Приказ основних података о документу

dc.creatorMarković, Bojan
dc.creatorVladimirov, Sote
dc.creatorČudina, Olivera
dc.creatorOdović, Jadranka
dc.creatorKarljiković-Rajić, Katarina
dc.date.accessioned2019-09-02T11:29:26Z
dc.date.available2019-09-02T11:29:26Z
dc.date.issued2012
dc.identifier.issn1420-3049
dc.identifier.urihttps://farfar.pharmacy.bg.ac.rs/handle/123456789/1722
dc.description.abstractThe permeation properties of twenty newly synthesized alpha-alkoxyalkanoyl and alpha-aryloxyalkanoyl C-21 esters of standard corticosteroids: Fluocinolone acetonide, dexamethasone, triamcinolone acetonide and hydrocortisone were established using a PAMPA assay (70% silicone oil and 30% isopropyl myristate). The data were compared with parent corticosteroids with addition of mometasone furoate and hydrocortisone acetate. All newly synthesized corticosteroid C-21 esters have effective permeability coefficients higher then -6, mostly followed with high values of retention factors and low permeation. The examined compounds were grouped through relationship between obtained retention factors and permeation parameters (groups I-III). The classification confirmed group I (membrane retentions as well as permeation lower then 30%) for all corticosteroid standards except mometasone furoate, a potent topical corticosteroid which, with high membrane retention (81%) and low permeation (7.7%) fits into group III. The largest number of new synthesized corticosteroids C-21 esters, among them all fluocinolone acetonide C-21 esters, have high membrane retentions (32.4%-86.5%) and low permeations (1.3%-27.1%), fitting in group III. The classification was related to previously obtained anti-inflammatory activity data for the fluocinolone acetonide C-21 esters series. According to the PAMPA results the new synthesized esters could be considered as potential new prodrugs with useful benefit/risk ratio.en
dc.publisherMDPI, Basel
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.sourceMolecules
dc.subjectcorticosteroid C-21 estersen
dc.subjectprodrugen
dc.subjectPAMPAen
dc.subjectmembrane retentionen
dc.subjectpermeation parameteren
dc.titleA PAMPA Assay as Fast Predictive Model of Passive Human Skin Permeability of New Synthesized Corticosteroid C-21 Estersen
dc.typearticle
dc.rights.licenseBY
dcterms.abstractМарковић, Бојан; Владимиров, Соте; Карљиковић-Рајић, Катарина; Одовић, Јадранка; Чудина, Оливера;
dc.citation.volume17
dc.citation.issue1
dc.citation.spage480
dc.citation.epage491
dc.citation.other17(1): 480-491
dc.citation.rankM22
dc.identifier.wos000299535700032
dc.identifier.doi10.3390/molecules17010480
dc.identifier.pmid22222907
dc.identifier.scopus2-s2.0-84856199554
dc.identifier.fulltexthttps://farfar.pharmacy.bg.ac.rs//bitstream/id/537/1720.pdf
dc.type.versionpublishedVersion


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Приказ основних података о документу