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

J Microencapsul. 2019 Jun;36(4):317-326. doi: 10.1080/02652048.2019.1624849. Epub 2019 Jun 19.

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: HPLC; Nanocapsules; lovastatin; pulmonary delivery; simvastatin.

MeSH terms

  • Drug Delivery Systems
  • Drug Liberation
  • Drug Stability
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / administration & dosage*
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / chemistry
  • Lipids / chemistry
  • Lovastatin / administration & dosage*
  • Lovastatin / chemistry
  • Nanocapsules / chemistry*
  • Nebulizers and Vaporizers
  • Particle Size
  • Simvastatin / administration & dosage*
  • Simvastatin / chemistry

Substances

  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Lipids
  • Nanocapsules
  • Lovastatin
  • Simvastatin