drug nanocarriers
Yongjiu Lv (2018)
10.1080/02652040701532981
Solid lipid nanoparticles formed by solvent-in-water emulsion–diffusion technique: Development and influence on insulin stability
L. Battaglia (2007)
10.1016/S0378-5173(00)00378-1
Characterisation of a novel solid lipid nanoparticle carrier system based on binary mixtures of liquid and solid lipids.
V. Jenning (2000)
10.1080/02652040010000361
Encapsulation of retinoids in solid lipid nanoparticles (SLN).
V. Jenning (2001)
10.1016/j.ijpharm.2011.02.001
Cryogenic transmission electron microscopy (cryo-TEM) for studying the morphology of colloidal drug delivery systems.
J. Kuntsche (2011)
10.1023/A:1011042627714
Incorporation of the Model Drug Ubidecarenone into Solid Lipid Nanoparticles
H. Bunjes (2004)
10.1155/2011/132435
Peptide-Loaded Solid Lipid Nanoparticles Prepared through Coacervation Technique
Marina Gallarate (2011)
10.1016/S1773-2247(10)50057-1
Cisplatin-loaded SLN produced by coacervation technique
M. Gallarate (2010)
10.1002/BIP.360330608
Enhanced solubility of proteins and peptides in nonpolar solvents through hydrophobic ion pairing
M. Powers (1993)
10.1007/s11095-008-9569-4
Dissolution Media Simulating Conditions in the Proximal Human Gastrointestinal Tract: An Update
E. Jantratid (2008)
10.1016/J.JCIS.2004.10.012
Design and characterization of a new drug nanocarrier made from solid-liquid lipid mixtures.
M. Garcia-Fuentes (2005)
10.1016/J.ADDR.2007.04.007
Solid lipid nanoparticles as a drug delivery system for peptides and proteins.
A. Almeida (2007)
10.1016/j.ijpharm.2016.04.044
Impact of lipases on the protective effect of SEDDS for incorporated peptide drugs towards intestinal peptidases.
G. Leonavičiūtė (2016)
10.1039/c7nr07736j
The stimulation of GLP-1 secretion and delivery of GLP-1 agonists via nanostructured lipid carriers.
N. Shrestha (2018)
10.1016/j.ijpharm.2018.02.038
Lipid-based nanosuspensions for oral delivery of peptides, a critical review.
Camille Dumont (2018)
10.3109/03639045.2014.909840
Physicochemical characterization techniques for solid lipid nanoparticles: principles and limitations
N. Kathe (2014)
10.1080/03639040802130061
Lipid Nanoparticles with a Solid Matrix (SLN®, NLC®, LDC®) for Oral Drug Delivery
M. Muchow (2008)
10.1016/J.COCIS.2011.06.007
Structural properties of solid lipid based colloidal drug delivery systems
H. Bunjes (2011)
10.1016/0378-5173(95)04388-8
Thymopentin in solid lipid nanoparticles
S. Morel (1996)
10.1016/j.ijpharm.2014.05.047
In vivo evaluation of an oral self-microemulsifying drug delivery system (SMEDDS) for leuprorelin.
Fabian Hintzen (2014)



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