Linked Life Data

11337057

Source:http://linkedlifedata.com/resource/pubmed/id/11337057

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2001-5-4
pubmed:abstractText
The purpose of this study was to investigate the feasibility of buccal delivery of a model peptide, endomorphin-1 (ENI), using stability and in vitro permeation studies. ENI is a recently isolated mu-opiate receptor agonist with high selectivity and specificity for this receptor subtype. Stability studies were conducted in various buffers and the drug was shown to be stable in both acidic and basic buffer systems. In the presence of full thickness porcine buccal epithelium, ENI was unstable with only 23.4+/-15.7% intact drug present after 6 h. The region responsible for this degradation was found to coincide with the major barrier region of the buccal epithelium as delineated through stability experiments in the presence of partial thickness buccal epithelium. Various peptidase inhibitors were used to isolate the enzyme(s) responsible for this degradation. Diprotin-A, a potent inhibitor of dipeptidyl peptidase IV, provided significant inhibition of the degradation of ENI in the presence of buccal epithelium. In vitro permeation studies revealed that the permeability coefficient of ENI across porcine buccal epithelium was 5.67+/-4.74x10(-7) cm/s. The enzymatic degradation of ENI was found not to be rate limiting to the drug's permeation across buccal epithelium, as diprotin-A did not increase the permeation of ENI. Sodium glycocholate as well as sodium taurocholate were also ineffective in enhancing the permeation of ENI across porcine buccal epithelium.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0168-3659
pubmed:author
pubmed:issnType
Print
pubmed:day
18
pubmed:volume
73
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
31-6
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2001
pubmed:articleTitle
Transbuccal peptide delivery: stability and in vitro permeation studies on endomorphin-1.
pubmed:affiliation
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, TX 79106, USA.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't