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

Qin Shu,Qihe Chen,Jianan Wu

doi:10.3390/molecules24213939

Abstract

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.

Highlights

Great attention was paid to the study of pharmacokinetics and the development of biopharmaceutics in the second half of the last century, when enormous progress was obtained in the field of pharmaceutical industry [1]
This study has successfully constructed soy phosphatidylcholine-cholesterol liposomes modified by mannosylerythritol lipid-A (MEL-A) and loading betulinic acid, and obtained the optimal liposome formulation with 3:1 of SPC
MEL-A modified liposome can strengthen the destruction of mitochondrial membrane potential in HepG2 cells by betulinic acid (BA)

Summary

Introduction

Great attention was paid to the study of pharmacokinetics and the development of biopharmaceutics in the second half of the last century, when enormous progress was obtained in the field of pharmaceutical industry [1]. Liposomes, described as spherical lipid vesicles with phospholipid bilayer structure [2], were one of the first nano-sized drug delivery systems, which has been successfully produced and applied into clinical fields. After discovered in 1961 by Alec Bangham et al [3], lots of researchers have declared great applications of liposomes in diverse fields, such as delivery of drugs, biomolecules and genes [4]. As for drugs with different solubility, there are different ways to be encapsulated in liposomes: hydrophobic compounds are embedded in the phospholipid bilayer, and hydrophilic compounds are entrapped in the aqueous cavity

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