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Updated: Oct 25, 2026

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Self-assembled nanoparticles of oleanolic acid as a potential functional food ingredient with improved dispersibility
Quanrun He1, Zhiyuan Zhen1, Yong Zhu1
1Shenzhen Key Laboratory of Steroid Drug Discovery and Development, Department of Pharmaceutical Science, Division of Biomedical Health Sciences, School of Medicine, The Chinese University of Hong Kong, Shenzhen, China.
Abstract:
Oleanolic acid (OA) is a plant-derived pentacyclic triterpenoid with anti-obesity and anti-inflammatory activities, but its poor solubility limits bioavailability. In this study, self-assembled OA nanoparticles (OA-NM) were prepared via an anti-solvent method to enhance dispersibility and efficacy. OA-NM exhibited uniform spherical morphology (∼228 nm), good stability, and supramolecular reorganization driven mainly by hydrophobic interactions and hydrogen bonding. Its cellular uptake occurred primarily via clathrin-mediated endocytosis. Compared with free OA, OA-NM showed lower cytotoxicity and enhanced bioactivity. In 3T3-L1 adipocytes, OA-NM reduced lipid accumulation, suppressed adipogenic gene expression, improved mitochondrial function, and restored insulin signaling. In LPS-stimulated RAW264.7 macrophages, OA-NM inhibited M1 polarization, promoted M2 transition, and suppressed NF-κB-mediated inflammation. Overall, self-assembly significantly improves the functional performance of OA, highlighting OA-NM as a promising strategy to enhance the utilization of hydrophobic dietary bioactives for metabolic health applications.
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