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酸敏释药胶束作为一种新型的靶向给药系统,具有增溶疏水性药物、载药量高,酸敏感释药等优势。可通过物理包埋或酸敏感键共价连接药物的方式包载药物。在肿瘤组织的偏酸环境下,物理包埋载药胶束由于共聚物亲脂嵌段质子化或亲水亲脂嵌段水解分离、共聚物失去两亲性,胶束解聚释药;而以共价连接方式包载的药物经酸敏键断裂释放。现主要从载药方式及释药机制方面探讨酸敏释药胶束作为肿瘤靶向给药系统的研究进展。
As a new targeted drug delivery system, acid sensitive drug releasing micelles have the advantages of solubilizing hydrophobic drugs, high drug loading, and acid sensitive drug delivery. Drugs may be encapsulated by physically entrapped or acid-sensitive bonds covalently attached to the drug. Under the acidic condition of the tumor tissue, the drug-loaded micelles lose amphiphilic and micellar depolymerization and release drugs due to the protonation of the lipophilic block or the hydrophilic-lipophilic block hydrolysis of the copolymer. Drugs entrapped by covalent attachment are released by acidic cleavage. Nowadays, the research progress of acid sensitive drug-releasing micelles as a tumor targeting drug delivery system is mainly discussed from the aspect of drug loading and drug release mechanism.