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A PAMPA Assay as Fast Predictive Model of Passive Human Skin Permeability of New Synthesized Corticosteroid C-21 Esters
dc.creator | Marković, Bojan | |
dc.creator | Vladimirov, Sote | |
dc.creator | Čudina, Olivera | |
dc.creator | Odović, Jadranka | |
dc.creator | Karljiković-Rajić, Katarina | |
dc.date.accessioned | 2019-09-02T11:29:26Z | |
dc.date.available | 2019-09-02T11:29:26Z | |
dc.date.issued | 2012 | |
dc.identifier.issn | 1420-3049 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/1722 | |
dc.description.abstract | The 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.publisher | MDPI, Basel | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS// | |
dc.rights | openAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | Molecules | |
dc.subject | corticosteroid C-21 esters | en |
dc.subject | prodrug | en |
dc.subject | PAMPA | en |
dc.subject | membrane retention | en |
dc.subject | permeation parameter | en |
dc.title | A PAMPA Assay as Fast Predictive Model of Passive Human Skin Permeability of New Synthesized Corticosteroid C-21 Esters | en |
dc.type | article | |
dc.rights.license | BY | |
dcterms.abstract | Марковић, Бојан; Владимиров, Соте; Карљиковић-Рајић, Катарина; Одовић, Јадранка; Чудина, Оливера; | |
dc.citation.volume | 17 | |
dc.citation.issue | 1 | |
dc.citation.spage | 480 | |
dc.citation.epage | 491 | |
dc.citation.other | 17(1): 480-491 | |
dc.citation.rank | M22 | |
dc.identifier.wos | 000299535700032 | |
dc.identifier.doi | 10.3390/molecules17010480 | |
dc.identifier.pmid | 22222907 | |
dc.identifier.scopus | 2-s2.0-84856199554 | |
dc.identifier.fulltext | https://farfar.pharmacy.bg.ac.rs//bitstream/id/537/1720.pdf | |
dc.type.version | publishedVersion |