Nanoencapsulation of a glucocorticoid improves barrier function and anti-inflammatory effect on monolayers of pulmonary epithelial cell lines.

Autor: Rigo LA; Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil., Carvalho-Wodarz CS; Drug Delivery (DDEL), Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), University Campus, Building E8.1, D-66123 Saarbrücken, Germany., Pohlmann AR; Departamento de Química Orgânica, Instituto de Química, UFRGS, Av. Bento Gonçalves 9500, 91501-970, Brazil., Guterres SS; Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil., Schneider-Daum N; Drug Delivery (DDEL), Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), University Campus, Building E8.1, D-66123 Saarbrücken, Germany., Lehr CM; Drug Delivery (DDEL), Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), University Campus, Building E8.1, D-66123 Saarbrücken, Germany., Beck RCR; Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil. Electronic address: ruy.beck@ufrgs.br.
Jazyk: angličtina
Zdroj: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V [Eur J Pharm Biopharm] 2017 Oct; Vol. 119, pp. 1-10. Date of Electronic Publication: 2017 May 13.
DOI: 10.1016/j.ejpb.2017.05.006
Abstrakt: The anti-inflammatory effect of polymeric deflazacort nanocapsules (NC-DFZ) was investigated, and possible improvement of epithelial barrier function using filter grown monolayers of Calu-3 cells was assessed. NC prepared from poly(ε-caprolactone) (PCL) had a mean size around 200nm, slightly negative zeta potential (∼-8mV), and low polydispersity index (<0.10). Encapsulation of DFZ had an efficiency of 85%. No cytotoxic effects were observed at particle concentration of 9.85×10 11 NC/ml, which was therefore chosen to evaluate the effect of NC-DFZ at 1% (w/v) of PCL and 0.5% (w/v) of DFZ on the epithelial barrier function of Calu-3 monolayers. Nanoencapsulated drug at 0.5% (w/v) increased transepithelial electrical resistance and decreased permeability of the paracellular marker sodium fluorescein, while non-encapsulated DFZ failed to improve these parameters. Moreover, NC-DFZ reduced the lipopolysaccharide (LPS) mediated secretion of the inflammatory marker IL-8. In vitro dissolution testing revealed controlled release of DFZ from nanocapsules, which may explain the improved effect of DFZ on the cells. These data suggest that nanoencapsulation of pulmonary delivered corticosteroids could be advantageous for the treatment of inflammatory conditions, such as asthma and chronic obstructive pulmonary diseases.
(Copyright © 2017 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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