National Engineering Research Center for Biomaterials, Sichuan University, 29 Wangjiang Road, Chengdu, China.
Biomaterials. 2010 Sep;31(27):7124-31. doi: 10.1016/j.biomaterials.2010.06.011. Epub 2010 Jun 26.
Disassemblable micelles for intracellular delivery of doxorubicin were developed based on a reduction-degradable amphiphilic polyamide amine-g-polyethylene glycol graft copolymer containing disulfide linkages throughout the main chain. The micelles are spherical of less than 50 nm in diameter, and can load doxorubicin in the core with drug loading content up to 20%. The micelles are stable in normal physiological condition, and quickly disassemble in reductive condition due to the cleavage of the disulfide linkages. The drug release of the micelles in normal condition is less than 25% within 24 h, whereas in the presence of reductive agent, DTT, the micelles can quickly release the entire loaded drug within 10 h. CLSM observation showed that the micelles can effectively deliver the drug cargo into nuclei after internalized through endocytosis. Cytotoxicity of the drug-loaded disassemblable micelles was demonstrated using human cervical cancer cell line (HeLa) and human liver carcinoma cell line (HepG2).
基于一种含有贯穿主链的二硫键的还原降解两亲性聚酰胺-胺-聚乙二醇接枝共聚物，开发了用于阿霉素细胞内递送的可解体胶束。胶束为小于 50nm 的球形，可将阿霉素包载于内核中，载药率高达 20%。胶束在正常生理条件下稳定，由于二硫键的断裂，在还原条件下迅速解体。在正常条件下，24 小时内药物释放小于 25%，而在还原剂 DTT 的存在下，胶束可在 10 小时内迅速释放全部载药。CLSM 观察表明，胶束可通过内吞作用有效将药物递送至细胞核内。用人宫颈癌细胞系（HeLa）和人肝癌细胞系（HepG2）对载药可解体胶束的细胞毒性进行了研究。
