Surfactant systems for nasal zidovudine delivery: structural, rheological and mucoadhesive properties

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dc.contributor.authorCarvalho, Flavia C. [UNESP]
dc.contributor.authorBarbi, Mariana S. [UNESP]
dc.contributor.authorSarmento, Victor Hugo V.
dc.contributor.authorChiavacci, Leila Aparecida [UNESP]
dc.contributor.authorNetto, Flavia M.
dc.contributor.authorGremião, Maria Palmira Daflon [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade Federal de Sergipe (UFS)
dc.contributor.institutionUniversidade Estadual de Campinas (UNICAMP)
dc.date.accessioned2014-05-20T13:24:59Z
dc.date.available2014-05-20T13:24:59Z
dc.date.issued2010-04-01
dc.description.abstractObjectives Zidovudine is the antiretroviral drug most frequently used for the treatment of AIDS. Although its effectiveness is recognized, it undergoes extensive first-pass metabolism and exhibits poor oral bioavailability. The nasal route is an option for enhanced therapeutic efficacy and to reduce the extent of the first-pass effect. There are some mechanisms that limit intranasal absorption, such as mucociliary clearance, which rapidly removes the formulation from the nasal cavity. To improve the nasal residence time of zidovudine on the nasal mucosa, we aimed to develop a mucoadhesive surfactant system for zidovudine nasal administration.Methods Systems composed of PPG-5-CETETH-20 as surfactant, oleic acid and water were characterized by polarized light microscopy, small-angle X-ray scattering and rheological measurements. Mucoadhesion was investigated by phase behaviour studies, rheological synergism and mucoadhesive strength determination.Key findings Results indicate that the original formulations were microemulsions that displayed phase transition to a lamellar phase when brought into contact with aqueous nasal simulated mucus. The phase transition was accompanied by an increase in system elasticity and, irrespective of phase behaviour, all the systems showed a good mucoadhesive force. Thus, a viscous and mucoadhesive liquid crystalline matrix could be formed when the formulations were in contact with simulated mucus, which may prolong the residence time of zidovudine in the nasal cavity.Conclusions These findings indicate a potentially useful system for nasal administration of zidovudine.en
dc.description.affiliationState Univ São Paulo, UNESP, Sch Pharmaceut Sci, Araraquara, Brazil
dc.description.affiliationUniv Fed Sergipe, Itabaiana, SE, Brazil
dc.description.affiliationUniv Estadual Campinas, UNICAMP, Campinas, SP, Brazil
dc.description.affiliationUnespState Univ São Paulo, UNESP, Sch Pharmaceut Sci, Araraquara, Brazil
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.format.extent430-439
dc.identifierhttp://onlinelibrary.wiley.com/doi/10.1211/jpp.62.04.0004/full
dc.identifier.citationJournal of Pharmacy and Pharmacology. Malden: Wiley-blackwell, v. 62, n. 4, p. 430-439, 2010.
dc.identifier.doi10.1211/jpp/62.04.0004
dc.identifier.issn0022-3573
dc.identifier.lattes9129780536724256
dc.identifier.urihttp://hdl.handle.net/11449/7894
dc.identifier.wosWOS:000277102200004
dc.language.isoeng
dc.publisherWiley-Blackwell
dc.relation.ispartofJournal of Pharmacy and Pharmacology
dc.relation.ispartofjcr2.309
dc.relation.ispartofsjr0,657
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectliquid crystalen
dc.subjectmicroemulsionen
dc.subjectmucoadhesionen
dc.subjectoscillatory rheologyen
dc.subjectphase behaviouren
dc.titleSurfactant systems for nasal zidovudine delivery: structural, rheological and mucoadhesive propertiesen
dc.typeArtigo
dcterms.licensehttp://olabout.wiley.com/WileyCDA/Section/id-406071.html
dcterms.rightsHolderWiley-blackwell
unesp.author.lattes9129780536724256
unesp.author.orcid0000-0001-7586-539X[1]
unesp.author.orcid0000-0001-6882-002X[3]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

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