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论文摘要

平阳霉素-活性炭纳米微粒行口腔癌淋巴化疗的靶向性评价

Lymphatic targeting study of pingyangmycin-activated carbon nanoparticles treating oral cancer lymph node metastasis

作者:孙明磊 谢卫红 王昌美 温玉明

Author:SUN Ming-lei1, XIE Wei-hong1, WANG Chang-mei2, WEN Yu-ming2

收稿日期:2011-06-25          年卷(期)页码:2011,29(03):253-253-256

期刊名称:华西口腔医学杂志

Journal Name:West China Journal of Stomatology

关键字:活性炭,纳米微粒,平阳霉素,淋巴结转移,靶向治疗,

Key words:activated carbon,nanoparticle,pingyangmycin,lymph node metastasis,targeted therapy,

基金项目:

卫生部科学研究基金资助项目(98-1-221)

中文摘要

目的观察平阳霉素-活性炭纳米微粒(PYM-CH-NP)经鼠癌周黏膜下给药后,活性药物在体内各组织器官中的分布情况,探讨PYM-CH-NP对淋巴结转移灶的靶向性。方法采用改良氯胺T法将125I标记平阳霉素(PYM),应用淋巴结高转移癌株U14建立昆明小鼠颈淋巴结转移模型。将360只颈淋巴结转移模型小鼠随机分为PYM-CH-NP组、PYM组和阴性对照组,分别于癌周黏膜下注射PYM-CH-NP、PYM水溶液和空白活性炭纳米微粒,给药后0.5、1、4、8、12、24、48、72、96、120、144、168 h处死动物,取血、心、肝、脾、肺、肾和颈淋巴结,检测各时间点各组织器官内平阳霉素的放射活性,计算各样本单位重量的药物放射活性(比放射活性),并计算药物的选择性指数(SI)和靶向指数(TI)。结果PYM-CH-NP组各时间点颈淋巴结内药物浓度显著高于PYM组(P<0.001),4 h后血、心、肝、脾、肺、肾等器官中药物浓度均低于PYM组(P<0.001)。PYM组各时间点的SI均小于1,而PYM-CH-NP组SI和TI最低值为1.793和1.562,最高为72 h时的68.126和14.623。结论PYM-CH-NP可显著增加淋巴结转移灶内的药物浓度,同时非靶器官药物分布减少,降低了药物的全身毒副反应。

英文摘要

Objective To investigate the drug distribution in tissues of cervical lymph node metastasis mice model after submucosa adjacent cancer injection of pingyangmycin-activated carbon nanoparticles(PYM-CH-NP) and evaluate the lymph targeting effect of PYM-CH-NP. Methods Pingyangmycin(PYM) was radiolabeled with 125I by modified the chloramine T method. Cervical lymph node metastasis mice model was established by buccal submucosa inoculation of a high lymph metastasis cell line U14 cancer cell. 360 mice models burdened with cervical lymph metastasis were randomly divided into 3 groups. PYM group was treated with PYM water solution, PYM-CH-NP group was treated with PYM-CH-NP. Negative control group was injected with activated carbon nanoparticles. PYM-CH-NP and pingyangmycin water solution were injected in pericancer submucosa of the mice respectively. The radioactivity of drug in blood, heart, liver, spleen, lung, kidney and cervical lymph node were measured after 0.5, 1, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 h administration. The radioactivity of each samples per unit weight were calculated. The selectivity index(SI)and targeting index(TI) of drug were calculated. Results The radioactivity of drug in cervical lymph node of PYMCH- NP group was much higher than PYM group in each time point(P

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