摘要
目的制备淋巴靶向平阳霉素纳米活性炭（PYM—ACH—NP），观察经荷瘤鼠癌周黏膜下注射PYM-ACH—NP后，活性药物平阳霉素在体内各组织器官的药物分布特点，探讨PYM—ACH—NP对淋巴结转移灶的靶向性。方法制备活性炭纳米微粒（ACH—NP），观察ACH—NP对平阳霉素（PYM）吸附效率。采用改良氯胺T法将放射性核素^125I-NaI标记PYM，应用淋巴结高转移癌株U14建立昆明小鼠颈淋巴结转移动物模型，随机分为PYM组和PYM—ACH—NP组，于癌周黏膜下按10mg／kg的剂量分别注射PYM水溶液和PYM—ACH—NP，给药72h后处死小鼠，取血、心、肝、脾、肺、肾和颈淋巴结，检测各组织器官内的PYM的比放射活性，以考察药物在体内的组织分布情况，对所得数据行t检验。结果PYM—ACH—NP平均粒径为178nm，随ACH—NP投入比例的增高，对PYM的吸附率相应增高，10：1质量比下吸附率达99．38％。癌周黏膜下注射给药后，PYM—ACH—NP组颈淋巴结转移灶内药物比放射活性为（148．72±29．35）cpm／mg远高于PYM组（10．17±2．11）cpm／mg（P〈0．01）；PYM—ACH—NP组血、心、肝、脾、肺、肾等器官中的药物比放射活性分别为（2．18±0．39）、（1．19±0．21）、（2．41±0．50）、（1．09±0．24）、（1．95±0．47）、（2．21±0．44）cpm／mg，显著低于PYM组相应各组织中的值（17．22±3．04）、（2．48±0．47）、（6．94±1．38）、（4．12±0．79）、（8．25±2．04）、（18．83±3．89）cpm／mg，差异有统计学意义（P〈0．01）。结论ACH—NP对PYM的吸附率高，PYM-ACH—NP具有良好的淋巴靶向性，经癌周黏膜下给药后，可显著提高淋巴结内的药物浓度，同时减少全身重要脏器的药物分布，降低了药物的全身不良反应。
Objective To explore the possibility of anticancer drug targeting to lymph metastasis using activated charcoal nanoparticles as a drug delivery carrier, the drug distribution in tissues of cervical lymph node metastasis mice model after submucosa adjacent cancer injection of pingyangmycin （ PYM ） absorbed in activated charcoal nano-particles （ACH-NP） and the lymph targeting effect of PYM-ACH-NP. Methods PYM-ACH-NP was prepared by mixed the ACH-NP ± PYM ± saline and shaken for 20 min. The absorbency of PYM on ACH-NP was evaluated. Cervical lymph node metastasis mice model was established by buecal submucosa implantation of a high lymph metastasis cell line U14 cancer cells （5 x 109/L）. PYM was radiolabeled with lzsI by the modified chloramine T method. Thirty Kunming mice models burdened with cervical lymph metastasis were randomly divided into control group, PYM-treated group and PYM- ACH-NP-treated group. The animal in each group was injected with 0. 2 mL saline or corresponding drugs （equal to l0 mg/kg PYM） respectively. The radioactivity of PYM in blood, heart, liver, spleen, lung, kidney and cervical lymph node was detected 72 h after administration. Specific radioactivity of each sam- ple was calculated. Results The average diameter of PYM-ACH-NP was 176 nm. The absorbency of PYM on ACH-NP was increased with the increased ratio of ACH-NP to PYM. In PYM-CH-NP group, specific radioactivity of PYM was significantly higher in cervical lymph node （ 148.72 ± 29. 35 ） cpm/mg than in PYM group （ 10. 17 ± 2. 11 ） cpm/mg （ P 〈 0. 01 ） , meanwhile the specific radioactivity of drug in the blood, heart, liver, spleen, lung and kidney of PYM-CH-NP group was （2. 18 ±0. 39）, （1.19 ±0. 21）, （2. 41 ± 0. 50 ）, （ 1.09 ± 0. 24 ）, （ 1.95 ± 0. 47 ） and （ 2. 21 ± 0. 44 ） cpm/mg respectively, which was significantly lower than in PYM group （17.22 ±3.04）, （2.48 ±0.47）, （6.94 ± 1.38）, （4.12 ±0.79）, （8.25 ± 2.04）, （18.83 ± 3.89） cpm/mg. The u
出处
《中华实验外科杂志》
CAS
CSCD
北大核心
2011年第6期990-992,共3页
Chinese Journal of Experimental Surgery
关键词
纳米微粒
活性炭
平阳霉素
淋巴结转移
Nanoparticle
Activated carbon
Pingyangmyein
Lymph metastasis
