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Utilize este identificador para referenciar este registo: http://hdl.handle.net/10314/4052

Título: Lyophilized tablets for focal delivery of fluconazole and itraconazole through vaginal mucosa, rational design and in vitro evaluation
Autores: Valle, Maria José de Jesús
Coutinho, Paula
Ribeiro, Maximiano Prata
Navarro, Amparo Sánchez
Palavras Chave: Vaginal delivery
Liposomes
Albumin microparticles
Lyophilized tablets
Itraconazole
Fluconazole
Data: Sep-2018
Citação: Maria José de Jesús Valle, Paula Coutinho, Maximiano Prata Ribeiro, Amparo Sánchez Navarro, Lyophilized tablets for focal delivery of fluconazole and itraconazole through vaginal mucosa, rational design and in vitro evaluation, European Journal of Pharmaceutical Sciences, Volume 122, 2018, Pages 144-151
Resumo: The present work deals with the rational design and in vitro evaluation of vaginal tablets for focal delivery of fluconazole (FLZ) and itraconazol (ITZ). Drug loaded liposomes with and without d-alpha-tocopheryl polyethylene glycol 1000 succinate (vit E TPGS) were prepared by direct sonication of the components and mixed with albumin to obtain albusomes. Tablets were obtained by direct compression of the lyophilized cake. The influence of vit E TPGS on size, zeta potential and entrapment efficiency (EE%) of liposomes and albusomes was evaluated. Tablet swelling and drug release were studied by in vitro assays. Vit E TPGS neither affected the zeta potential nor the EE% of liposomes and albusomes, but affected the liposomes size and the tablet disintegration time. A rapid erosion was observed for the tablets with the highest content of vitamin, while a slow swelling for those lacking the vitamin (swelling index = 57.76 ± 13.51%). A faster drug release profile was obtained for the former compared to the latter. The in vitro assay showed that FLZ diffused and solved in the vaginal fluid simulant while ITZ remained into the albusomes, which slowly released ITZ-albumin complex and ITZ-loaded liposomes, both suitable carriers for drug transport to deeper vaginal endothelium.
URI: http://hdl.handle.net/10314/4052
Aparece nas Colecções:Artigos em Revista Internacional (ESS)

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