Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs

dc.contributor.authorde Araújo, Patricia Rocha [UNESP]
dc.contributor.authorCalixto, Giovana Maria Fioramonti [UNESP]
dc.contributor.authorda Silva, Isabel Cristiane [UNESP]
dc.contributor.authorde Paula Zago, Lucas Henrique [UNESP]
dc.contributor.authorOshiro Junior, João Augusto
dc.contributor.authorPavan, Fernando Rogério [UNESP]
dc.contributor.authorRibeiro, Anderson Orzari
dc.contributor.authorFontana, Carla Raquel [UNESP]
dc.contributor.authorChorilli, Marlus [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionParaíba State University
dc.contributor.institutionUniversidade Federal do ABC (UFABC)
dc.description.abstractThe vaginal mucosa is a very promising route for drug administration due to its high permeability and the possibility to bypass first pass metabolism; however, current vaginal dosage forms present low retention times due to their dilution in vaginal fluids, which hampers the efficacy of many pharmacological treatments. In order to overcome these problems, this study proposes to develop a mucoadhesive in situ gelling liquid crystalline precursor system composed of 30% of oleic acid and cholesterol (7:1), 40% of ethoxylated and propoxylated cetyl alcohol, and 30% of a dispersion of 16% Poloxamer 407. The effect of the dilution with simulated vaginal fluid (SVF) on this system was evaluated by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheological studies, texture profile analysis (TPA), mucoadhesion study, in vitro drug release test using hypericin (HYP) as drug model, and cytotoxicity assay. PLM and SAXS confirmed the formation of an isotropic system. After the addition of three different concentrations of SVF (30, 50, and 100%), the resultant formulations presented anisotropy and characteristics of viscous lamellar phases. Rheology shows that formulations with SVF behaved as a non-Newtonian fluid with suitable shear thinning for vaginal application. TPA and mucoadhesion assays indicated the formation of long-range ordered systems as the amount of SVF increases which may assist in the fixation of the formulation on the vaginal mucosa. The formulations were able to control about 75% of the released HYP demonstrating a sustained release profile. Finally, all formulations acted as safe vaginal drug delivery systems.en
dc.description.affiliationSchool of Pharmaceutical Sciences São Paulo State University (UNESP)
dc.description.affiliationParaíba State University
dc.description.affiliationCenter for Natural Sciences and Humanities Federal University of ABC (UFABC)
dc.description.affiliationUnespSchool of Pharmaceutical Sciences São Paulo State University (UNESP)
dc.identifier.citationAAPS PharmSciTech, v. 20, n. 6, 2019.
dc.relation.ispartofAAPS PharmSciTech
dc.rights.accessRightsAcesso aberto
dc.subjectdrug delivery system
dc.subjectliquid crystalline system
dc.subjectvaginal administration
dc.titleMucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugsen