Two-block double-sensitive camptothecin polymer prodrug taking benzeneboronic ester as connecting unit and preparation method of two-block double-sensitive camptothecin polymer prodrug

• Main Authors: YU JIAHUI, HUANG YUSHU, XU YANYUN, YOU DONGLEI, WU YANQIAN
• Format: Patent
• Language: Chinese; English
• Published: 09.07.2019
• Subjects: CHEMISTRY; COMPOSITIONS BASED THEREON; HUMAN NECESSITIES; HYGIENE; MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONSONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC MACROMOLECULAR COMPOUNDS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; THEIR PREPARATION OR CHEMICAL WORKING-UP

The invention discloses a two-block double-sensitive camptothecin polymer prodrug taking benzeneboronic ester as a connecting unit and a preparation method of the two-block double-sensitive camptothecin polymer prodrug. The two-block double-sensitive camptothecin polymer prodrug takes benzeneboronic catechol ester (BC) as the connecting unit, polyethylene glycol-polyglutamate disulfide ethanol camptothecin two-block polymer (PEG-BC-PGlu-ss-CPT) is synthesized, thereby constructing a self-assembly prodrug nano micelle, namely PEG-BC@PGlu-ss-CPT; PEG-BC is taken as a macroinitiator an initiatorto perform an open-loop polymerization reaction on a reduction-sensitive camptothecin monomer to obtain the two-block double-sensitive camptothecin polymer prodrug PEG-BC-PGlu-ss-CPT taking the benzeneboronic ester as the connecting unit. The prepared prodrug micelle can improve the solubility of camptothecin and improve the stability of a camptothecin lactone ring so as to overcome the limitationof camptothecin clinical