CAJ | 학술논문

目的：构建一种新型的磁靶向定位灌注化疗膀胱癌的吡柔比星纳米制剂，并探讨其磁靶向定位及抗膀胱癌细胞特性，为定位灌注化疗膀胱癌的临床应用提供帮助。方法通过N－N′－羰基二咪唑（CDI）交联剂将治疗膀胱癌的临床药物吡柔比星（ pirarubicin，THP）连接在表面氨基化的四氧化三铁（ Fe3 O4）磁性纳米粒上，制备具有磁性的THP纳米制剂，并在体外考察其磁定位性能和对膀胱癌细胞的抑制作用。结果THP成功地连接到了粒径40 nm左右的Fe3 O4磁性纳米粒上，磁性药物制剂在不同pH值的缓冲液中药物在90％以上，并可在外界磁场作用下定位于靶向部位。对膀胱癌细胞可造成THP和Fe3 O4双重抑制效果，抑制率高达58．44％。结论该纳米制剂可通过外界磁场定位于靶向部位，膀胱癌细胞抑制效果明显，为临床定位灌注化疗的应用奠定了基础。
목적：구건일충신형적자파향정위관주화료방광암적필유비성납미제제，병탐토기자파향정위급항방광암세포특성，위정위관주화료방광암적림상응용제공방조。방법통과N－N′－탄기이미서（CDI）교련제장치료방광암적림상약물필유비성（ pirarubicin，THP）련접재표면안기화적사양화삼철（ Fe3 O4）자성납미립상，제비구유자성적THP납미제제，병재체외고찰기자정위성능화대방광암세포적억제작용。결과THP성공지련접도료립경40 nm좌우적Fe3 O4자성납미립상，자성약물제제재불동pH치적완충액중약물재90％이상，병가재외계자장작용하정위우파향부위。대방광암세포가조성THP화Fe3 O4쌍중억제효과，억제솔고체58．44％。결론해납미제제가통과외계자장정위우파향부위，방광암세포억제효과명현，위림상정위관주화료적응용전정료기출。
Objective We synthesized novel magnetic pirarubicin nanoparticles for targeted intravesical chemotherapy to treat bladder cancer .Methods Pirarubicin was grafted on Fe 3 O4 nanoparticles which were surface-functionalized with amino-groups via N, N′-Carbonyldiimidazoleas targeted intravesical infusion chemotherapy agents.Mimetic position in vitro by external magnetic field and inhibition to bladder cancer cells of prepared agents were demonstrated.Results Pirarubicin was successfully grafted on magnetic Fe3 O4 nanoparticles whose size were around 40 nm.The residual of pirarubicin on the pharmaceutic agents was above 90% in buffer solutions of various pH.They also could be positioned to certain area by external magnetic. Meanwhile, the prepared magnetic pirarubicin nanoparticles gave multiple-inhibition to bladder cancer cells by THP and Fe3 O4.The inhibition rate was up to 58.44% after co-cultured for 2 h.Conclusions These magnetic pirarubicin nanoparticles have a great potential for clinical use in infusion chemotherapy.