Development of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment

Alanood S Almurshedi, 1,* Hessah A Aljunaidel, 2 Bushra Alquadeib, 1 Basmah N Aldosari, 1,* Iman M Alfaqiah, 1 Salma S Almarshidy, 1 Eram KD Eltahir, 1 Amany Z Mohamoud 1 1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Drug Regulatory Affairs, Novart...

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Autores principales: Almurshedi AS, Aljunaidel HA, Alquadeib B, Aldosari BN, Alfagih IM, Almarshidy SS, Eltahir EKD, Mohamoud AZ
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Publicado: Dove Medical Press 2021
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spelling oai:doaj.org-article:10fb590a12374f4d960d04cf72568f432021-12-02T14:25:40ZDevelopment of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment1178-2013https://doaj.org/article/10fb590a12374f4d960d04cf72568f432021-03-01T00:00:00Zhttps://www.dovepress.com/development-of-inhalable-nanostructured-lipid-carriers-for-ciprofloxac-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Alanood S Almurshedi, 1,* Hessah A Aljunaidel, 2 Bushra Alquadeib, 1 Basmah N Aldosari, 1,* Iman M Alfaqiah, 1 Salma S Almarshidy, 1 Eram KD Eltahir, 1 Amany Z Mohamoud 1 1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Drug Regulatory Affairs, Novartis, Riyadh, Saudi Arabia*These authors contributed equally to this workCorrespondence: Alanood S AlmurshediDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 58488, Riyadh, 11594, Saudi ArabiaTel +966 118055013Fax +966 114697507Email marshady@ksu.edu.saPurpose: Ciprofloxacin (CIP) has poor lung targeting after oral inhalation. This study developed optimized inhalable nanostructured lipid carriers (NLCs) for CIP to enhance deposition and accumulation in deeper parts of the lungs for treatment of noncystic fibrosis bronchiectasis (NCFB).Methods: NLC formulations based on stearic acid and oleic acid were successfully prepared by hot homogenization and in vitro-characterized. CIP-NLCs were formulated into nanocomposite micro particles (NCMPs) for administration in dry powder inhalation (DPI) formulations by spray-drying (SD) using different ratios of chitosan (CH) as a carrier. DPI formulations were evaluated for drug content and in vitro deposition, and their mass median aerodynamic diameter (MMAD), fine particle fraction (FPF), fine particle dose (FPD), and emitted dose (ED) were determined.Results: The CIP-NLCs were in the nanometric size range (102.3 ± 4.6 nm), had a low polydispersity index (0.267 ± 0.12), and efficient CIP encapsulation (98.75% ± 0.048%), in addition to a spherical and smooth shape with superior antibacterial activity. The in vitro drug release profile of CIP from CIP-NLCs showed 80% release in 10 h. SD of CIP-NLCs with different ratios of CH generated NCMPs with good yield (> 65%). The NCMPs had a corrugated surface, but with increasing lipid:CH ratios, more spherical, smooth, and homogenous NCMPs were obtained. In addition, there was a significant change in the FPF with increasing lipid:CH ratios (P ˂  0.05). NCMP-1 (lipid:CH = 1:0.5) had the highest FPD (45.0 μg) and FPF (49.2%), while NCMP-3 (lipid:CH = 1:1.5) had the lowest FPF (37.4%). All NCMP powders had an MMAD in the optimum size range of 3.9– 5.1 μm.Conclusion: Novel inhalable CIP NCMP powders are a potential new approach to improved target ability and delivery of CIP for NCFB treatment.Keywords: ciprofloxacin, NCFB, NLCs, NCMPs, DPI, aerosolizationAlmurshedi ASAljunaidel HAAlquadeib BAldosari BNAlfagih IMAlmarshidy SSEltahir EKDMohamoud AZDove Medical Pressarticleciprofloxacinncfbnlcsncmpsdpiaerosolization.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 2405-2417 (2021)
institution DOAJ
collection DOAJ
language EN
topic ciprofloxacin
ncfb
nlcs
ncmps
dpi
aerosolization.
Medicine (General)
R5-920
spellingShingle ciprofloxacin
ncfb
nlcs
ncmps
dpi
aerosolization.
Medicine (General)
R5-920
Almurshedi AS
Aljunaidel HA
Alquadeib B
Aldosari BN
Alfagih IM
Almarshidy SS
Eltahir EKD
Mohamoud AZ
Development of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment
description Alanood S Almurshedi, 1,* Hessah A Aljunaidel, 2 Bushra Alquadeib, 1 Basmah N Aldosari, 1,* Iman M Alfaqiah, 1 Salma S Almarshidy, 1 Eram KD Eltahir, 1 Amany Z Mohamoud 1 1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Drug Regulatory Affairs, Novartis, Riyadh, Saudi Arabia*These authors contributed equally to this workCorrespondence: Alanood S AlmurshediDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 58488, Riyadh, 11594, Saudi ArabiaTel +966 118055013Fax +966 114697507Email marshady@ksu.edu.saPurpose: Ciprofloxacin (CIP) has poor lung targeting after oral inhalation. This study developed optimized inhalable nanostructured lipid carriers (NLCs) for CIP to enhance deposition and accumulation in deeper parts of the lungs for treatment of noncystic fibrosis bronchiectasis (NCFB).Methods: NLC formulations based on stearic acid and oleic acid were successfully prepared by hot homogenization and in vitro-characterized. CIP-NLCs were formulated into nanocomposite micro particles (NCMPs) for administration in dry powder inhalation (DPI) formulations by spray-drying (SD) using different ratios of chitosan (CH) as a carrier. DPI formulations were evaluated for drug content and in vitro deposition, and their mass median aerodynamic diameter (MMAD), fine particle fraction (FPF), fine particle dose (FPD), and emitted dose (ED) were determined.Results: The CIP-NLCs were in the nanometric size range (102.3 ± 4.6 nm), had a low polydispersity index (0.267 ± 0.12), and efficient CIP encapsulation (98.75% ± 0.048%), in addition to a spherical and smooth shape with superior antibacterial activity. The in vitro drug release profile of CIP from CIP-NLCs showed 80% release in 10 h. SD of CIP-NLCs with different ratios of CH generated NCMPs with good yield (> 65%). The NCMPs had a corrugated surface, but with increasing lipid:CH ratios, more spherical, smooth, and homogenous NCMPs were obtained. In addition, there was a significant change in the FPF with increasing lipid:CH ratios (P ˂  0.05). NCMP-1 (lipid:CH = 1:0.5) had the highest FPD (45.0 μg) and FPF (49.2%), while NCMP-3 (lipid:CH = 1:1.5) had the lowest FPF (37.4%). All NCMP powders had an MMAD in the optimum size range of 3.9– 5.1 μm.Conclusion: Novel inhalable CIP NCMP powders are a potential new approach to improved target ability and delivery of CIP for NCFB treatment.Keywords: ciprofloxacin, NCFB, NLCs, NCMPs, DPI, aerosolization
format article
author Almurshedi AS
Aljunaidel HA
Alquadeib B
Aldosari BN
Alfagih IM
Almarshidy SS
Eltahir EKD
Mohamoud AZ
author_facet Almurshedi AS
Aljunaidel HA
Alquadeib B
Aldosari BN
Alfagih IM
Almarshidy SS
Eltahir EKD
Mohamoud AZ
author_sort Almurshedi AS
title Development of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment
title_short Development of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment
title_full Development of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment
title_fullStr Development of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment
title_full_unstemmed Development of Inhalable Nanostructured Lipid Carriers for Ciprofloxacin for Noncystic Fibrosis Bronchiectasis Treatment
title_sort development of inhalable nanostructured lipid carriers for ciprofloxacin for noncystic fibrosis bronchiectasis treatment
publisher Dove Medical Press
publishDate 2021
url https://doaj.org/article/10fb590a12374f4d960d04cf72568f43
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