Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery

Mohammed M Mehanna,1,2 Salma M Mohyeldin,1 Nazik A Elgindy1 1Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonCorrespondence: Mohammed M MehannaDepar...

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Autores principales:	Mehanna MM, Mohyeldin SM, Elgindy NA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	carbohydrate - inhalation - nanocomposite - rifampicin - tuberculosis Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7dc40e6a83dc499581baae5090734096
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spelling	oai:doaj.org-article:7dc40e6a83dc499581baae50907340962021-12-02T04:38:35ZRifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery1178-2013https://doaj.org/article/7dc40e6a83dc499581baae50907340962019-11-01T00:00:00Zhttps://www.dovepress.com/rifampicin-carbohydrate-spray-dried-nanocomposite-a-futuristic-multipa-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Mohammed M Mehanna,1,2 Salma M Mohyeldin,1 Nazik A Elgindy1 1Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonCorrespondence: Mohammed M MehannaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, P.O.Box 11 - 50 - 20 Riad El Solh, Beirut 11072809, LebanonTel +96171708661Email mmhanna@bau.edu.lbPurpose: Rifampicin, a first-line anti-tuberculosis drug, was loaded into a carbohydrate-based spray-dried nanocomposite with the aim to design a dry powder inhalation formulation. This strategy can enable efficient distribution of rifampicin within the lungs, localizing its action, enhancing its bioavailability and reducing its systemic exposure consequently side effects.Methods: The respirable nanocomposite was developed utilizing spray drying of rifampicin nanosuspension employing a combination of mannitol, maltodextrin and leucine as microparticles matrix formers. Detailed physicochemical characterization and in-vitro inhalation properties of the nanocomposite particles were investigated. Compatibility studies were carried out using differential scanning calorimetry and Infrared spectroscopy techniques. Moreover, pulmonary in-vitro cytotoxicity on alveolar basal epithelial cells was performed and evaluated.Results: Nanocomposite-based rifampicin-loaded dry inhalable powder containing maltodextrin, mannitol and leucine at a ratio of 2:1:1 was successfully formulated. Rifampicin loading efficiency into the carbohydrate nanocomposite was in the range of 89.3% to 99.2% w/w with a suitable particle size (3.47–6.80 μm) and unimodal size distribution. Inhalation efficiency of the spray-dried nanosuspension was significantly improved after transforming into an inhalable carbohydrate composite. Specifically, mannitol-based powder had higher respirable fraction (49.91%) relative to the corresponding formulation of maltodextrin. Additionally, IC50 value of rifampicin nanocomposite was statistically significantly higher than that of free drug thus providing superior safety profile on lung tissues.Conclusion: The obtained results suggested that spray drying of rifampicin nanosuspension utilizing carbohydrates as matrix formers can enhance drug inhalation performance and reduce cellular toxicity. Thus, representing an effective safer pulmonary delivery of anti-tuberculosis drugs.Keywords: carbohydrate, inhalation, nanocomposite, rifampicin, tuberculosisMehanna MMMohyeldin SMElgindy NADove Medical Pressarticlecarbohydrate - inhalation - nanocomposite - rifampicin - tuberculosisMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 9089-9112 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	carbohydrate - inhalation - nanocomposite - rifampicin - tuberculosis Medicine (General) R5-920
spellingShingle	carbohydrate - inhalation - nanocomposite - rifampicin - tuberculosis Medicine (General) R5-920 Mehanna MM Mohyeldin SM Elgindy NA Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery
description	Mohammed M Mehanna,1,2 Salma M Mohyeldin,1 Nazik A Elgindy1 1Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonCorrespondence: Mohammed M MehannaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, P.O.Box 11 - 50 - 20 Riad El Solh, Beirut 11072809, LebanonTel +96171708661Email mmhanna@bau.edu.lbPurpose: Rifampicin, a first-line anti-tuberculosis drug, was loaded into a carbohydrate-based spray-dried nanocomposite with the aim to design a dry powder inhalation formulation. This strategy can enable efficient distribution of rifampicin within the lungs, localizing its action, enhancing its bioavailability and reducing its systemic exposure consequently side effects.Methods: The respirable nanocomposite was developed utilizing spray drying of rifampicin nanosuspension employing a combination of mannitol, maltodextrin and leucine as microparticles matrix formers. Detailed physicochemical characterization and in-vitro inhalation properties of the nanocomposite particles were investigated. Compatibility studies were carried out using differential scanning calorimetry and Infrared spectroscopy techniques. Moreover, pulmonary in-vitro cytotoxicity on alveolar basal epithelial cells was performed and evaluated.Results: Nanocomposite-based rifampicin-loaded dry inhalable powder containing maltodextrin, mannitol and leucine at a ratio of 2:1:1 was successfully formulated. Rifampicin loading efficiency into the carbohydrate nanocomposite was in the range of 89.3% to 99.2% w/w with a suitable particle size (3.47–6.80 μm) and unimodal size distribution. Inhalation efficiency of the spray-dried nanosuspension was significantly improved after transforming into an inhalable carbohydrate composite. Specifically, mannitol-based powder had higher respirable fraction (49.91%) relative to the corresponding formulation of maltodextrin. Additionally, IC50 value of rifampicin nanocomposite was statistically significantly higher than that of free drug thus providing superior safety profile on lung tissues.Conclusion: The obtained results suggested that spray drying of rifampicin nanosuspension utilizing carbohydrates as matrix formers can enhance drug inhalation performance and reduce cellular toxicity. Thus, representing an effective safer pulmonary delivery of anti-tuberculosis drugs.Keywords: carbohydrate, inhalation, nanocomposite, rifampicin, tuberculosis
format	article
author	Mehanna MM Mohyeldin SM Elgindy NA
author_facet	Mehanna MM Mohyeldin SM Elgindy NA
author_sort	Mehanna MM
title	Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery
title_short	Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery
title_full	Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery
title_fullStr	Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery
title_full_unstemmed	Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery
title_sort	rifampicin-carbohydrate spray-dried nanocomposite: a futuristic multiparticulate platform for pulmonary delivery
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/7dc40e6a83dc499581baae5090734096
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Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery

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