Synthesis, Characterization of Liposomes Modified with Biosurfactant MEL-A Loading Betulinic Acid and Its Anticancer Effect in HepG2 Cell

• Main Authors: Qin Shu, Jianan Wu, Qihe Chen
• Format: Article
• Language: English
• Published: MDPI AG 2019-10-01
• Series: Molecules
• Subjects: liposomes; betulinic acid (ba); mannosylerythritol lipid-a (mel-a); hepg2; anticancer activity
• Online Access: https://www.mdpi.com/1420-3049/24/21/3939

As a novel natural compound delivery system, liposomes are capable of incorporating lipophilic bioactive compounds with enhanced compound solubility, stability and bioavailability, and have been successfully translated into real-time clinical applications. To construct the soy phosphatidylcholine (SPC)−cholesterol (Chol) liposome system, the optimal formulation was investigated as 3:1 of SPC to Chol, 10% mannosylerythritol lipid-A (MEL-A) and 1% betulinic acid. Results show that liposomes with or without betulinic acid or MEL-A are able to inhibit the proliferation of HepG2 cells with a dose-effect relation remarkably. In addition, the modification of MEL-A in liposomes can significantly promote cell apoptosis and strengthen the destruction of mitochondrial membrane potential in HepG2 cells. Liposomes containing MEL-A and betulinic acid have exhibited excellent anticancer activity, which provide factual basis for the development of MEL-A in the anti-cancer applications. These results provide a design thought to develop delivery liposome systems carrying betulinic acid with enhanced functional and pharmaceutical attributes.