Vaginal Polyelectrolyte Layer-by-Layer Films Based on Chitosan Derivatives and Eudragit® S100 for pH Responsive Release of Tenofovir

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dc.contributor.authorCazorla Luna, Raúl
dc.contributor.authorMartín Illana, Araceli
dc.contributor.authorNotario Pérez, Fernando
dc.contributor.authorBedoya del Olmo, Luis Miguel
dc.contributor.authorTamayo, Aitana
dc.contributor.authorRuiz-Caro, Roberto
dc.contributor.authorRubio, Juan
dc.contributor.authorVeiga Ochoa, María Dolores
dc.date.accessioned2023-06-17T09:16:49Z
dc.date.available2023-06-17T09:16:49Z
dc.date.issued2020-01-09
dc.description.abstractWomen are still at high risk of contracting the human immunodeficiency virus (HIV) virus due to the lack of protection methods under their control, especially in sub-Saharan countries. Polyelectrolyte multilayer smart vaginal films based on chitosan derivatives (chitosan lactate, chitosan tartate, and chitosan citrate) and Eudragit® S100 were developed for the pH-sensitive release of Tenofovir. Films were characterized through texture analysis and scanning electron microscopy (SEM). Swelling and drug release studies were carried out in simulated vaginal fluid and a mixture of simulated vaginal and seminal fluids. Ex vivo mucoadhesion was evaluated in bovine vaginal mucosa. SEM micrographs revealed the formation of multilayer films. According to texture analysis, chitosan citrate was the most flexible compared to chitosan tartrate and lactate. The swelling studies showed a moderate water uptake (<300% in all cases), leading to the sustained release of Tenofovir in simulated vaginal fluid (up to 120 h), which was accelerated in the simulated fluid mixture (4–6 h). The films had high mucoadhesion in bovine vaginal mucosa. The multilayer films formed by a mixture of chitosan citrate and Eudragit® S100 proved to be the most promising, with zero toxicity, excellent mechanical properties, moderate swelling (<100%), high mucoadhesion capacity, and Tenofovir release of 120 h and 4 h in vaginal fluid and the simulated fluid mixture respectively.
dc.description.departmentDepto. de Farmacia Galénica y Tecnología Alimentaria
dc.description.departmentDepto. de Farmacología, Farmacognosia y Botánica
dc.description.facultyFac. de Farmacia
dc.description.refereedTRUE
dc.description.sponsorshipMinisterio de Ciencia e Innovación (MICINN)/FEDER
dc.description.statuspub
dc.eprint.idhttps://eprints.ucm.es/id/eprint/68532
dc.identifier.doi10.3390/md18010044
dc.identifier.issn1660-3397
dc.identifier.officialurlhttps://doi.org/10.3390/md18010044
dc.identifier.relatedurlhttps://www.mdpi.com/1660-3397/18/1/44
dc.identifier.urihttps://hdl.handle.net/20.500.14352/8526
dc.issue.number1
dc.journal.titleMarine Drugs
dc.language.isoeng
dc.page.initial44
dc.publisherMDPI
dc.relation.projectIDMAT2016-76416-R
dc.rightsAtribución 3.0 España
dc.rights.accessRightsopen access
dc.rights.urihttps://creativecommons.org/licenses/by/3.0/es/
dc.subject.keywordchitosan lactate
dc.subject.keywordchitosan tartrate
dc.subject.keywordchitosan citrate
dc.subject.keywordEudragit® S100
dc.subject.keywordlayer-by-layer film
dc.subject.keywordmucoadhesive film
dc.subject.keywordTenofovir controlled release
dc.subject.keywordpH responsive release
dc.subject.keywordvaginal preexposure prophylaxis
dc.subject.keywordHIV sexual transmission
dc.subject.ucmEnfermedades infecciosas
dc.subject.ucmBiología molecular (Farmacia)
dc.subject.ucmFarmacología (Farmacia)
dc.subject.unesco3205.05 Enfermedades Infecciosas
dc.subject.unesco3209 Farmacología
dc.titleVaginal Polyelectrolyte Layer-by-Layer Films Based on Chitosan Derivatives and Eudragit® S100 for pH Responsive Release of Tenofovir
dc.typejournal article
dc.volume.number18
dspace.entity.typePublication
relation.isAuthorOfPublication9650bd31-3f91-48e9-86e2-106ce0fa0fa1
relation.isAuthorOfPublication1e5c77de-d7e9-4ca0-a7d0-90862963a643
relation.isAuthorOfPublication43dc7f8e-706a-45be-9539-21ec412cd069
relation.isAuthorOfPublication29bd420d-26c9-4026-b32c-14d44ef64b88
relation.isAuthorOfPublication.latestForDiscovery9650bd31-3f91-48e9-86e2-106ce0fa0fa1
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