Ultra-small, highly negatively charged archaeolipid nanoparticles for active targeting to macrophages of the inflamed mucosa

HIGA L, JEREZ H, DE FARIAS MA, PORTUGALRV, ROMERO EL, MORILLA MJ.

NANOMEDICINE

FUTURE MEDICINE LTD

Lugar: Londres; Año: 2017

1743-5889

Aims.Develop nanoparticulate agents for oral targeted delivery of dexamethasone (Dex) to macrophages of inflamed mucosa.Materials  methods.Solid archaeolipid nanoparticles (SAN-Dex) (compritol/ Halorubrum tebenquichensepolar archaeolipids/ soybean phosphatidylcholine/ Tween 80 4; 0.9; 0.3; 3% w/w) loaded with Dex were prepared. Their mucopenetration, stability under digestion, and in vitroanti-inflammatory activity, were determined.Results and conclusions.Ultra-smallSAN-Dex strongly reduced the levels of TNF-α, IL-6 and IL-12 on J774A1 cells stimulated with LPS as compared to free Dex or loaded in ordinary solid lipid nanoparticles (SLN-Dex). After in vitro digestion,the anti-inflammatory activity of SAN-Dex was retained, while that of SLN-Dex was lost. Because of their structural and pharmacodynamic features, SAN-Dex may be suitable for oral targeted delivery to inflamed mucosa.