Planta Med 2022; 88(15): 1574-1575
DOI: 10.1055/s-0042-1759357
Poster Session II

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

E Escobar
Universidad De Antioquia, Medellin, Colombia
,
M Fernandez
Universidad De Antioquia, Medellin, Colombia
,
L F Echeverri
Universidad De Antioquia, Medellin, Colombia
,
S Acin
Universidad De Antioquia, Medellin, Colombia
,
D L Muñoz
Universidad De Antioquia, Medellin, Colombia
,
J Orozco
Universidad De Antioquia, Medellin, Colombia
,
N Balcazar∗
Universidad De Antioquia, Medellin, Colombia
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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.



Publication History

Article published online:
12 December 2022

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  • References

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