Preparation and Characterization of Chitosan Nanoparticles for Zidovudine Nasal Delivery

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dc.contributor.authorBarbi, Mariana da Silva [UNESP]
dc.contributor.authorCarvalho, Flavia Chiva [UNESP]
dc.contributor.authorKiill, Charlene Priscila [UNESP]
dc.contributor.authorBarud, Hernane da Silva [UNESP]
dc.contributor.authorSantagneli, Silvia Helena [UNESP]
dc.contributor.authorLima Ribeiro, Sidney Jose [UNESP]
dc.contributor.authorGremião, Maria Palmira Daflon [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2015-03-18T15:55:44Z
dc.date.available2015-03-18T15:55:44Z
dc.date.issued2015-01-01
dc.description.abstractZidovudine (AZT) is the antiretroviral drug most frequently used for the treatment of Acquired Immunodeficiency Syndrome. Its low oral bioavailability demands the development of innovative strategies to overcome the first pass metabolism. The nasal route is an option for enhanced therapeutic efficacy and to reduce the extent of the first-pass effect. In this article, AZT loaded chitosan nanoparticles were prepared by a modified ionotropic gelation method with sodium tripolyphosphate. The increase proportion of CS (NP1 10:01 (w/w)) promoted the formation of smaller nanoparticles (260 nm), while raising the proportion of TPP (NP2 5:1 w/w) increased the nanoparticles size (330 nm). The incorporation of AZT increased the nanoparticles size for both AZT-loaded nanoparticles AZT-loaded NP1 (406 nm) and AZT-loaded NP2 (425 nm). The incorporation of AZT into NP1 did not change the electrophoretic mobility, however, in AZT-loaded NP2 there was a significant increase. The positive surface of the nanoparticles is very important for the mucoadhesive properties due interaction with the sialic groups of the mucin. Nuclear resonance magnetic data showed that the higher concentration of chitosan in the nanoparticles favored the interaction of few phosphate units (pyrophosphate) by ionic interaction Scanning electron microscopy, revealed that the nanoparticles are nearly spherical shape with porous surface. The entrapment efficiency of AZT, was 17.58%+/- 1.48 and 11.02%+/- 2.05 for NP1 and NP2, respectively. The measurement of the mucoadhesion force using mucin discs and nasal tissue obtained values of NP1 = 2.12 and NP2 = 4.62. In vitro permeation study showed that the nanoparticles promoted an increase in the flux of the drug through the nasal mucosa. In view of these results, chitosan nanoparticles were found to be a promising approach for the incorporation of hydrophilic drugs and these results suggest that the CS-containing nanoparticles have great potential for nasal AZT administration.en
dc.description.affiliationUNESP Univ Estadual Paulista, Paulista State Univ, Sch Pharmaceut Sci, Fac Ciencias Farmaceut,Lab Farmacos & Medicamento, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUNESP Univ Estadual Paulista, Inst Quim, BR-14800900 Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP Univ Estadual Paulista, Paulista State Univ, Sch Pharmaceut Sci, Fac Ciencias Farmaceut,Lab Farmacos & Medicamento, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP Univ Estadual Paulista, Inst Quim, BR-14800900 Araraquara, SP, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.format.extent865-874
dc.identifierhttp://dx.doi.org/10.1166/jnn.2015.9180
dc.identifier.citationJournal Of Nanoscience And Nanotechnology. Valencia: Amer Scientific Publishers, v. 15, n. 1, p. 865-874, 2015.
dc.identifier.doi10.1166/jnn.2015.9180
dc.identifier.issn1533-4880
dc.identifier.lattes9129780536724256
dc.identifier.urihttp://hdl.handle.net/11449/117291
dc.identifier.wosWOS:000345054000152
dc.language.isoeng
dc.publisherAmer Scientific Publishers
dc.relation.ispartofJournal Of Nanoscience And Nanotechnology
dc.relation.ispartofjcr1.354
dc.relation.ispartofsjr0,326
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectSystem for Drug Deliveryen
dc.subjectNanoparticlesen
dc.subjectChitosanen
dc.subjectNasalen
dc.subjectMucoadhesionen
dc.subjectAIDSen
dc.subjectZidovudiveen
dc.titlePreparation and Characterization of Chitosan Nanoparticles for Zidovudine Nasal Deliveryen
dc.typeArtigo
dcterms.rightsHolderAmer Scientific Publishers
unesp.author.lattes9129780536724256
unesp.author.orcid0000-0001-7586-539X[2]
unesp.author.orcid0000-0002-8162-6747[6]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

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