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

Authors Almurshedi AS, Aljunaidel HA, Alquadeib B, Aldosari BN, Alfagih IM, Almarshidy SS, Eltahir EKD, Mohamoud AZ

Received 2 November 2020

Accepted for publication 9 March 2021

Published 25 March 2021 Volume 2021:16 Pages 2405—2417


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Dr Yan Shen

Alanood S Almurshedi, 1,* Hessah A Aljunaidel, 2 Bushra Alquadeib, 1 Basmah N Aldosari, 1,* Iman M Alfagih, 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 work

Correspondence: Alanood S Almurshedi
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 58488, Riyadh, 11594, Saudi Arabia
Tel +966 118055013
Fax +966 114697507
Email [email protected]

Purpose: 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

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