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Original Articles

Lipid-core nanocapsules are an alternative to the pulmonary delivery and to increase the stability of statins

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Pages 317-326 | Received 23 Dec 2018, Accepted 23 May 2019, Published online: 19 Jun 2019
 

Abstract

Aims: Lipid-core nanocapsules (LNCs) loaded with simvastatin (SV, SV-LNC) or lovastatin (LV, LV-LNC) were formulated for pulmonary administration.

Methods: The LNC suspensions were characterized physicochemically, their stability was evaluated, and drug delivery by the pulmonary route was tested in vitro.

Results: The loaded LNCs had a particle size close to 200 nm, a low polydispersity index, and a zeta potential around −20 mV. The encapsulation efficiency was high for SV (99.21 ± 0.7%) but low for LV (20.34 ± 1.2%). SV release from nanocapsules was slower than it was from SV in solution, with a monoexponential release profile, and the drug emitted and aerosol output rate was higher for SV-LNCs (1.58 µg/s) than for SV in suspension (0.54 µg/s).

Conclusions: SV-LNCs had a median aerodynamic diameter of 3.51 µm and a highly respirable fraction (61.9%), indicating that nanoparticles are a suitable system for efficient delivery of simvastatin to the lung.

Disclosure statement

There is no conflict of interest to declare.

Additional information

Funding

The authors thank the financial support of Fundação de Amparo à Pesquisa do estado do Rio Grande do Sul (FAPERGS, Brazil) under Grant 1016671, Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq, Brazil) and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (Capes, Brazil) under Grant 001.

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