Functionalized nanoformulation based on enriched-triterpenes fraction target adipose tissue, as a potential treatment to obesity and type-2 diabetes: preliminary data

Previous studies have shown that the intraperitoneal administration of enriched triterpenes extracts (OBE100), obtained from Eucalyptus tereticornis, reduces metabolic alterations in a diet-induced obese (DIO) mouse model [1]. The present work aims to develop a phytotherapeutic prototype of triterpenes encapsulated in functionalized nanoparticles (FNP) to target abdominal adipose tissue in a DIO model. Encapsulating therapeutic principles in functional nanocarriers allows the site, dose, and release time control.

The PLGA-b-PEG-Maleimide polymer was conjugated with the peptide P3 (CKGGRAKDC) labelled with cyanine 7 (CY7). Peptide P3 binds to prohibitin, a marker of adipose tissue [2]. The PLGA-b-PEG, PLGA-b-PEG-Peptide and OBE 100 were used to form the FNP using the emulsion-solvent evaporation technique. The FNP was purified, and the particle size, Z-potential, encapsulation efficiency (EE) and loading capacity (LC) were determined. The size was checked by scanning electron microscopy (SEM), and the CY7 fluorochrome in the assembled particle was verified. The FNP was administered intravenously in the DIO mouse model, and its body distribution was evaluated ex vivo.

We developed a FPN with size of 278 nm, + 3,1 ZP, 0,16 PDI, 80% EE, 1 – 4% LC. SEM confirmed the size and showed a homogeneous distribution. The functionalization of the nanoparticles was verified by the Cy7 fluorescence marker anchored to the peptide. The affinity of the FNP to adipose tissue after 1.5H of intravenous administration of 80 mg OBE100/kg animal weight was demonstrated.

A formulation of FNP was developed based on a natural extract with potential antidiabetic activity to be selectively directed towards abdominal adipose tissue.

• References

• 1 Acín S, Muñoz DL, Alis Guillen A. et al. Triterpene-enriched fractions from Eucalyptus tereticornis ameliorate metabolic alterations in a mouse model of diet-induced obesity. J Ethnopharmacol 2021; 265: 113298
• 2 Kolonin MG, Saha PK, Chan L. et al. Reversal of obesity by targeted ablation of adipose tissue. Nat Med 2004; 10: 625-632

Publication History

Article published online:
12 December 2022