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Development of inhalable hyaluronan/mannitol composite dry powders for flucytosine repositioning in local therapy of lung infections.
Costabile, G; d'Angelo, I; d'Emmanuele di Villa Bianca, R; Mitidieri, E; Pompili, B; Del Porto, P; Leoni, L; Visca, P; Miro, A; Quaglia, F; Imperi, F; Sorrentino, R; Ungaro, F.
Afiliación
  • Costabile G; Laboratory of Drug Delivery, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
  • d'Angelo I; Di.S.T.A.Bi.F., Second University of Napoli, Via Vivaldi 43, 81100 Caserta, Italy.
  • d'Emmanuele di Villa Bianca R; Laboratory of Pharmacology, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
  • Mitidieri E; Laboratory of Pharmacology, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
  • Pompili B; Department of Biology and Biotechnology "Charles Darwin", Sapienza University of Roma, Via dei Sardi 70, 00185 Roma, Italy.
  • Del Porto P; Department of Biology and Biotechnology "Charles Darwin", Sapienza University of Roma, Via dei Sardi 70, 00185 Roma, Italy.
  • Leoni L; Department of Sciences, University Roma Tre, Viale Marconi, 446, 00146 Roma, Italy.
  • Visca P; Department of Sciences, University Roma Tre, Viale Marconi, 446, 00146 Roma, Italy.
  • Miro A; Laboratory of Drug Delivery, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
  • Quaglia F; Laboratory of Drug Delivery, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
  • Imperi F; Department of Biology and Biotechnology "Charles Darwin", Sapienza University of Roma, Via dei Sardi 70, 00185 Roma, Italy.
  • Sorrentino R; Laboratory of Pharmacology, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
  • Ungaro F; Laboratory of Drug Delivery, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy. Electronic address: ungaro@unina.it.
J Control Release ; 238: 80-91, 2016 09 28.
Article en En | MEDLINE | ID: mdl-27449745
Flucytosine (5-fluorocytosine, 5-FC) is a fluorinated analogue of cytosine currently approved for the systemic treatment of fungal infections, which has recently demonstrated a very promising antivirulence activity against the bacterial pathogen Pseudomonas aeruginosa. In this work, we propose novel inhalable hyaluronic acid (HA)/mannitol composite dry powders for repositioning 5-FC in the local treatment of lung infections, including those affecting cystic fibrosis (CF) patients. Different dry powders were produced in one-step by spray-drying. Powder composition and process conditions were selected after in depth formulation studies aimed at selecting the 5-FC/HA/mannitol formulation with convenient aerosolization properties and drug release profile in simulated lung fluids. The optimized 5-FC/HA/mannitol powder for inhalation (HyaMan_FC#3) was effectively delivered from different breath-activated dry powder inhalers (DPI) already available to CF patients. Nevertheless, the aerodynamic assessment of fine particles suggested that the developed formulation well fit with a low-resistance DPI. HyaMan_FC#3 inhibited the growth of the fungus Candida albicans and the production of the virulence factor pyoverdine by P. aeruginosa at 5-FC concentrations that did not affect the viability of both wild type (16HBE14o-) and CF (CFBE41o-) human bronchial epithelial cells. Finally, pharmacokinetics of HyaMan_FC#3 inhalation powder and 5-FC solution after intratracheal administration in rats were compared. In vivo results clearly demonstrated that, when formulated as dry powder, 5-FC levels in both bronchoalveolar lavage fluid and lung tissue were significantly higher and sustained over time as compared to those obtained with the 5-FC solution. Of note, when the same 5-FC amount was administered intravenously, no significant drug amount was found in the lung at each time point from the injection. To realize a 5-FC lung concentration similar to that obtained by using HyaMan_FC#3, a 6-fold higher dose of 5-FC should be administered intravenously. Taken together, our data demonstrate the feasibility to deliver 5-FC by the pulmonary route likely avoiding/reducing the well-known side effects associated to the high systemic 5-FC doses currently used in humans. Furthermore, our results highlight that an appropriate formulation design can improve the persistence of the drug at lungs, where microorganisms causing severe infections are located.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Reposicionamiento de Medicamentos / Inhaladores de Polvo Seco / Flucitosina / Ácido Hialurónico / Manitol / Antibacterianos / Antifúngicos Límite: Animals / Humans / Male Idioma: En Revista: J Control Release Asunto de la revista: FARMACOLOGIA Año: 2016 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Países Bajos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Reposicionamiento de Medicamentos / Inhaladores de Polvo Seco / Flucitosina / Ácido Hialurónico / Manitol / Antibacterianos / Antifúngicos Límite: Animals / Humans / Male Idioma: En Revista: J Control Release Asunto de la revista: FARMACOLOGIA Año: 2016 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Países Bajos