【摘要】 目的:观察注射用纳米羟喜树碱(HCPT纳 米针剂)静脉推注后小鼠体内组织分布情况,并与 注射用羟喜树碱(HCPT针剂)比较组织分布特征。 方法:BALB/c小鼠分别给予HCPT纳米针剂或 HCPT针剂,10mg·kg-1尾静脉推注给药。给药后 15min,1和2h,采用HPLC方法检测小鼠各组织和 血浆中羟喜树碱的含量,并对不同剂型和不同取样 时间进行比较。结果:(1)HCPT纳米针剂在肝组 织中浓度最高,分布顺序:肝>肾>脾>肠>胃> 肺>心。(2)HCPT纳米针剂在肝、肾、脾、肺、胃的 药物浓度均显著高于HCPT针剂(P<0.05),肝组 织药物浓度最高,是HCPT针剂组的37.66倍 (15min)。(3)HCPT纳米针剂给药后在肝组织保 留时间长,而HCPT针剂组给药后没有显著蓄积的 靶组织。结论:HCPT纳米针剂与HCPT针剂相比, 能够更多地进入组织器官并具有明显的肝组织靶向 性,在肝组织中可较长时间保持较高药物浓度。更多还原

【Abstract】 AIM: To investigate the tissue distribution performance of 10-hydroxycamptothecin(HCPT) nanoparticle injection in mice and those of HCPT nanoparticle injection’s peculiar tissue distribu-tion transformation in mice by comparing with control substance——HCPT common injection. METHODS: HCPT(nanoparticle or lyophilized injection) was administered to BALB/c mice by bolus injection at dose of 10 mg·kg -1 body weight. Drug levels in various tissues were detected by HPLC and UV detector at 15, 60 and 120 min after injection. Characteristics of tissue distribution were contrasted between different dosages and sample forms. RESULTS: (1) The highest concentration of HCPT nanoparticle injection was obtained in liver. And the sequence of HCPT levels in various tissues was: liver>kidney>spleen>stomach>lung>heart.(2) Concentration of nanoparticle injection were higher than lyophilized form in several kinds tissues (e.g. liver, spleen, lung, kidney, stomach). Especially in liver, HCPT nanoparticle injection reached 37.66 times of the common form. (3) HCPT nanoparticle injection prolonged obviously accumulated in liver, while no conspicuous visible accumulated organs in common form group. CONCLUSION: Comparing with common forms, HCPT nanoparticle injection could distribute into organs more extensively and reflect great liver targeting capability.更多还原