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Biopharmaceutical Characterisation Of Insulin And Recombinant Human Growth Hormone Loaded Lipid Submicron Particles Produced By Supercritical Gas Micro-atomisation.

S. Salmaso, Sara Bersani, N. Elvassore, A. Bertucco, P. Caliceti
Published 2009 · Chemistry, Medicine

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Homogeneous dispersions of insulin and recombinant human growth hormone (rh-GH) in tristearin/phosphatidylcholine/PEG mixtures (1.3:1.3:0.25:0.15 w/w ratio) were processed by supercritical carbon dioxide gas micro-atomisation to produce protein-loaded lipid particles. The process yielded spherical particles, with a 197+/-94 nm mean diameter, and the insulin and rh-GH recovery in the final product was 57+/-8% and 48+/-5%, respectively. In vitro, the proteins were slowly released for about 70-80 h according to a diffusive mechanism. In vivo, the insulin and glucose profiles in plasma obtained by subcutaneous administration of a dose of particles containing 2 microg insulin to diabetic mice overlapped that obtained with 2 microg of insulin in solution. Administration of a dose of particles containing 5 microg insulin resulted in faster and longer glycaemia reduction. Oral administration of 20 and 50 microg insulin equivalent particles produced a significant hypoglycaemic effect. The glucose levels decreased since 2h after administration, reaching about 50% and 70% glucose reduction in 1-2h with the lower and higher dose, respectively. As compared to subcutaneous administration, the relative pharmacological bioavailability obtained with 20 and 50 microg equivalent insulin particles was 7.7% and 6.7%, respectively. Daily subcutaneous administration of 40 microg of rh-GH-loaded particles to hypophysectomised rats induced similar body weight increase as 40 microg rh-GH in solution. The daily oral administration of 400 microg rh-GH equivalent particles elicited a slight body weight increase, which corresponded to a relative pharmacological bioavailability of 3.4% compared to subcutaneous administration.
This paper references
10.1016/J.SUPFLU.2008.06.002
Spherical microparticles production by supercritical antisolvent precipitation: Interpretation of results
E. Reverchon (2008)
Applications of supercritical CO 2 in the fabrication of polymer systems for drug delivery and tissue engineering ☆
O. R. Davies (2008)
10.1016/J.SUPFLU.2008.10.005
Rational design of drug–polymer co-formulations by CO2 anti-solvent precipitation
Johannes Kluge (2009)
10.1016/J.COPBIO.2003.10.007
Drug delivery in biotechnology: present and future.
G. Orive (2003)
10.1002/jps.21434
Production of solid lipid submicron particles for protein delivery using a novel supercritical gas-assisted melting atomization process.
S. Salmaso (2009)
10.1016/J.ADDR.2007.04.007
Solid lipid nanoparticles as a drug delivery system for peptides and proteins.
A. Almeida (2007)
10.1023/A:1007696723125
Design and In Vivo Evaluation of An Oral Delivery System for Insulin
M. Marschütz (2004)
Oral delivery of rhGH : preliminary mechanistic considerations
M. K. Marschütz (2000)
10.1016/J.EJPB.2007.05.007
Preparation and physicochemical characterization of supercritically dried insulin-loaded microparticles for pulmonary delivery.
M. Amidi (2008)
10.1016/J.SUPFLU.2008.10.001
Supercritical fluids processing of polymers for pharmaceutical and medical applications
E. Reverchon (2009)
10.1016/J.ADDR.2006.12.001
Applications of supercritical CO2 in the fabrication of polymer systems for drug delivery and tissue engineering.
O. R. Davies (2008)
Effect of high pressure gases on phase behavior of solid lipids
A. Tandya
10.1016/J.JCONREL.2003.10.015
Effective protein release from PEG/PLA nano-particles produced by compressed gas anti-solvent precipitation techniques.
Paolo Caliceti (2004)
10.1016/j.ejpb.2008.09.003
Lipid nanoparticles for parenteral delivery of actives.
Medha D. Joshi (2009)
10.1016/S0169-409X(98)00072-6
Current status and future prospects of parenteral insulin regimens, strategies and delivery systems for diabetes treatment.
Jeandidier (1999)
10.1016/J.ADDR.2007.08.019
Current challenges in non-invasive insulin delivery systems: a comparative review.
E. Khafagy (2007)
10.1016/J.EJPB.2004.10.006
Strategic approaches for overcoming peptide and protein instability within biodegradable nano- and microparticles.
U. Bilati (2005)
10.1016/0731-7085(89)80080-9
Assays for human growth hormones.
D. Bangham (1989)
10.1016/j.jconrel.2008.11.026
Lipid extrudates as novel sustained release systems for pharmaceutical proteins.
S. Schulze (2009)
10.1016/J.IJPHARM.2006.08.016
Dense gas processing of polymeric controlled release formulations.
Andrian Tandya (2007)
10.1111/J.1365-2621.2002.TB08837.X
Characterization and thermal stability of polymorphic forms of synthesized tristearin
J.‐H. Oh (2002)
10.1007/BF02976925
Protein drug oral delivery: The recent progress
H. J. Lee (2002)
10.1016/J.BEJ.2008.04.001
Design and in vivo evaluation of solid-in-oil suspension for oral delivery of human growth hormone
Hiromu Yoshiura (2008)
10.1016/J.EJPB.2007.07.013
Approval of new biopharmaceuticals 1999-2006: comparison of the US, EU and Japan situations.
K. Tsuji (2008)
10.1016/J.EJPS.2006.05.008
Preparing and evaluating delivery systems for proteins.
L. Jorgensen (2006)
10.1016/S0927-7765(02)00053-X
Design of lipid nanoparticles for the oral delivery of hydrophilic macromolecules
M. Garcia-Fuentes (2003)
ORAL LIPID-BASED FORMULATIONS : BRIDGING THE GAP BETWEEN KNOWLEDGE AND KNOW-HOW
D. Hauss (2007)
10.1038/nm1610
A ligand-receptor fusion of growth hormone forms a dimer and is a potent long-acting agonist
I. Wilkinson (2007)
10.1016/J.IJPHARM.2006.07.026
Lectin-modified solid lipid nanoparticles as carriers for oral administration of insulin.
N. Zhang (2006)
10.1016/J.SUPFLU.2005.11.016
Effect of high-pressure gases on phase behaviour of solid lipids
S. Spilimbergo (2006)
Applications of supercritical CO 2 in the fabrication of polymer systems for drug delivery and tissue engineering
O. R. avies (2008)
10.1016/0168-3659(87)90034-4
A simple equation for description of solute release I. Fickian and non-fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs
P. L. Ritger (1987)
10.1016/S0169-409X(97)00051-3
Recombinant human growth hormone poly(lactic-co-glycolic acid) microsphere formulation development.
Jones (1997)
10.1016/J.IJPHARM.2004.11.014
Protein aggregation and its inhibition in biopharmaceutics.
W. Wang (2005)
10.1016/J.JCONREL.2007.09.013
Nano/micro technologies for delivering macromolecular therapeutics using poly(D,L-lactide-co-glycolide) and its derivatives.
R. C. Mundargi (2008)
10.1016/B0-08-045044-X/00050-X
Peptide and Protein Drugs: Issues and Solutions
J. J. Nestor (2007)
10.1016/J.ADDR.2007.02.002
Application of supercritical fluid to preparation of powders of high-molecular weight drugs for inhalation.
H. Okamoto (2008)
10.1016/J.SUPFLU.2006.01.014
Solubility of carbon dioxide in three lipid-based biocarriers
A. R. Sousa (2006)
10.1016/S0169-409X(01)00105-3
Solid lipid nanoparticles: production, characterization and applications.
W. Mehnert (2001)
10.1016/J.ADDR.2007.09.010
Lipid excipients and delivery systems for pharmaceutical development: a regulatory perspective.
M. Chen (2008)
Nano / microtechnologies for delivering macromolecular therapeutics using poly ( d , l - lactide - co - glycolide ) and its derivatives
J. J. Nestor (2007)
10.1016/J.DRUDIS.2006.08.005
Is the oral route possible for peptide and protein drug delivery?
M. Morishita (2006)



This paper is referenced by
10.3109/10717544.2014.991001
Novel drug delivery system: an immense hope for diabetics
Vineet Kumar Rai (2016)
10.2174/1381612821666150416100943
Characterization of particulate drug delivery systems for oral delivery of Peptide and protein drugs.
Philip Carsten Christophersen (2015)
10.1016/j.jconrel.2017.09.025
Animal models for evaluation of oral delivery of biopharmaceuticals
Stine Harloff-Helleberg (2017)
10.2217/nnm.10.32
Nanoscale particle therapies for wounds and ulcers.
R. Cortivo (2010)
10.1201/B19038-27
Supercritical Fluid Technology for Encapsulation
Ángel Martín (2015)
10.2174/2211738507666190925112942
Scalable Manufacturing Processes for Solid Lipid Nanoparticles.
Giulia Anderluzzi (2019)
10.3390/ma4112017
Dense CO2 as a Solute, Co-Solute or Co-Solvent in Particle Formation Processes: A Review
Ana V. M. Nunes (2011)
10.1186/1556-276X-8-386
Characteristics of lipid micro- and nanoparticles based on supercritical formation for potential pharmaceutical application
Islane Espírito Santo (2013)
Development of a Novel Drug Delivery System to Enhance the Oral Bioavailability of Lactoferrin
Xudong Yao (2015)
10.1016/J.SUPFLU.2015.07.010
Curcumin-loaded solid lipid particles by PGSS technology
A. S. Pedro (2016)
10.1016/j.chroma.2009.12.019
Supercritical fluid extraction: Recent advances and applications.
M. Herrero (2010)
10.2217/NNM.12.110
Nanostructuring molecular materials as particles and vesicles for drug delivery, using compressed and supercritical fluids.
Elisa C. Elizondo (2012)
10.3390/ma3031928
Targeted Delivery of Protein Drugs by Nanocarriers
R. Solaro (2010)
10.1016/J.SUPFLU.2016.05.036
Encapsulation of Vitamin B2 in solid lipid nanoparticles using supercritical CO2
R. Couto (2017)
10.1016/j.ejpb.2013.07.017
Solid lipid particles for oral delivery of peptide and protein drugs I--elucidating the release mechanism of lysozyme during lipolysis.
P. C. Christophersen (2013)
10.1208/s12248-014-9619-2
Solid Lipid Particles for Oral Delivery of Peptide and Protein Drugs III — the Effect of Fed State Conditions on the In Vitro Release and Degradation of Desmopressin
P. C. Christophersen (2014)
10.4155/TDE.11.125
Supercritical fluid-mediated methods to encapsulate drugs: recent advances and new opportunities.
A. Naylor (2011)
10.1002/047167849x.bio057.pub2
Progress in Supercritical Fluid Technology for Fats and Oils Processing
Feral Temelli (2020)
10.1016/j.jconrel.2017.04.038
Lipophilic peptide character - What oral barriers fear the most.
O. Zupančič (2017)
10.1016/J.JDDST.2017.06.018
Advances on the formulation of proteins using nanotechnologies
Irene Santalices (2017)
10.1007/s11095-014-1337-z
Solid Lipid Particles for Oral Delivery of Peptide and Protein Drugs II – The Digestion of Trilaurin Protects Desmopressin from Proteolytic Degradation
P. C. Christophersen (2014)
10.1016/j.ijpharm.2014.11.003
Development of multicore hybrid particles for drug delivery through the precipitation of CO2 saturated emulsions.
V. S. Gonçalves (2015)
10.1201/B19242-8
Methods for Particle Production: Antisolvent Techniques
Concepción Domingo Pascual (2015)
Nanosistemas para el tratamiento de la diabetes mellitus por vía transmucosal
Angela Valle Gallego (2011)
10.1016/J.SUPFLU.2010.05.013
Production of lipid microparticles containing bioactive molecules functionalized with PEG
Keti Vezzù (2010)
10.4172/JBB.1000027
Pharmaceutical Technologies for Enhancing Oral Bioavailability of Poorly Soluble Drugs
Y. R. Krishnaiah (2010)
10.1517/17425247.2012.717068
Oral delivery of peptides and proteins using lipid-based drug delivery systems
P. Li (2012)
10.1016/j.ijpharm.2016.02.019
Lipid-based nanoformulations for peptide delivery.
N. Matougui (2016)
10.2217/NNM-2016-0265
Lipid-based nanocarriers for the oral administration of biopharmaceutics.
T. Karamanidou (2016)
10.1016/j.ejpb.2016.08.002
In vitro and in vivo evaluation of an oral multiple-unit formulation for colonic delivery of insulin.
A. Maroni (2016)
10.1016/j.addr.2018.07.010
Supercritical carbon dioxide‐based technologies for the production of drug nanoparticles/nanocrystals – A comprehensive review☆
Luís Padrela (2018)
10.1002/adhm.201700433
Supercritical Fluid Technology: An Emphasis on Drug Delivery and Related Biomedical Applications
Ranjith Kumar Kankala (2017)
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