Respirable spray dried vancomycin coated magnetic nanoparticles for localized lung delivery

Int J Pharm. 2022 Jan 5:611:121318. doi: 10.1016/j.ijpharm.2021.121318. Epub 2021 Nov 24.

Abstract

Bacterial pneumonia is a common pulmonary infection responsible for premature death. Biomaterials based-carriers loaded with antibiotics enhance drug potency through localizing the therapy, minimizing the associated adverse effects, and improving patient compliance. Herein, this study reports the preparation of an inhalable dry powder formulation composed of a nano-in-microparticles. Vancomycin was adsorbed on the core of magnetic nanoparticles followed by spray drying into lactose/dextran to optimize the aerodynamic performance and allow the local delivery of the drug into the bacterial pneumonia infection site. Lactose and Dextran are polysaccharides commonly used for pulmonary delivery due to their optimum aerodynamic performance and biocompatibility. The preparation of the nano-in-micro particles with optimum properties was confirmed using FTIR, TEM, SEM, Laser-diffraction, ICP-AES and TGA. The TEM micrographs confirmed the formation of spherical magnetic nanoparticles with a diameter 14.7 ± 5.9 nm and a coating thickness 3 - 16 nm, while laser diffraction showed that outer microparticles exhibited a mean diameter < 5 µm. The formulations demonstrated a promising activity against S. aureus and MRSA and better biocompatibility using MTT assay. In vivo safety and pharmacokinetic studies confirmed the localization of VAN in lung tissue and minimized adverse effects compared to free VAN. Therefore, the developed nano-in-microparticles confers a good potential for eradication of lung infections.

Keywords: MRSA; Magnetic nanoparticles; Microparticles; Pulmonary; Spray drying; Vancomycin.

MeSH terms

  • Humans
  • Lung
  • Magnetite Nanoparticles*
  • Staphylococcus aureus
  • Vancomycin*

Substances

  • Magnetite Nanoparticles
  • Vancomycin