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Article Dans Une Revue Journal of Controlled Release Année : 2011

Formulation and in vivo evaluation of sodium alendronate spray-dried microparticles intended for lung delivery

Letícia Cruz
  • Fonction : Auteur
Elias Fattal
Leandro Tasso
  • Fonction : Auteur
Gabrielle Freitas
  • Fonction : Auteur
Adriano Carregaro
  • Fonction : Auteur
Sílvia Guterres
  • Fonction : Auteur
Adriana Pohlmann
  • Fonction : Auteur

Résumé

Spray-dried powders for lung delivery of sodium alendronate (SA) were prepared from hydroalcoholic solutions. Formulations display geometric particle size below to 12 µm and spherical shape associated to a hollow structure. The addition of leucine and ammonium bicarbonate leads to porous particles with rough surfaces. The tapped density ranges from 0.016 to 0.062 g/cm 3 , decreasing with the increase of the leucine concentration. For all formulations, the calculated aerodynamic diameters are lower than 5 µm. The in vitro aerodynamic evaluation shows that all powders present a high emitted fraction of 100%, a fine particle fraction ranging from 34.4% to 62.0% and an alveolar fraction ranging from to 23.7% to 42.6%. An optimized sample was evaluated regarding sodium alendronate acute pulmonary toxicity and lung bioavailability. The bronchoalveolar lavage study shows that the intratracheal administration of sodium alendronate dry powder and sodium alendronate aqueous solution do not induce significant increases of lung toxicity indicators as compared with the positive control. Moreover, the intratracheal administration of sodium alendronate dry powder results in a 6.23 ± 0.83% bioavailability, a 3.5-fold increase as compared to oral bioavailability. Finally, these results suggest that sodium alendronate pulmonary delivery could be a new and promising administration route.
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Dates et versions

hal-04101301 , version 1 (19-05-2023)

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Letícia Cruz, Elias Fattal, Leandro Tasso, Gabrielle Freitas, Adriano Carregaro, et al.. Formulation and in vivo evaluation of sodium alendronate spray-dried microparticles intended for lung delivery. Journal of Controlled Release, 2011, 152 (3), pp.370-375. ⟨10.1016/j.jconrel.2011.02.030⟩. ⟨hal-04101301⟩
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