Aiming at the problem of drugs into the brain Fudan provides a new idea for the design of liposome drugs

for Drug into the brain problem Fudan provides new ideas for liposome drug design

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Xinmin Evening News (correspondent re-news reporter Shi Jie) for the brain into the brain problem, Fudan University accounted for Changyou Group to make new progress in the study of liposome delivery mechanism, will be brain tumor and nerve regression Liposome drug design for sexual diseases offers new ideas.

This afternoon, Nature and Communication published the relevant research results online – “Reducing natural IgM adsorption can enhance the immunocompatibility of targeted liposomes”, and the Changyou group revealed stable peptides. The in vivo delivery of molecules to brain-targeted liposomes plays a “double-edged sword” regulatory mechanism, clarifying that surface-adsorption of native IgM can reverse-regulate the immunocompatibility of brain-targeted liposomes. In response to the problem of drugs entering the brain, it provides new ideas for the design of liposome drugs for the treatment of brain diseases such as brain tumors and neurodegenerative diseases.

It is reported that liposome drug surface modification targets polypeptide molecules, which can be delivered to target sites via receptor-mediated methods, in order to improve drug efficacy and reduce toxic side effects. However, after the targeted liposome enters the body, the protease contained in the blood or intracellular lysosome can rapidly degrade the liposome surface-modified polypeptide molecule, which seriously threatens its stability. Fudan University’s School of Basic Medicine, Zhan Changyou Group and School of Pharmacy Lu Weiyue’s research group used reverse-isomeric technology to design and obtain stable peptide molecules, which greatly improved enzyme stability and retained receptor binding activity, mediating lipids. Targeted delivery of body drugs.

 A new approach to liposome drug design for Fudan, a drug-inducing brain problem

Positively charged stable long peptide molecules play a “double-edged sword” role in the in vivo behavior of liposomes, that is, such molecules can improve stability to retain biological activity; but in the process of blood circulation, targeting liposomes A large amount of adsorption of natural IgM exacerbates the recognition of liposomes by the body’s immune system and accumulates in the liver and spleen, so that the blood circulation time of the liposome is suddenly reduced, and the body is cleared. To this end, the research team used computer-aided design and regulation of the molecular structure of the stable peptide, such as reducing the number of positive charges and shortening the length of the polypeptide, effectively reducing the amount of natural IgM adsorption on the surface of the liposome, successfully improving its immunocompatibility and reducing Targeting the immunogenicity of liposomes and prolonging blood circulation time. This study reveals a stable polypeptide-mediated targeting of liposome in vivo delivery regulation mechanisms, and also provides new ideas for the overall optimization of targeted liposomes.

Guan Juan, Ph.D., Fudan Basic Medical College, and Dr. Shen Qing, Shanghai Institute of Oncology, are the co-first authors of the paper. Researcher Zhan Changyou is the correspondent author, Professor Lu Weiyue, Associate Professor Qian Wei and Shanghai The First People’s Hospital Neurosurgery Building Mei Qing Chief Physician participated in the relevant research. The research was funded by the Youth Thousand Talents Program of the Central Organization Department, the National Natural Science Foundation of China, the Shanghai Municipal Science and Technology Commission and the Education Commission, and the State Key Laboratory of Polymer Molecular Engineering of Fudan University.