Novel Ginsenoside Rg3-based and Paclitaxel-coloaded liposomes for glioma target therapy
作者单位：Department of Pharmaceutics School of Pharmacy Fudan University ＆ Key Laboratory of Smart Drug Delivery Ministry of Education
会议名称：《2018年第十二届中国药物制剂大会》
会议日期：2018年
学科分类：100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学]
关 键 词：ginsenoside Rg3 liposome brain Tumor targeting paclitaxel TAM TME
摘 要：Accumulation of most currently used anti-tumor agents in malignant glioma is far from perfect because of their non-targeted nature and difficulty in crossing the blood-brain barrier/blood-tumor barrier（BBB/BBTB）. Attempts to overcome this challenge have been focused on nanoparticle drug delivery system, such as nanoparticles, liposomes and other self-assembling systems. And various ligands are usually modified on the surface of these nanocarriers to construct brain-targeted delivery systems that can overcome BBB/BBTB barriers, target to tumor cells. However, most target ligands are polypeptides, whose preparation costs are high and process is complicated, and they often ignore the complicated brain tumor mircroenvironment（TME）, which contains many different noncancerous cell types in addition to cancer cells, also might limite the success of glioma treatment. Therefore, it is imperative to develop new nano preparations that can not only across BBB/BBTB but also regulate the TME to improve drug delivery efficiency and glioma treatment. In our previous studies, we have successfully developed a novel ginsenoside Rh2-based liposomes. It is a novel liposome prepared by replacing ginsenoside Rh2 with *** can not only break the clinical limitations of traditional liposomes due to the various defects of cholesterol but also mediate endocytosis through glucose receptors to the uptake of tumor cells. GLUT-1 can mediate the delivery across the BBB for those substances with similar structures of glucose, including mannose and glucose analogs. Ginsenoside Rg3 resembles with Rh2 in structure, and it contains 2 glucose molecules, which may account for helping the liposome cross the BBB/BBTB. Moreover, ginsenoside Rg3 has good anti-tumor activity. Besides when it combinate with other chemotherapeutic agents may lead to an improved treatment efficacy by synergistic effects. Furthermore, ginsenoside Rg3 also plays a role in the improvement of host immunity in tumor-bearing