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

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.

Keywords:

• Nanocapsules
• pulmonary delivery
• HPLC
• simvastatin
• lovastatin

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.