REVERSIBLY CROSS-LINKED BIODEGRADABLE POLYMER VESICLE WITH POSITIVELY CHARGED INTERNAL MEMBRANE AND PREPARATION METHOD AND USE FOR PREPARING ANTI-TUMOR DRUG THEREOF
A reversibly cross-linked biodegradable polymer vesicle with a positively charged internal membrane, and a preparation method and application for preparing an anti-tumor drug thereof. A tumor-targeting, reduction-sensitive reversibly cross-linked, and intracellularly decrosslinkable biodegradable polymer vesicle with the positively charged internal membrane is based on a block polymer PEG-P(TMC-DTC)-SP or PEG-P(LA-DTC)-SP. The vesicle provides high performance loading and protection of a biomacromolecule, including a protein, DNA and siRNA, and a physiologically negatively charged small molecule drug. The vesicle can also deliver the biomacromolecule and the physiologically negatively charged small molecule drug into a tumor cell in vivo to induce apoptosis of the tumor cell. The system offers unique advantages, including easy handling during preparation, outstanding biocompatibility, excellent controlled-release for a drug, superb in vivo circulation stability, cancer cell targeting, significant induction of cancer cell apoptosis and the like. As such, the invention has great potential to become a nanosystem platform combining the advantages of simplicity, stability, and multiple functionality for use in high-efficiency, active targeting and delivery of a nucleic acid to a carcinoma in situ.Linvention concerne une vésicule de polymère biodégradable réticulée de manière réversible et à membrane interne chargée positivement, un procédé de préparation de cette dernière, et une application de cette dernière pour préparer un médicament antitumoral. La vésicule de polymère biodégradable capable de cibler des tumeurs, sensible à la réduction et réticulée de manière réversible et perdant sa réticulation en milieu intracellulaire, dont la membrane interne est chargée positivement, est basée sur un bloc polymère de type PEG-P(TMC-DTC)-SP ou PEG-P(LA-DTC)-SP. La vésicule permet une performance élevée de chargement et de protection dune macromolécule biologique, qui peut être
