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Poly(Glycerol Adipate-co-ω-Pentadecalactone) Spray-Dried Microparticles as Sustained Release Carriers for Pulmonary Delivery

Tawfeek, H and Khidr, S and Samy, E and Ahmed, S and Murphy, MF and Mohammed, A and Shabir, A and Hutcheon, GA and Saleem, IY (2011) Poly(Glycerol Adipate-co-ω-Pentadecalactone) Spray-Dried Microparticles as Sustained Release Carriers for Pulmonary Delivery. Pharmaceutical Research, 28 (9). pp. 2086-2097. ISSN 0724-8741

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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.

Item Type: Article
Additional Information: The original publication is available at www.springerlink.com
Uncontrolled Keywords: 1115 Pharmacology And Pharmaceutical Sciences
Subjects: R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Divisions: Pharmacy & Biomolecular Sciences
Publisher: Springer Netherlands
Related URLs:
Date Deposited: 11 Nov 2015 08:22
Last Modified: 11 Nov 2015 08:22
URI: http://researchonline.ljmu.ac.uk/id/eprint/2123

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