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Formulation And Characterization Of An Oily-based System For Oral Delivery Of Insulin.

A. Elsayed, Mayyas M. Al Remawi, N. Qinna, A. Farouk, A. Badwan
Published 2009 · Chemistry, Medicine

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The present work explored the possibility of formulating an oral insulin delivery system by combining the advantages of nanoencapsulation and the use of oily vehicle. The parameters affecting formulation such as association efficiency were characterized. The preparation was evaluated for its chemical, physical and biological stability. The preparation has unimodal particle size distribution with a mean diameter of 108+/-9 nm. Insulin was protected from gastric enzymes by incorporation into lipid-based formulation. The results of RP HPLC and ELISA indicated that insulin was able to withstand the preparation procedure. Insulin in the preparations was stable for a period of one month at storage temperatures of 4 and 25 degrees C. It was also biologically active and stable as demonstrated by the remarkable reduction of blood glucose levels of the STZ-diabetic rats after oral administration of the preparation. Moreover, hypoglycemic effect of nanoparticles administered orally was sustained for a longer period of time compared to the subcutaneous injection. These results clearly evidenced the ability of the nanoparticles to enhance the pharmacological response of insulin when given orally and could be used to deliver other peptides.
This paper references
10.1016/0003-9861(90)90673-M
Ionization behavior of native and mutant insulins: pK perturbation of B13-Glu in aggregated species.
N. Kaarsholm (1990)
10.1016/S0378-5173(00)00349-5
Factors limiting the oral bioavailability of N-acetylglucosaminyl-N-acetylmuramyl dipeptide (GMDP) and enhancement of absorption in rats by delivery in a water-in-oil microemulsion.
K. Lyons (2000)
10.1023/A:1012059501947
Interaction Between Polyalkylcyanoacrylate Nanoparticles and Peritoneal Macrophages: MTT Metabolism, NET Reduction, and NO Production
Teresa Cruz (2004)
10.1017/9781107588431.010
頚椎部 instability の計測法
見松 健太郎 (1997)
Preparation and characterization of nanoparticles shelled with chitosan for oral insulin delivery , Biomacromolecules
F. Mi Lin (2005)
10.1016/S0168-3659(03)00126-3
Chitosan-based gastrointestinal delivery systems.
Radi Hejazi (2003)
10.1023/A:1015887001987
Chemical Stability of Insulin. 2. Formation of Higher Molecular Weight Transformation Products During Storage of Pharmaceutical Preparations
Jens Jorgen Veilgaard Brange (1992)
Oral insulin delivery1
Gerardo Carino (1999)
10.1016/S0169-409X(98)00075-1
Oral insulin delivery.
Carino (1999)
10.1016/S0168-3659(97)00266-6
Floating dosage forms: an in vivo study demonstrating prolonged gastric retention.
L. Whitehead (1998)
10.1016/S0378-5173(98)00314-7
Uptake of PMMA nanoparticles from the gastrointestinal tract after oral administration to rats: modification of the body distribution after suspension in surfactant solutions and in oil vehicles
L. Araujo (1999)
10.1016/j.geb.2003.09.006
Preparation
M. Voorneveld (2004)
10.1016/j.jconrel.2008.03.018
Characterization of water-in-oil microemulsion for oral delivery of earthworm fibrinolytic enzyme.
Mao-Bo Cheng (2008)
10.1007/s11095-007-9270-z
Role of a Novel Excipient Poly(Ethylene Glycol)-b-Poly(L-Histidine) in Retention of Physical Stability of Insulin in Aqueous Solutions
Ajay Taluja (2007)
10.1021/BM0607776
Preparation and characterization of nanoparticles shelled with chitosan for oral insulin delivery.
Yu-Hsin Lin (2007)
10.3109/03639049609065908
Human Insulin: Basic Sciences to Therapeutic Uses
Y. Chien (1996)
10.1002/JPS.2600791016
Lactic acid oligomer microspheres containing hydrophilic drugs.
R. Wada (1990)
xxx–xxx 11 ARTICLE IN PRESS Please cite this article in press as Formulation and characterization of an oily-based system for oral delivery of insulin
A Elsayed (2009)
10.1021/JS970124I
Poly(alkyl cyanoacrylate) nanospheres for oral administration of insulin.
C. Damgé (1997)
10.1016/J.ARCMED.2005.03.012
Insulin therapy: current alternatives.
F. Gómez-Pérez (2005)
10.1016/S0939-6411(03)00160-7
Structure and interactions in chitosan hydrogels formed by complexation or aggregation for biomedical applications.
J. Berger (2004)
10.1023/A:1012059501947
Interaction Between Polyalkylcyanoacrylate Nanoparticles and Peritoneal Macrophages: MTT Metabolism, NET Reduction, and NO Production
Teresa Cruz (1997)
10.1089/1520915041705929
The physiological rationale for oral insulin administration.
E. Arbit (2004)
Chitin Chemistry
G.A.F. Roberts (1992)
10.1016/S0378-5173(02)00002-9
Effects of formulation variables on characteristics of poly (ethylcyanoacrylate) nanocapsules prepared from w/o microemulsions.
S. Watnasirichaikul (2002)
10.1515/9783111576855-016
K
Martin P. Catherwood (1824)
10.1016/j.ijpharm.2007.11.052
Preparation, characterization and antibacterial activities of chitosan, N-trimethyl chitosan (TMC) and N-diethylmethyl chitosan (DEMC) nanoparticles loaded with insulin using both the ionotropic gelation and polyelectrolyte complexation methods.
A. Sadeghi (2008)
10.1023/A:1015887001987
Chemical Stability of Insulin. 2. Formation of Higher Molecular Weight Transformation Products During Storage of Pharmaceutical Preparations
J. Brange (2004)
10.1016/j.nano.2006.04.009
Nanoencapsulation II. Biomedical applications and current status of peptide and protein nanoparticulate delivery systems.
Catarina Reis (2006)
10.1002/JPS.10149
Formulation pH modulates the interaction of insulin with chitosan nanoparticles.
Zengshuan Ma (2002)
10.1016/J.JCONREL.2004.10.012
Influence of molecular weight on oral absorption of water soluble chitosans.
S. Chae (2005)
10.1016/J.NANO.2006.04.009
Nanoencapsulation II. Biomedical applications and current status of peptide and protein nanoparticulate delivery systems.
C. Reis (2006)
10.1016/J.IJPHARM.2005.04.016
A lecithin-based microemulsion of rh-insulin with aprotinin for oral administration: Investigation of hypoglycemic effects in non-diabetic and STZ-induced diabetic rats.
A. Cilek (2005)
10.1016/J.EJPB.2004.10.006
Strategic approaches for overcoming peptide and protein instability within biodegradable nano- and microparticles.
U. Bilati (2005)
10.1007/s11095-007-9488-9
Safe and Effective Permeation Enhancers for Oral Drug Delivery
K. Whitehead (2007)
10.1016/S0731-7085(97)00096-4
The application of capillary electrophoresis for monitoring effects of excipients on protein conformation.
K. A. McIntosh (1998)
10.1016/J.IJPHARM.2007.05.015
Peroral delivery of insulin using chitosan derivatives: a comparative study of polyelectrolyte nanocomplexes and nanoparticles.
Anchalee Jintapattanakit (2007)
10.1248/CPB.44.235
Instability of bovine insulin in poly(lactide-co-glycolide) (PLGA) microspheres.
T. Uchida (1996)
Gastro retentive dosage forms
A. Moses (1993)
10.1016/J.CARBPOL.2006.11.006
Calculation of Mark–Houwink–Sakurada (MHS) equation viscometric constants for chitosan in any solvent–temperature system using experimental reported viscometric constants data
M. Kasaai (2007)
10.1002/JPS.20520
Self-assembled polyelectrolyte nanocomplexes between chitosan derivatives and insulin.
S. Mao (2006)
10.1021/JS960297S
Toward understanding insulin fibrillation.
J. Brange (1997)
Non-absorbable lipid binder
N. Furda (1980)
10.1016/S0141-8130(00)00118-5
Chitosan as an enabling excipient for drug delivery systems. I. Molecular modifications.
S. Sabnis (2000)
10.1016/J.JCONREL.2006.08.013
Nanoparticles as potential oral delivery systems of proteins and vaccines: a mechanistic approach.
A. des Rieux (2006)
10.1016/J.EJPB.2006.03.011
Enhancing mechanism of Labrasol on intestinal membrane permeability of the hydrophilic drug gentamicin sulfate.
K. Koga (2006)
10.1016/S0378-5173(02)00548-3
Effect of molecular structure of chitosan on protein delivery properties of chitosan nanoparticles.
Y. Xu (2003)
10.1016/J.EURPOLYMJ.2007.03.042
Synthesis and characterization of PEG modified N-trimethylaminoethylmethacrylate chitosan nanoparticles
Siyu Zhu (2007)
10.1016/S0032-9592(98)00116-2
Optimum conditions for the precipitation of chitosan oligomers with DP 5-7 in concentrated hydrochloric acid at low temperature
M. Lee (1999)
10.1016/S0014-5793(97)01596-2
Domain structure and stability of human phenylalanine hydroxylase inferred from infrared spectroscopy
R. Chehín (1998)
Gastroretentive dosage forms.
A. Moes (1993)
10.1016/J.EJPS.2006.05.008
Preparing and evaluating delivery systems for proteins.
L. Jorgensen (2006)
10.1007/S10953-009-9405-4
Investigation of the Interactions in Complexes of Low Molecular Weight Chitosan with Ibuprofen
A. Qandil (2009)
10.1016/J.CARBPOL.2005.10.026
Effects of molecular weight, degree of acetylation and ionic strength on surface tension of chitosan in dilute solution
Gao Qun (2006)
10.1016/0378-5173(94)00386-J
Using microemulsion formulations for oral drug delivery of therapeutic peptides
J. M. Sarciaux (1995)
10.1007/s10989-005-9010-3
Development and Comparison of Different Nanoparticulate Polyelectrolyte Complexes as Insulin Carriers
B. Sarmento (2005)
10.1002/JPS.2600800623
Biological activity of insulin in microemulsion in mice.
D. G. Patel (1991)
10.1016/J.IJPHARM.2004.12.025
Pharmacological activity of peroral chitosan-insulin nanoparticles in diabetic rats.
Zengshuan Ma (2005)
10.1021/JS9502229
Lymphatic transport of halofantrine in the conscious rat when administered as either the free base or the hydrochloride salt: effect of lipid class and lipid vehicle dispersion.
C. J. Porter (1996)
10.1016/S0144-8617(00)00288-5
Acid hydrolysis of chitosans
K. M. Vårum (2001)
Protein instability toward organic solvent/water emulsification: implications for protein microencapsulation into microspheres.
H. Sah (1999)
10.3109/03639049609108355
Controlled-Release Drug Delivery Systems for Prolonged Gastric Residence: An Overview
A. Deshpande (1996)
10.1016/S0378-5173(99)00152-0
Instability, stabilization, and formulation of liquid protein pharmaceuticals.
W. Wang (1999)
10.1016/J.JPBA.2005.10.016
Quantitative determination of insulin entrapment efficiency in triblock copolymeric nanoparticles by high-performance liquid chromatography.
Xiongliang Xu (2006)
10.1016/J.JCONREL.2006.04.017
Polyionic hydrocolloids for the intestinal delivery of protein drugs: alginate and chitosan--a review.
M. George (2006)
10.1016/S0378-5173(96)04700-X
Influence of temperature and shaking on stability of insulin preparations : degradation kinetics
A. Oliva (1996)



This paper is referenced by
10.5772/58538
Nanoparticle Insulin Drug Delivery — Applications and New Aspects
H. Elçioğlu (2014)
10.1208/s12249-011-9647-5
Chitosan–Sodium Lauryl Sulfate Nanoparticles as a Carrier System for the In Vivo Delivery of Oral Insulin
A. Elsayed (2011)
A REVIEW OF RECENT TRENDS IN NON-INVASIVE INSULIN THERAPY FOR DIABETES MELLITUS
Sudha Bala (2014)
10.3390/molecules24234209
Nanoparticle Delivery Systems in the Treatment of Diabetes Complications
E. B. Souto (2019)
10.1007/978-3-319-26414-1
Natural Polymers: Industry Techniques and Applications
O. Olatunji (2016)
10.1016/j.jconrel.2017.09.003
Potential of insulin nanoparticle formulations for oral delivery and diabetes treatment
Chun Y Wong (2017)
10.3390/md16010032
Low Molecular Weight Chitosan-Insulin Complexes Solubilized in a Mixture of Self-Assembled Labrosol and Plurol Oleaque and Their Glucose Reduction Activity in Rats
Amani M. Elsayed (2018)
Subcutaneous and oral delivery of insulin
Zakieh Al Kurdi (2015)
10.1002/adbi.201800230
Origami Biosystems: 3D Assembly Methods for Biomedical Applications
Vladimir A. Bolaños Quiñones (2018)
10.23736/S0391-1977.19.03055-4
Oral insulin: an update.
Subhankar Chatterjee (2019)
10.1007/978-94-017-8896-0_7
Mucus as Physiological Barrier to Intracellular Delivery
Eleonore Fröhlich (2014)
10.1016/j.ijbiomac.2016.06.028
Enzyme coated beta-cyclodextrin for effective adsorption and glucose-responsive closed-loop insulin delivery.
T S Anirudhan (2016)
10.1007/s13346-017-0383-6
Incorporation of lipolysis in monolayer permeability studies of lipid-based oral drug delivery systems
Tanmoy Sadhukha (2017)
10.1021/mp5003653
Molecular mechanism of poly(vinyl alcohol) mediated prevention of aggregation and stabilization of insulin in nanoparticles.
Sanjay Rawat (2015)
10.2147/IJN.S86313
Probing insulin bioactivity in oral nanoparticles produced by ultrasonication-assisted emulsification/internal gelation
M. A. Lopes (2015)
10.1152/ajpgi.00107.2011
A review of the efficacy and safety of nanoparticle-based oral insulin delivery systems.
J. W. Card (2011)
Developing oral formulations for protein and peptide drugs
A. Parry (2013)
10.1007/978-3-319-26414-1_9
Pharmaceutical Applications of Natural Polymers
Atul Nayak (2016)
10.1080/09205063.2020.1725863
Preparation and characterization of polylactic-co-glycolic acid/insulin nanoparticles encapsulated in methacrylate coated gelatin with sustained release for specific medical applications
Elham Akhavan Farid (2020)
10.1002/9781119962977.CH11
Chitosan‐Based Systems for Mucosal Delivery of Biopharmaceuticals
Sonia Al-Qadi (2012)
Drug Design, Development and Therapy Dovepress Impact of Streptozotocin on Altering Normal Glucose Homeostasis during Insulin Testing in Diabetic Rats Compared to Normoglycemic Rats Nidal a Qinna
Adnan Ali H Badwan ()
10.1016/j.jddst.2020.101738
Formulation and characterisation of insulin-loaded chitosan nanoparticles capable of inducing glucose uptake in skeletal muscle cells in vitro
Chun Y Wong (2020)
10.1016/j.jsps.2019.09.009
Synthesis, characterization and evaluation of deacetylated xanthan derivatives as new excipients in the formulation of chitosan-based polyelectrolytes for the sustained release of tramadol
Meriem Boudoukhani (2019)
10.1016/J.JFF.2013.03.009
Evaluation of a functional food preparation based on chitosan as a meal replacement diet
N. Qinna (2013)
10.1080/1061186X.2020.1759078
Current status and applications of animal models in pre-clinical development of orally administered insulin-loaded nanoparticles
Chun Y Wong (2020)
10.1021/mp300009u
A prodrug nanoparticle approach for the oral delivery of a hydrophilic peptide, leucine(5)-enkephalin, to the brain.
A. Lalatsa (2012)
10.1016/j.jsps.2014.06.004
A review on the strategies for oral delivery of proteins and peptides and their clinical perspectives
Abdul Muheem (2016)
10.1016/j.addr.2016.04.001
Lipid-based nanocarriers for oral peptide delivery.
Zhigao Niu (2016)
10.2147/DDDT.S79885
Impact of streptozotocin on altering normal glucose homeostasis during insulin testing in diabetic rats compared to normoglycemic rats
N. Qinna (2015)
10.5772/52265
Oral Delivery of Insulin: Novel Approaches
Amani M. Elsayed (2012)
10.1016/j.ijpharm.2013.12.014
Development of insulin loaded mesoporous silica injectable particles layered by chitosan as a controlled release delivery system.
Amani M. Elsayed (2014)
10.2174/2211738507666190321110721
Nanotechnology in insulin delivery for management of diabetes.
Fatemah Bahman (2019)
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