Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
2001-12-17
pubmed:abstractText
The self-assembling properties of poly(vinyl alcohol) substituted with 2-hydroxypropyltrimethylammonium and with acyl chains of different molecular weights (butyryl, capryloyl, lauroyl, or myristoyl) were evaluated to assess the conditions favoring interaction with a poorly soluble drug such as indomethacin to increase its availability. To evaluate the effect of drug-polymer interactions on the solubility of the drug, phase-solubility diagrams were obtained from each substituted polymer at pH 2.0, 5.5, and 7.4 in the presence of indomethacin. To evaluate the availability of the free drug in solution, release profiles of the free drug from drug-polymer physical mixtures were obtained by a dissolution-diffusion apparatus containing a dialysis membrane allowing diffusion of the free drug towards a receiving phase where its concentration was determined over time. The phase-solubility diagrams revealed increasing drug solubility on increasing the polymer concentration. The drug-polymer affinity was slightly increased by lengthening the chain of the substituent on the polymer and was strongly increased by raising the pH of the aqueous phase. The thermodynamic evaluation of the drug-polymer interactions indicated that the interaction is enthalpically driven while the increase in drug-polymer affinity with increasing chain length could be attributed to an entropic contribution. The free drug availability from the drug-polymer systems increased on enhancing the drug-polymer affinity because it corresponded to an increase in the solubilizing effect of the polymer on the drug.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0022-3549
pubmed:author
pubmed:copyrightInfo
Copyright 2001 Wiley-Liss, Inc. and the American Pharmaceutical Association
pubmed:issnType
Print
pubmed:volume
90
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1435-44
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
2001
pubmed:articleTitle
Self-assembling poly(vinyl alcohol) derivatives, interactions with drugs and control of release.
pubmed:affiliation
Department of Pharmaceutical Sciences, Bologna University, Via S. Donato 19/2-40127, Bologna, Italy. orienti@biocfarm.unibo.it
pubmed:publicationType
Journal Article