Ultra-small solid archaeolipid nanoparticles for active targeting to macrophages of the inflamed mucosa. (May 2017)

• Record Type: Journal Article
• Authors: Higa, Leticia Herminia; Jerez, Horacio Emanuel; de Farias, Marcelo Alexandre; Portugal, Rodrigo Villares; Romero, Eder Lilia; Morilla, Maria Jose
• Is Part Of: Nanomedicine. Volume 12:Number 10(2017)
• Page Start: 1165
• Page End: 1175
• Publication Date: 2017-05
• Subjects: digestion stability -- inflammatory bowel disease -- oral delivery; Nanotechnology -- Periodicals; Medical technology -- Periodicals; Nanotechnology -- Therapeutic use -- Periodicals; 610.28
• DOI: 10.2217/nnm-2016-0437
• Languages: English
• ISSNs: 1743-5889

Abstract

Aim: Develop nanoparticulate agents for oral targeted delivery of dexamethasone (Dex) to macrophages of inflamed mucosa.Materials & methods: Solid archaeolipid nanoparticles (SAN-Dex) (compritol/ Halorubrum tebenquichense polar 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 vitro anti-inflammatory activity, were determined.Results: Ultra-small SAN-Dex strongly reduced the levels of TNF-α, IL-6 and IL-12 on J774A1 cells stimulated with lipopolysaccharides as compared with free Dex or loaded in ordinary solid lipid nanoparticles-Dex. After in vitro digestion, the anti-inflammatory activity of SAN-Dex was retained, while that of solid lipid nanoparticles-Dex was lost.Conclusion : Because of their structural and pharmacodynamic features, SAN-Dex may be suitable for oral targeted delivery to inflamed mucosa.