Anti-obesity effect of polymeric microparticles containing capsaicinoids

Capsaicinoids increase energy expenditure by about 50 kcal/day and can produce a clinically significant weight loss. However, the oral use of capsaicinoids is limited due to their pungency that can induce increased salivation, gastric secretion, and gastrointestinal disorders. In that sense, the aim of this work was to obtain and characterize capsaicinoids-loaded polycaprolactone (PCL) microparticles and to evaluate their anti-obesity potential using monosodium L-glutamate (MSG)-induced obese rats. PCL microparticles containing capsaicinoids were successfully prepared by simple emulsion/solvent evaporation. Micrometer-sized formulations with high drug-loading efficiencies were achieved. Considering the raw materials bands, no changes in FTIR assignments were recorded after the microencapsulation procedure. XRPD patterns and DSC analyses demonstrated that microencapsulation led to drug amorphization. PCL microparticles provided a remarkable decrease of dissolution rate of capsaicinoids without changing its biexponential release kinetic. In addition, capsaicinoids-loaded PCL microparticles played a positive role in decreasing Lee index, mesenteric and retroperitoneal fat deposits in obese rats. In summary, these formulations are feasible oral carriers for controlled release of capsaicinoids as an innovative strategy of low irritative effect for long-term use in obesity. This study was supported by Fundação Araucária (Brazil).