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

• Published in: Nanomedicine (London, England) Vol. 17; no. 15; pp. 1055 - 1075
• Main Authors: Heikal, Lamia A, El-Kamel, Amal H, Mehanna, Radwa A, Khalifa, Hoda M, Hassaan, Passainte S
• Format: Journal Article
• Language: English
• Published: Future Medicine Ltd 01.06.2022
• Subjects: chitosan nanoparticles; hydroxypropyl β-cyclodextrin; pharmacokinetics; pterostilbene
• ISSN: 1743-5889; 1748-6963
• DOI: 10.2217/nnm-2022-0158

To formulate and assess the oral anti-obesity effect of polymeric-based pterostilbene (PS)-loaded nanoparticles. Pterostilbene–hydroxypropyl β-cyclodextrin inclusion complex loaded in chitosan nanoparticles (PS/HPβCD-NPs) were prepared and characterized . Cytotoxicity, pharmacokinetics and anti-obesity effects were assessed on Caco-2 cell line and high-fat-diet-induced obesity rat model, respectively. assessment included histological examination, protein and gene expression of obesity biomarkers in adipose tissues. 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, gene expression and protein expression of SIRT1, COX2, IL-6 and leptin. 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. 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.