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目的观察生物可降解5-氟尿嘧啶聚乳酸纳米微粒(5-Fu-NPs)注射缓释剂用于肿瘤内局部给药的抗肿瘤活性。方法36只(SCID)小鼠随机分为6组,分别瘤内注射生理盐水的对照组、瘤内注射5-Fu-NPs(包括5-Fu 20 mg/kg体重和5-Fu 30 mg/kg体重)、无载药NPs、5-Fu注射液及腹腔注射5-Fu注射液,每3 d瘤内给药1次共3次。观察荷瘤鼠肿瘤生长、荷瘤鼠给药前、后血象及给药后肿瘤组织凋亡指数。结果瘤内注射5-Fu-NPs缓释剂组小鼠肿瘤生长缓慢,瘤体明显小于5-Fu(含5-Fu 20 mg/kg体重)腹腔注射给药组,相应的抑瘤率分别为2.93%、22.87%、27.57%、41.64%和50.43%,其中以瘤内注射5-Fu-NPs对小鼠胃癌有较高抑瘤率,呈现良好的量效关系,且对骨髓的副作用为最小。结论瘤内应用5-Fu-NPs缓释剂的抗肿瘤效果优于局部和全身单纯5-Fu给药。
Objective To observe the antitumor activity of biodegradable 5-fluorouracil-loaded polylactic acid nanoparticles (5-Fu-NPs) for sustained release in the tumor. Methods Thirty-six SCID mice were randomly divided into 6 groups. The mice in each group were injected intratumoral injection of 5-Fu-NPs (including 5-Fu 20 mg / kg body weight and 5-Fu 30 mg / kg Body weight), drug-free NPs, 5-Fu injection and intraperitoneal injection of 5-Fu injection, every 3 d intrathecal administration of a total of 3 times. The tumor growth of tumor-bearing mice was observed, the blood samples of tumor-bearing mice before and after administration and the apoptosis index of tumor tissues after administration. Results The tumor growth of the 5-Fu-NPs sustained-release group was slower than that of the 5-Fu-NPs sustained-release group. The tumor volume was significantly lower than that of the 5-Fu (containing 5-Fu 20 mg / kg body weight) intraperitoneal injection. 2.93%, 22.87%, 27.57%, 41.64% and 50.43% respectively. Among them, 5-Fu-NPs injected intratumorally had higher tumor inhibition rate, good dose-effect relationship and minimal side effects on bone marrow . Conclusion The antitumor effect of intratumoral 5-Fu-NPs sustained-release agent is superior to local and systemic administration of 5-Fu alone.