Mucoadhesive Vaginal Discs based on Cyclodextrin and Surfactants for the Controlled Release of Antiretroviral Drugs to Prevent the Sexual Transmission of HIV

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dc.contributor.authorNotario Pérez, Fernando
dc.contributor.authorMartín Illana, Araceli
dc.contributor.authorCazorla Luna, Raúl
dc.contributor.authorRuiz Caro, Roberto
dc.contributor.authorTamayo, Aitana
dc.contributor.authorRubio, Juan
dc.contributor.authorVeiga Ochoa, María Dolores
dc.date.accessioned2023-06-17T08:21:59Z
dc.date.available2023-06-17T08:21:59Z
dc.date.issued2020-04-02
dc.description.abstractThe strategies for developing vaginal microbicides to protect women against human immunodeficiency virus (HIV) sexual transmission are constantly changing. Although the initial dosage forms required daily administration to offer effective protection, the trend then moved towards sustained-release dosage forms that require less frequency of administration in order to improve women’s compliance with the treatment. Nevertheless, another possible strategy is to design on-demand products that can be used in a coitally-dependent manner and only need to be administered immediately before intercourse to offer protection. Vaginal discs based on freeze-dried hydroxypropylmethyl cellulose gels have been developed for this purpose, containing two surfactants, i.e., sodium dodecyl sulphate and polysorbate 60, alone or in combination with 2-hydroxypropyl-β cyclodextrin, to achieve a formulation capable of incorporating both hydrophilic and lipophilic drugs. Several studies have been carried out to evaluate how the inclusion of these substances modifies the structure of gels (viscosity and consistency studies) and the porosimetry of the freeze-dried discs (scanning electron microscopy micrographs, mechanical properties, swelling behaviour). The drug release and mucoadhesive properties of the discs have also been evaluated with a view to their clinical application. The systems combining sodium dodecyl sulphate and 2-hydroxypropyl-β-cyclodextrin were found to be adequate for the vaginal administration of both Tenofovir and Dapivirine and also offer excellent mucoadhesion to vaginal tissue; these discs could therefore be an interesting option for a coitally-dependent administration to protect women against HIV transmission.
dc.description.departmentDepto. de Farmacia Galénica y Tecnología Alimentaria
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/70308
dc.identifier.doi10.3390/pharmaceutics12040321
dc.identifier.issn1999-4923
dc.identifier.officialurlhttps://doi.org/10.3390/pharmaceutics12040321
dc.identifier.relatedurlhttps://www.mdpi.com/1999-4923/12/4/321
dc.identifier.urihttps://hdl.handle.net/20.500.14352/6779
dc.issue.number4
dc.journal.titlePharmaceutics
dc.language.isoeng
dc.page.initial321
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.cdu615.01/.03
dc.subject.keywordcoitally-dependent microbicide
dc.subject.keyworddapivirine
dc.subject.keywordfreeze-dried gels
dc.subject.keywordhuman immunodeficiency virus
dc.subject.keyword2-hydroxypropyl-β-cyclodextrin
dc.subject.keywordmucoadhesive vaginal discs
dc.subject.keywordsurfactant
dc.subject.keywordtenofovir
dc.subject.ucmFarmacología (Farmacia)
dc.subject.unesco3209 Farmacología
dc.titleMucoadhesive Vaginal Discs based on Cyclodextrin and Surfactants for the Controlled Release of Antiretroviral Drugs to Prevent the Sexual Transmission of HIV
dc.typejournal article
dc.volume.number12
dspace.entity.typePublication
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relation.isAuthorOfPublication1e5c77de-d7e9-4ca0-a7d0-90862963a643
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relation.isAuthorOfPublication.latestForDiscovery43dc7f8e-706a-45be-9539-21ec412cd069
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