Novel levodopa microparticles for pulmonary delivery and in vivo respiratory tract toxicity study

Rubia Lazzaretti Pereira; Aline Bergesch Barth; Leandro Tasso; Renata Platcheck Raffin; Silvia S. Guterres; Elfrides Eva Scherman Schapoval†

doi:10.22456/2527-2616.150700

Authors

Rubia Lazzaretti Pereira Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul (UFRGS) https://orcid.org/0009-0003-0686-1493
Aline Bergesch Barth Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul (UFRGS) https://orcid.org/0000-0002-4788-6051
Leandro Tasso Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul (UFRGS); Curso de Farmácia, Universidade de Caxias do Sul (UCS) https://orcid.org/0000-0001-7102-9204
Renata Platcheck Raffin Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul (UFRGS) https://orcid.org/0000-0001-6432-9997
Silvia S. Guterres Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul (UFRGS); Universidade Federal da Bahia (UFBA)
Elfrides Eva Scherman Schapoval† Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul (UFRGS)

DOI:

https://doi.org/10.22456/2527-2616.150700

Keywords:

pulmonary, drug delivery, microparticles, lung toxicity, inhaled therapy

Abstract

The aim of this study was to develop microparticles containing levodopa and a new combination of polymers for lung delivery and evaluate the pulmonary cytotoxicity in vivo of this novel formulation. Spray-drying technique was used to produce the powders containing levodopa, chitosan, HPMC and hyaluronic acid at different proportions and conditions. In addition, a cytotoxicity assay in rats was performed to evaluate the pulmonary membrane damage. The results showed good drug loading capacity (97.30% ± 0.5) and the obtained microparticles presented appropriate aerodynamic diameter for pulmonary delivery (4.18 ± 0.09 µm). The fine particle fraction found was 25.49 % and the bronchoalveolar lavage (BAL) study in vivo showed that levodopa microparticles did not cause considerable increment on the activity of marker enzymes in relation to the untreated control group. Therefore, no respiratory tract toxicity was observed with this novel formulation. The results also present an innovative combination of polymers for lung delivery.

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