Aim: To formulate and assess the oral anti-
obesity effect of polymeric-based
pterostilbene (PS)-loaded nanoparticles. Methods:
Pterostilbene-hydroxypropyl β-
cyclodextrin inclusion complex loaded in
chitosan nanoparticles (PS/HPβCD-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/HPβCD-NPs were successfully prepared with improved bioavailability compared with free PS. PS/HPβCD-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.