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Lipid Emulsions As Vehicles For Enhanced Nasal Delivery Of Insulin.

R. Mitra, I. Pezron, W. Chu, A. Mitra
Published 2000 · Medicine, Chemistry

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The objective of this work is to explore lipid emulsion based formulations of insulin as an enhancer of nasal absorption. Insulin was incorporated into the aqueous phases of water-in-oil (w/o) and oil-in-water (o/w) emulsions. The formulations were perfused through the nasal cavity of rats in situ. Enhancement of insulin absorption was observed when insulin was incorporated into the continuous aqueous phase of an o/w emulsion. The presence of a small fraction of oil droplets along with insulin in the aqueous phase appeared to favor insulin absorption. When the oil phase constitutes the external phase, as in w/o emulsion, no insulin absorption was noted. Inhibition of insulin absorption might arise from a rate limiting barrier effect of the membrane completely covered by a stagnant oil layer. The in situ model was validated by in vivo experiments, which also revealed an increase in insulin absorption with o/w emulsions. However at lower insulin doses there was no statistically significant enhancing effect. In situ perfusion experiments across rat nasal pathway appear to be an appropriate model to study the enhancement effect of nasal formulations.
This paper references
10.1002/JPS.2600740605
Mechanism of nasal absorption of drugs I: Physicochemical parameters influencing the rate of in situ nasal absorption of drugs in rats.
C. Huang (1985)
10.1023/A:1015808023310
Nasal Membrane and Intracellular Protein and Enzyme Release by Bile Salts and Bile Salt-Fatty Acid Mixed Micelles: Correlation with Facilitated Drug Transport
Z. Shao (2004)
10.1023/A:1018970006935
Nasal Absorption in the Rat. III. Effect of Lysophospholipids on Insulin Absorption and Nasal Histology
Susan G. Chandler (2004)
10.1016/0301-4622(91)85023-J
Insulin association in neutral solutions studied by light scattering.
S. Hvidt (1991)
10.1016/0005-2736(82)90307-8
Binding of insulin to the external surface of liposomes. Effect of surface curvature, temperature, and lipid composition.
J. Wiessner (1982)
10.1016/S0169-409X(97)00069-0
Microspheres as nasal drug delivery systems.
Pereswetoff-Morath (1998)
10.1016/0361-9230(85)90153-4
Peptides and the blood-brain barrier: Lipophilicity as a predictor of permeability
W. Banks (1985)
10.1046/J.1365-2273.1997.00019.X
The nasal delivery of drugs.
M. Quraishi (1997)
10.1016/S0169-409X(97)00060-4
Intranasal drug delivery.
Hussain (1998)
Effect of a conjugated bile salt on the pulmonary absorption of insulin in rats
Yuping Li (1993)
10.1016/S0169-409X(97)00059-8
Nasal mucociliary clearance as a factor in nasal drug delivery.
Merkus (1998)
10.1023/A:1015896405389
Absorption Enhancing Effect of Cyclodextrins on Intranasally Administered Insulin in Rats
F. H. H. M. Merkus (2004)
10.1016/0378-5173(95)00057-P
Preparation and characterization of a peptide containing w/o emulsion
Timm Trenktrog (1995)
10.1016/0378-5173(81)90058-2
Absorption of drugs from the nasal mucosa of rat
Hirai Shinichiro (1981)
10.1016/0378-5173(81)90010-7
Mechanisms for the enhancement of the nasal absorption of insulin by surfactants
Hirai Shinichiro (1981)
10.1016/0378-5173(81)90009-0
Effect of surfactants on the nasal absorption of insulin in rats
Hirai Shinichiro (1981)
10.3109/02652049709051136
Insulin in w/o/w multiple emulsions: biological activity after oral administration in normal and diabetic rats.
A. Cunha (1997)
10.1111/j.1464-5491.1992.tb01792.x
Intranasal Administration of Insulin With Phospholipid as Absorption Enhancer: Pharmacokinetics in Normal Subjects
K. Drejer (1992)
10.1021/JS980125Q
Enhanced colonic and rectal absorption of insulin using a multiple emulsion containing eicosapentaenoic acid and docosahexaenoic acid.
A. Suzuki (1998)
10.1073/PNAS.82.21.7419
Nasal absorption of insulin: enhancement by hydrophobic bile salts.
G. Gordon (1985)



This paper is referenced by
Peroral and nasal delivery of insulin with PheroidTM technology
Ian Dewald Oberholzer (2009)
Research Article Optimization of Formulation of Insulin Microspheres for Oral Delivery
Sanjay R. Patel (2013)
10.3109/10717544.2011.600784
Evaluation of submicron emulsion as vehicles for rapid-onset intranasal delivery and improvement in brain targeting of zolmitriptan
Chaoqun Yu (2011)
10.3390/molecules14093754
Nasal Delivery of High Molecular Weight Drugs
Y. Ozsoy (2009)
10.1007/978-0-387-74901-3
Drug Absorption Studies
C. Ehrhardt (2008)
Non invasive insulins: advanced insulin therapy over this decade
T. Rajeswari (2011)
10.1208/s12249-020-01805-x
Preparation and Evaluation of Mebendazole Microemulsion for Intranasal Delivery: an Alternative Approach for Glioblastoma Treatment.
Julio Mena-Hernández (2020)
20 Nasal Delivery of Peptide Drugs
D. Pillion (2006)
10.1117/12.462526
Investigation of phosphatidylcholine enhancing FITC-insulin across buccal mucosa by confocal laser scanning microscopy
Weiqun Tian (2002)
10.1533/9781908818683.59
Routes of administration of insulin
T. A. Sonia (2015)
10.2165/00003088-200342130-00003
Absorption Enhancers for Nasal Drug Delivery
S. Davis (2003)
10.1007/978-0-387-74901-3_5
In Situ and Ex Vivo Nasal Models for Preclinical Drug Development Studies
R. Agu (2008)
10.1201/B10846-9
Transdermal Drug Delivery
Vasant V. Ranade (2011)
10.1177/0885328206060436
Insulin Loaded Eudragit L100 Microspheres for Oral Delivery: Preliminary in vitro Studies
D. Jain (2006)
10.15171/PS.2019.14
Non-Invasive and Less Degradative Ways of Insulin Administration
S. Allahyari (2019)
10.1517/13543776.12.3.331
Prodrug strategies in nasal drug delivery
I. Pezron (2002)
ORAL DELIVERY OF INSULIN USING COMPOSITE POLYMERIC MICROPARTICLES
Rajesh Kumar (2014)
Formulation , in vitro and in vivo evaluation of oral sustained release insulin-loaded microspheres based on Eudragit ® RS 100
Mumuni A. Momoh (2015)
10.1002/biot.201300093
Facile preparation of well‐defined near‐monodisperse chitosan/sodium alginate polyelectrolyte complex nanoparticles (CS/SAL NPs) via ionotropic gelification: A suitable technique for drug delivery systems
P. Liu (2013)
10.1016/J.BIOMATERIALS.2006.12.024
A thermosensitive hydrogel based on quaternized chitosan and poly(ethylene glycol) for nasal drug delivery system.
J. Wu (2007)
10.1080/10611860801900090
The release and analgesic activities of morphine and its ester prodrug, morphine propionate, formulated by water-in-oil nanoemulsions
J. Wang (2008)
10.1080/10717540802006377
Permeation Studies and Histological Examination of Sheep Nasal Mucosa Following Administration of Different Nasal Formulations with or without Absorption Enhancers
E. Karasulu (2008)
Preparation of Pentablock Nanomicellar Formulations for Prostate Cancer Drug Delivery Systems
Alex Oselu Owiti (2018)
EUDRAGIT COATED MICROPARTICULATE DELIVERY OF BOVINE INSULIN FOR ORAL DELIVERY
Rajesh Kumar (2014)
The Use of Polyglycol Succinates for the Microencapsulation of Insulin
R. Sariri (2002)
10.1039/c3cs60436e
Emerging micro- and nanotechnology based synthetic approaches for insulin delivery.
Ran Mo (2014)
10.1201/9780203219935-22
In vitro methodologies to study nasal delivery using excised mucosa
A. Koch (2002)
10.3109/10611860903386938
Formulation of intranasal mucoadhesive temperature-mediated in situ gel containing ropinirole and evaluation of brain targeting efficiency in rats
S. Khan (2010)
Nasal delivery of recombinant human growth hormone with pheroid technology
J. D. Steyn (2006)
10.1002/jps.22314
Poloxamer/cyclodextrin/chitosan-based thermoreversible gel for intranasal delivery of fexofenadine hydrochloride.
H. Cho (2011)
10.1016/S1773-2247(10)50043-1
Chitosan-coated lipid nanocarriers for therapeutic applications
F. Oyarzun-Ampuero (2010)
10.1002/JPS.10114
Insulin aggregation and asymmetric transport across human bronchial epithelial cell monolayers (Calu-3).
I. Pezron (2002)
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