caa a22 4500 445311894 CHVBK 20180317142633.0 cr unu---uuuuu 170323e20110901xx s 000 0 eng 10.1007/s11095-011-0433-6 doi (NATIONALLICENCE)springer-10.1007/s11095-011-0433-6 Poly(Glycerol Adipate-co-ω-Pentadecalactone) Spray-Dried Microparticles as Sustained Release Carriers for Pulmonary Delivery [Elektronische Daten] [Hesham Tawfeek, Sayed Khidr, Eman Samy, Sayed Ahmed, Mark Murphy, Afzaal Mohammed, Anjum Shabir, Gillian Hutcheon, Imran Saleem] ABSTRACT: Purpose: The aim of this work was to optimize biodegradable polyester poly(glycerol adipate-co-ω-pentadecalactone), PGA-co-PDL, microparticles as sustained release (SR) carriers for pulmonary drug delivery. Methods: Microparticles were produced by spray drying directly from double emulsion with and without dispersibility enhancers (L-arginine and L-leucine) (0.5-1.5%w/w) using sodium fluorescein (SF) as a model hydrophilic drug. Results: Spray-dried microparticles without dispersibility enhancers exhibited aggregated powders leading to low fine particle fraction (%FPF) (28.79 ± 3.24), fine particle dose (FPD) (14.42 ± 1.57μg), with a mass median aerodynamic diameter (MMAD) 2.86 ± 0.24μm. However, L-leucine was significantly superior in enhancing the aerosolization performance (L-arginine:%FPF 27.61 ± 4.49-26.57 ± 1.85; FPD 12.40 ± 0.99-19.54 ± 0.16μg and MMAD 2.18 ± 0.35-2.98 ± 0.25μm, L-leucine:%FPF 36.90 ± 3.6-43.38 ± 5.6; FPD 18.66 ± 2.90-21.58 ± 2.46μg and MMAD 2.55 ± 0.03-3.68 ± 0.12μm). Incorporating L-leucine (1.5%w/w) reduced the burst release (24.04 ± 3.87%) of SF compared to unmodified formulations (41.87 ± 2.46%), with both undergoing a square root of time (Higuchi's pattern) dependent release. Comparing the toxicity profiles of PGA-co-PDL with L-leucine (1.5%w/w) (5mg/ml) and poly(lactide-co-glycolide), (5mg/ml) spray-dried microparticles in human bronchial epithelial 16HBE14o- cell lines, resulted in cell viability of 85.57 ± 5.44 and 60.66 ± 6.75%, respectively, after 72h treatment. Conclusion: The above data suggest that PGA-co-PDL may be a useful polymer for preparing SR microparticle carriers, together with dispersibility enhancers, for pulmonary delivery. Springer Science+Business Media, LLC, 2011 dry powder inhalation nationallicence microparticles nationallicence polyester polymers nationallicence pulmonary drug delivery nationallicence sustained drug release nationallicence Tawfeek Hesham School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut Khidr Sayed Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt aut Samy Eman Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt aut Ahmed Sayed Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt aut Murphy Mark School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut Mohammed Afzaal Aston Pharmacy School, Aston University, Birmingham, UK aut Shabir Anjum Aston Pharmacy School, Aston University, Birmingham, UK aut Hutcheon Gillian School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut Saleem Imran School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut Pharmaceutical Research Springer US; http://www.springer-ny.com 28/9(2011-09-01), 2086-2097 0724-8741 28:9<2086 2011 28 11095 https://doi.org/10.1007/s11095-011-0433-6 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s11095-011-0433-6 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Tawfeek Hesham School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut NATIONALLICENCE 700 1- Khidr Sayed Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt aut NATIONALLICENCE 700 1- Samy Eman Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt aut NATIONALLICENCE 700 1- Ahmed Sayed Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt aut NATIONALLICENCE 700 1- Murphy Mark School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut NATIONALLICENCE 700 1- Mohammed Afzaal Aston Pharmacy School, Aston University, Birmingham, UK aut NATIONALLICENCE 700 1- Shabir Anjum Aston Pharmacy School, Aston University, Birmingham, UK aut NATIONALLICENCE 700 1- Hutcheon Gillian School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut NATIONALLICENCE 700 1- Saleem Imran School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, L3 3AF, Liverpool, UK aut NATIONALLICENCE 773 0- Pharmaceutical Research Springer US; http://www.springer-ny.com 28/9(2011-09-01), 2086-2097 0724-8741 28:9<2086 2011 28 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer