The aim of this work was to produce an inhalable dry powder formulation of a new anti-biofilm compound (SC38). For this purpose, chitosan was used as a polymeric carrier and L-leucine as a dispersibility enhancer. SC38 was entrapped by spray-drying into previously optimized chitosan microparticles. The final formulation was fully characterized in vitro in terms of particle morphology, particle size and distribution, flowability, aerodynamic properties, anti-biofilm activity and effects on lung cell viability. The SC38-loaded chitosan microparticles exhibited favorable aerodynamic properties with emitted and respirable fractions higher than 80 % and 45 % respectively. The optimized formulation successfully inhibited biofilm formation at microparticle concentrations starting from 20 μg/mL for methicillin-sensitive and 100 μg/mL for methicillin-resistant Staphylococcus aureus and showed a relatively safe profile in lung cells after 72 h exposure. Future in vivo tolerability and efficacy studies are needed to unravel the potential of this novel formulation for the treatment of difficult-to-treat biofilm-mediated lung infections.

Xiroudaki S., Sabbatini S., Pecoraro C., Cascioferro S., Diana P., Wauthoz N., et al. (2023). Development of a new indole derivative dry powder for inhalation for the treatment of biofilm-associated lung infections. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 631 [10.1016/j.ijpharm.2022.122492].

Development of a new indole derivative dry powder for inhalation for the treatment of biofilm-associated lung infections

Pecoraro C.;Cascioferro S.;Diana P.;
2023-01-01

Abstract

The aim of this work was to produce an inhalable dry powder formulation of a new anti-biofilm compound (SC38). For this purpose, chitosan was used as a polymeric carrier and L-leucine as a dispersibility enhancer. SC38 was entrapped by spray-drying into previously optimized chitosan microparticles. The final formulation was fully characterized in vitro in terms of particle morphology, particle size and distribution, flowability, aerodynamic properties, anti-biofilm activity and effects on lung cell viability. The SC38-loaded chitosan microparticles exhibited favorable aerodynamic properties with emitted and respirable fractions higher than 80 % and 45 % respectively. The optimized formulation successfully inhibited biofilm formation at microparticle concentrations starting from 20 μg/mL for methicillin-sensitive and 100 μg/mL for methicillin-resistant Staphylococcus aureus and showed a relatively safe profile in lung cells after 72 h exposure. Future in vivo tolerability and efficacy studies are needed to unravel the potential of this novel formulation for the treatment of difficult-to-treat biofilm-mediated lung infections.
Xiroudaki S., Sabbatini S., Pecoraro C., Cascioferro S., Diana P., Wauthoz N., et al. (2023). Development of a new indole derivative dry powder for inhalation for the treatment of biofilm-associated lung infections. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 631 [10.1016/j.ijpharm.2022.122492].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/578561
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