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Eur J Pharm Sci. 2016 Apr 30;86:34-40. doi: 10.1016/j.ejps.2016.02.023. Epub 2016 Mar 2.

Influence of amine-modified poly(vinyl alcohol)s on vibrating-membrane nebulizer performance and lung toxicity.

Author information

1
Medical Clinic II, Department of Internal Medicine, Justus-Liebig-Universität, Giessen, Germany; Department of Pharmaceutics and Biopharmacy, Philipps-Universität, Marburg, Germany. Electronic address: moritz.beck-broichsitter@innere.med.uni-giessen.de.
2
Department of Pharmaceutics and Biopharmacy, Philipps-Universität, Marburg, Germany.
3
Department of Pharmaceutical Sciences, State University of New York, Buffalo, USA.
4
Medical Clinic II, Department of Internal Medicine, Justus-Liebig-Universität, Giessen, Germany.

Abstract

A suitable aerosol droplet size and formulation output rate is essential for the therapy of lung diseases under application of nebulizers. The current study investigated the potential of amine-modified poly(vinyl alcohol)s as excipients for inhalation delivery. A change of conductivity (effective at <0.1mg/ml) and viscosity (effective at >0.1mg/ml) of samples that were supplemented with charge-modified polymers had a significant influence on the generated droplet size (shift from ~8 to ~4 μm) and formulation throughput rate (shift from ~0.2 to ~1.0 g/min), where polymers with a higher amine density (and molecular weight) showed an elevated activity. Biocompatibility assessment of polymers in A549 cells and an isolated lung model resulted in cell lysis and lung edema formation dependent on the type (degree of amine substitution) and dose of polymer applied. Suitable compositions and concentrations of amine-modified poly(vinyl alcohol)s were identified with respect to an optimized nebulizer performance and acceptable biocompatibility. Charge-modified polymers represent novel excipients with potential to improve inhalation therapy.

KEYWORDS:

Aerosol; Amine-modified poly(vinyl alcohol); Lung delivery; Toxicity; Vibrating-membrane nebulizer

PMID:
26946442
DOI:
10.1016/j.ejps.2016.02.023
[Indexed for MEDLINE]

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