Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1989-8-25
pubmed:abstractText
Protease inhibition has been postulated to be one of the several mechanisms by which penetration enhancers promote the mucosal absorption of peptide and protein drugs. The objective of this study was to determine whether protease inhibition by Na glycocholate and polyoxyethylene-9-lauryl ether, two extensively studied enhancers, led to suppression of insulin proteolysis over a range of insulin concentrations. To this end, the rate of insulin proteolysis in nasal tissue supernatants of the albino rabbit was determined in the presence of 0.1-2% Na glycocholate and polyoxyethylene-9-lauryl ether and at insulin concentrations ranging from 5 to 100 microM. Partly due to self-association, insulin was self-stabilizing against nasal proteolysis as its concentration was raised from 5 to 100 microM. At insulin concentrations lower than 50 microM, both Na glycocholate and polyoxyethylene-9-lauryl ether reduced the rate of insulin proteolysis. By contrast, at 100 microM insulin concentration, both enhancers accelerated insulin proteolysis. Such an effect was attributed to the deaggregation of insulin by the enhancers, increasing the proportion of monomers available for nasal proteolysis. The incorporation of 0.1 mM PCMPS, a potent inhibitor of insulin proteolysis, partly overcame the accelerating effect of Na glycocholate on insulin proteolysis.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0024-3205
pubmed:author
pubmed:issnType
Print
pubmed:volume
45
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
167-74
pubmed:dateRevised
2011-11-17
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Effect of sodium glycocholate and polyoxyethylene-9-lauryl ether on the hydrolysis of varying concentrations of insulin in the nasal homogenates of the albino rabbit.
pubmed:affiliation
University of Southern California, School of Pharmacy, Los Angeles 90033.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't