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Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles

Inhalable dry powders containing poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were developed for the delivery of tadalafil (TAD) for treatment of life-treating pulmonary arterial hypertension. Taguchi design was employed to evaluate the effects of different formulation variables on the ph...

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Autores principales: Varshosaz, Jaleh, Taymouri, Somayeh, Hamishehkar, Hamed, Vatankhah, Razieh, Yaghubi, Shadi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5465831/
https://www.ncbi.nlm.nih.gov/pubmed/28626480
http://dx.doi.org/10.4103/1735-5362.207203
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author Varshosaz, Jaleh
Taymouri, Somayeh
Hamishehkar, Hamed
Vatankhah, Razieh
Yaghubi, Shadi
author_facet Varshosaz, Jaleh
Taymouri, Somayeh
Hamishehkar, Hamed
Vatankhah, Razieh
Yaghubi, Shadi
author_sort Varshosaz, Jaleh
collection PubMed
description Inhalable dry powders containing poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were developed for the delivery of tadalafil (TAD) for treatment of life-treating pulmonary arterial hypertension. Taguchi design was employed to evaluate the effects of different formulation variables on the physicochemical characteristics of PLGA-NPs prepared using emulsion solvent evaporation method. Inhalable PLGA-NPs of TAD were successfully prepared by co-spray drying the PLGA-NPs with inert carriers. Physicochemical characteristics and in vitro deposition of the aerosolized drug were also evaluated. The optimized formulation was prepared using 7.5 mg of PLGA, 2.5 mg of TAD, sonication time of 6 min and 2% polyvinyl alcohol (PVA) as the stabilizer. The optimized aqueous/oil phase ratio for PLGA-NPs preparation was 10:1. Polymer/drug ratio was the most effective parameter on the release efficiency. Encapsulation efficiency, zeta potential and particle size of PLGA-NPs were more affected by aqueous/organic phase ratio. The spray dried powders containing PLGA-NPs had a mass median aerodynamic diameter (MMAD) in the range of 1.4–2.8 μm that was suitable for TAD delivery to the deep region of lung. The presence of L- leucine in mannitol containing formulations decreased the interparticulate forces between particles and increased significantly the process yield and fine particle fraction (FPF). The results indicated that prepared dry powders containing TAD-loaded PLGA-NPs were suitable for inhalation and has the potential for the treatment of pulmonary arterial hypertension.
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spelling pubmed-54658312017-06-16 Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles Varshosaz, Jaleh Taymouri, Somayeh Hamishehkar, Hamed Vatankhah, Razieh Yaghubi, Shadi Res Pharm Sci Original Article Inhalable dry powders containing poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were developed for the delivery of tadalafil (TAD) for treatment of life-treating pulmonary arterial hypertension. Taguchi design was employed to evaluate the effects of different formulation variables on the physicochemical characteristics of PLGA-NPs prepared using emulsion solvent evaporation method. Inhalable PLGA-NPs of TAD were successfully prepared by co-spray drying the PLGA-NPs with inert carriers. Physicochemical characteristics and in vitro deposition of the aerosolized drug were also evaluated. The optimized formulation was prepared using 7.5 mg of PLGA, 2.5 mg of TAD, sonication time of 6 min and 2% polyvinyl alcohol (PVA) as the stabilizer. The optimized aqueous/oil phase ratio for PLGA-NPs preparation was 10:1. Polymer/drug ratio was the most effective parameter on the release efficiency. Encapsulation efficiency, zeta potential and particle size of PLGA-NPs were more affected by aqueous/organic phase ratio. The spray dried powders containing PLGA-NPs had a mass median aerodynamic diameter (MMAD) in the range of 1.4–2.8 μm that was suitable for TAD delivery to the deep region of lung. The presence of L- leucine in mannitol containing formulations decreased the interparticulate forces between particles and increased significantly the process yield and fine particle fraction (FPF). The results indicated that prepared dry powders containing TAD-loaded PLGA-NPs were suitable for inhalation and has the potential for the treatment of pulmonary arterial hypertension. Medknow Publications & Media Pvt Ltd 2017-06 /pmc/articles/PMC5465831/ /pubmed/28626480 http://dx.doi.org/10.4103/1735-5362.207203 Text en Copyright: © 2017 Research in Pharmaceutical Sciences http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.
spellingShingle Original Article
Varshosaz, Jaleh
Taymouri, Somayeh
Hamishehkar, Hamed
Vatankhah, Razieh
Yaghubi, Shadi
Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles
title Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles
title_full Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles
title_fullStr Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles
title_full_unstemmed Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles
title_short Development of dry powder inhaler containing tadalafil-loaded PLGA nanoparticles
title_sort development of dry powder inhaler containing tadalafil-loaded plga nanoparticles
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5465831/
https://www.ncbi.nlm.nih.gov/pubmed/28626480
http://dx.doi.org/10.4103/1735-5362.207203
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