Polymeric nanoformulation prototype based on a natural extract for the potential treatment of type 2 diabetes mellitus

Triterpene-enriched fractions (TFs) from Eucalyptus tereticornis demonstrated efficiency when administered intraperitoneally in diet-induced obesity (DIO) mouse model to treat obesity-related type 2 diabetes mellitus (T2DM); however, its oral administration has not yet led to satisfactory results. In this context, we developed a polymeric nanoformulation to transport TFs orally in DIO mice and control obesity and T2DM effects. We encapsulated TFs in a polylactic-co-glycolic acid-based nanocarrier, physicochemically characterized the nano -carriers, and evaluated TFs in-vitro release kinetics, in-vivo metabolic biomarkers, and released triterpenes in a simulated in-vitro human gastrointestinal model. The nanoformulation showed a TFs release of 80% in the first 6h in-vitro, and the in-vivo assay demonstrated a decrease in mice weight, glycaemia, glucose, and insulin intoler-ance. Finally, triterpenes released up to 75% in the simulated in-vitro human intestine. These results open the way for developing new strategies of therapeutic agents with natural products to control obesity and T2DM.

Automated summary

Triterpene-enriched fractions (TFs) from Eucalyptus tereticornis effectively treated obesity-related type 2 diabetes mellitus (T2DM) in mice through intraperitoneal administration, but not orally. To address this, a polymer-based nanoformulation was developed to orally transport TFs in mice and control obesity and T2DM. The nanoformulation exhibited high release of TFs in vitro, leading to weight loss and improved glucose and insulin intolerance in vivo. This study suggests new strategies for using natural products to treat obesity and T2DM.