非内吞依赖型生物大分子药物胞质递送策略研究进展  

Advances in Cytoplasmic Delivery Strategies for Non-Endocytosis-Dependent Biomolecules

作　　者：袁静静 郑宇钊 徐晨枫 殷婷婕 YUAN Jingjing;ZHENG Yuzhao;XU Chenfeng;YIN Tingjie(School of Pharmacy,China Pharmaceutical University,Nanjing Jiangsu 210000,China;Department of Pharmacy,Union Hospital,Tongji Medical College,Huazhong University of Science and Technology,Wuhan Hubei 430022,China)

机构地区：[1]中国药科大学药学院,江苏南京210000 [2]华中科技大学同济医学院附属协和医院药学部,湖北武汉430022

出　　处：《广西师范大学学报（自然科学版）》2024年第1期1-8,共8页Journal of Guangxi Normal University:Natural Science Edition

基　　金：国家自然科学基金(81972835);国家自然科学青年科学基金(82003693)。

摘　　要：生物大分子药物由于具有高效、高特异性等优点,已成为新一代治疗药物的重要组成部分,但其分子稳定性差、易被酶解、难以跨越生物膜。传统的生物大分子药物纳米递送策略的有效性主要受限于溶酶体逃逸效率低,针对性开发非内吞依赖型的胞质直接递送策略具有重要意义。本文综述细胞穿透肽、低pH插入肽、清道夫受体介导的非内吞作用、膜融合、内质网途径、硫醇介导、基于液-液相分离技术的非内体捕获型生物大分子药物胞内递送策略的效应机制和研究进展,并分析了技术转化难点。Biomacromolecular drugs have become an important component of the new generation of therapeutic drugs due to their high efficiency and specificity.However,their molecular stability are poor,and they are prone to enzymatic hydrolysis,and are difficult to cross biofilms.The effectiveness of traditional nano delivery strategies for biomacromolecule drugs is mainly limited by the low escape efficiency of lysosome.It is of great significance to develop endocytosis independent direct cytoplasmic delivery strategies.This paper reviews the effect mechanism and research progress of cell penetrating peptide,low pH insertion peptide,scavenger receptor mediated non endocytosis,membrane fusion,endoplasmic reticulum pathway,mercaptan mediated,non endosome capture based intracellular delivery strategy of biomacromolecule drugs based on liquid-liquid phase separation technology,and analyzes the difficulties in technology transformation.

关 键 词：生物大分子药物 细胞穿透肽 巯醇 入胞 内质网途径 膜融合 

分 类 号：R943[医药卫生—药剂学]