Journalartikel

Nebulization performance of biodegradable sildenafil-loaded nanoparticles using the Aeroneb® Pro: Formulation aspects and nanoparticle stability to nebulization


AutorenlisteBeck-Broichsitter, Moritz; Kleimann, Pia; Gessler, Tobias; Seeger, Werner; Kissel, Thomas; Schmehl, Thomas

Jahr der Veröffentlichung2012

Seiten398-408

ZeitschriftInternational Journal of Pharmaceutics

Bandnummer422

Heftnummer1-2

ISSN0378-5173

eISSN1873-3476

DOI Linkhttps://doi.org/10.1016/j.ijpharm.2011.10.012

VerlagElsevier


Abstract

Polymeric nanoparticles meet the increasing interest for drug delivery applications and hold great promise to improve controlled drug delivery to the lung. Here, we present a series of investigations that were carried out to understand the impact of formulation variables on the nebulization performance of novel biodegradable sildenafil-loaded nanoparticles designed for targeted aerosol therapy of life-threatening pulmonary arterial hypertension.

Narrowly distributed poly(D, L-lactide-co-glycolide) nanoparticles (size: similar to 200 nm) were prepared by a solvent evaporation technique using poly(vinyl alcohol) (PVA) as stabilizer. The aerodynamic and output characteristics using the Aeroneb (R) Pro nebulizer correlated well with the dynamic viscosity of the employed fluids for nebulization. The nebulization performance was mainly affected by the amount of employed stabilizer, rather than by the applied nanoparticle concentration. Nanoparticles revealed physical stability against forces generated during aerosolization, what is attributed to the adsorbed PVA layer around the nanoparticles. Sildenafil was successfully encapsulated into nanoparticles (encapsulation efficiency: similar to 80%). Size, size distribution and sildenafil content of nanoparticles were not affected by nebulization and the in vitro drug release profile demonstrated a sustained sildenafil release over similar to 120 min.

The current study suggests that the prepared sildenafil-loaded nanoparticles are a promising pharmaceutical for the therapy of pulmonary arterial hypertension. (c) 2011 Elsevier B.V. All rights reserved.




Zitierstile

Harvard-ZitierstilBeck-Broichsitter, M., Kleimann, P., Gessler, T., Seeger, W., Kissel, T. and Schmehl, T. (2012) Nebulization performance of biodegradable sildenafil-loaded nanoparticles using the Aeroneb® Pro: Formulation aspects and nanoparticle stability to nebulization, International Journal of Pharmaceutics, 422(1-2), pp. 398-408. https://doi.org/10.1016/j.ijpharm.2011.10.012

APA-ZitierstilBeck-Broichsitter, M., Kleimann, P., Gessler, T., Seeger, W., Kissel, T., & Schmehl, T. (2012). Nebulization performance of biodegradable sildenafil-loaded nanoparticles using the Aeroneb® Pro: Formulation aspects and nanoparticle stability to nebulization. International Journal of Pharmaceutics. 422(1-2), 398-408. https://doi.org/10.1016/j.ijpharm.2011.10.012



Schlagwörter


AEROSOL GENERATIONBiodegradable polyestersDRUG-DELIVERYNEBULIZATIONPLGAPOLYMERIC NANOPARTICLESpulmonary arterial hypertensionPULMONARY ARTERIAL-HYPERTENSIONpulmonary drug deliverySILDENAFILsolvent evaporation


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