Ultra-Small Solid Archaeolipid Nanoparticles for Active Targeting to Macrophages of the Inflamed Mucosa

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.

Keywords:

• digestion stability
• inflammatory bowel disease
• oral delivery

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184

Acknowledgements

The authors would like to thank MA de Farias and RV Portugal from the Electron Microscopy Laboratory, Brazilian Nanotechnology National Laboratory, for sample preparation and data acquisition of Cryo-TEM images.

Financial & competing interests disclosure

This work was supported by Secretaria de Investigaciones, Universidad Nacional de Quilmes. HE Jerez has a fellowship from National Council for Scientific and Technological Research (CONICET). HL Higa, EL Romero and MJ Morilla are members of the Research Career Program from CONICET. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.