Poly(glycerol adipate-co-ω-pentadecalactone) spray-dried microparticles as sustained release carriers for pulmonary delivery

Tawfeek, Hesham, Khidr, Sayed, Samy, Eman, Ahmed, Sayed, Murphy, Mark, Mohammed, Afzaal, Shabir, Anjum, Hutcheon, Gillian and Saleem, Imran (2011). Poly(glycerol adipate-co-ω-pentadecalactone) spray-dried microparticles as sustained release carriers for pulmonary delivery. Pharmaceutical Research, 28 (9), pp. 2086-2097.


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±1.57 μg), with a mass median aerodynamic diameter (MMAD) 2.86±0.24 μm. 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±0.16 μg and MMAD 2.18±0.35-2. 98±0.25 μm, L-leucine:%FPF 36.90±3.6-43.38±5. 6; FPD 18.66±2.90-21.58±2.46 μg and MMAD 2.55±0.03-3. 68±0.12 μm). 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) (5 mg/ml) and poly(lactide-co-glycolide), (5 mg/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 72 h 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.

Publication DOI: https://doi.org/10.1007/s11095-011-0433-6
Divisions: Life & Health Sciences > Pharmacy
Life & Health Sciences
Life & Health Sciences > Applied Health Research Group
Uncontrolled Keywords: dry powder inhalation,microparticles,polyester polymers,pulmonary drug delivery,sustained drug release,Pharmaceutical Science,Organic Chemistry,Molecular Medicine,Pharmacology (medical),Biotechnology,Pharmacology
Full Text Link: http://research ... jmu.ac.uk/2123/
Related URLs: http://www.scop ... tnerID=8YFLogxK (Scopus URL)
http://link.spr ... 1095-011-0433-6 (Publisher URL)
Published Date: 2011-09
Authors: Tawfeek, Hesham
Khidr, Sayed
Samy, Eman
Ahmed, Sayed
Murphy, Mark
Mohammed, Afzaal ( 0000-0002-5212-3040)
Shabir, Anjum
Hutcheon, Gillian
Saleem, Imran

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