Improved oral nutraceutical-based intervention for the management of obesity: pterostilbene-loaded chitosan nanoparticles

Aim: To formulate and assess the oral anti-obesity effect of polymeric-based pterostilbene (PS)-loaded nanoparticles. Methods: Pterostilbene-hydroxypropyl beta-cyclodextrin inclusion complex loaded in chitosan nanoparticles (PS/HP beta CD-NPs) were prepared and characterized in vitro. Cytotoxicity, pharmacokinetics and anti-obesity effects were assessed on Caco-2 cell line and high-fat-diet-induced obesity rat model, respectively. in vivo assessment included histological examination, protein and gene expression of obesity biomarkers in adipose tissues. Results: Safe PS/HP beta CD-NPs were successfully prepared with improved bioavailability compared with free PS. PS/HP beta CD-NPs showed an improved anti-obesity effect, as supported by histological examination, lipid profile, UCP1 gene expression and protein expression of SIRT1, COX2, IL-6 and leptin. Conclusion: Orally administered PS nanoparticles represent a new and promising anti-obesity strategy owing to the sustainable weight loss and minimal side effects; this may be of great socio-economic impact. Plain language summary: Weight gain or obesity represents a major health risk and leads to diseases including cancer and heart disease. Most anti-obesity medications have significant side effects, and there are notable challenges concerning their availability in the body to produce an effect. Pterostilbene is a herbal drug with beneficial anti-obesity effects. However, it has problems such as poor solubility which restrict its use. The aim of the study was to formulate pterostilbene in a nano-based delivery system and fully characterize its anti-obesity effect when given orally. We evaluated the safety and anti-obesity effects of pterostilbene nanoparticles in cells and in obese rats fed on a high-fat diet. We also looked at how the body absorbs, distributes and gets rid of these nanoparticles. The prepared nanoparticles were nontoxic, with an improved anti-obesity effect; they decreased cholesterol levels and helped in changing white fat (which stores fat) to brown fat (which burns calories). We conclude that the developed pterostilbene nanoparticles, given orally, are a new and promising anti-obesity strategy given their long-lasting effect on weight loss and the minimal side effects. This may be of great economic and societal impact.

Automated summary

This study aimed to formulate and evaluate the oral anti-obesity effect of pterostilbene-loaded nanoparticles. The nanoparticles were successfully prepared and showed improved bioavailability and an enhanced anti-obesity effect compared to free pterostilbene. The nanoparticles decreased cholesterol levels and facilitated the conversion of white fat to brown fat, resulting in sustainable weight loss and minimal side effects. These findings suggest that orally administered pterostilbene nanoparticles could be a promising anti-obesity strategy with significant socio-economic impact.