吉西他滨-纳米活性碳混悬液在大鼠体内淋巴靶向性的研究

Study on the ability to delivery gencitabine to lymph nodes of Sprague-Dawley rat after injection of carbon activated absorbing gencitabine

目的:比较自制吉西他滨-纳米活性碳混悬液(GCB-CH)及吉西他滨水溶液(GCB)在大鼠体内的淋巴靶向性。方法:将72只SD大鼠随机分为两组,分别于右后脚掌皮下注射含6 mg吉西他滨的纳米活性碳混悬液和水溶液,于注射后1,2,4,7,10,14 h分别每组各处死6只大鼠,取其腹股沟淋巴及血浆测其浓度,比较试验组与对照组对淋巴的靶向指数(TI)、选择性指数(SI)及相对摄取率(RE)。结果:吉西他滨-纳米活性碳混悬液在淋巴中的浓度明显高于水溶液在淋巴里的浓度,在6个时间点的靶向指数及选择陛指数均大于1,淋巴组织对混悬液的相对摄取率是水溶液的6.87倍。结论:以21 nm活性碳为载体的吉西他滨有良好淋巴趋附性;21 nm活性碳是淋巴化疗的理想的药物载体。

OBJECTIVE To compare the difference of the ability to deliver the carbon activated absorbing gencitabine（GCB- CH） and gencitabine to lymph nodes of Sprague-Dawley rats. METHODS 72 Sprague-Dawley rats were divided into 2 groups randomLy with 36 in each group. CJCB-CH which contained 6 mg gencitabine and gencitabine（6 mg） were respectively injected into ratg right sole vein. At 1,2,4,7,10,14 h after drug administration, 6 rats in both groups were sacrificed and gencitabine concentration in the plasma and inguinal lymph node were determined by HPLC. Targeting ability was evaluated by targeting index（TI）, selectivity index（SI） and relative extraction efficiency（RE） were compared. RESULTS Values of TI and SI were more than 1 at 6 time points. The area under GCB concentration-time curve of inguinal lymph node in GCB-CH group was 6. 87 times as many as that in GCB group. CONCLUSION GCB-CH can specifically deliver gencitabine to lymph nodes 21 nm active carbon was a good medicine carrier to be used in lymphatic chemotherapy.