摘要
目的:考察N-三甲基壳聚糖(TMC)包衣的多柔比星(ADM)阳离子脂质体抗肿瘤活性及对肿瘤新生血管的靶向性。方法:采用动物移植性肿瘤实验法,建立小鼠H_(22)肿瘤模型,比较TMC包衣脂质体组和其他各给药组的肿瘤抑制率并通过小鼠尾静脉注射异硫氰酸荧光素标记的葡聚糖(FITC-Dextran),分析肿瘤组织中的在体荧光,定性观察肿瘤新生血管的形态排布情况,定量测定肿瘤组织中的血管相对密度。结果:TMC包衣的ADM脂质体组,其小鼠的瘤重抑制率达53.47%,显著高于游离药物组和未包衣脂质体组(8.75%,34.88%)(P<0.05);给予TMC包衣ADM脂质体的小鼠,其肿瘤新生血管形态良好,排布均匀,血管分支少,而其他给药组的肿瘤新生血管多扭曲,粗细不均,一个节点有多个血管分支等;通过比较不同给药组肿瘤组织黏附的FITC-Dextran量,TMC包衣ADM脂质体组的肿瘤血管密度明显低于游离药物组和未包衣脂质体组(P<0.05)。结论:TMC包衣的ADM阳离子脂质体不仅具有较强的抗肿瘤活性,而且具有很好的肿瘤新生血管靶向性。
To study the anti-tumor activity and the tumor angiogenesis targeting of adriamycin （ADM） cationic lipo- somes coated by N-trimethyl chitosan （TMC）. Method： The mice H22 tumor model was established by animal transplanted tumor experiment. In addition to compare the tumor inhibition rate of liposomes coated by TMC with that of the other experimental groups, the fluorescence in tumor tissue was also investigated through the tail vein injection of fluorescein isothiocyanate conjugated dextran （ FITC- Dextran）. The shape and arrangement conditions of tumor angiogenesis were observed qualitatively and relative density of tumor angio- genesis was also determined quantitatively. Result： The tumor weight inhibition rate of the mice given TMC-coated ADM liposomes was 53.47% ,which was significantly higher than that of free drug group and the uncoated liposomes group （8.75% and 34. 88% ,respec- tively） （P 〈 0. 05 ）. In the mice given TMC-coated ADM liposomes, the tumor angiogenesis had good shape, uniform arrangement and small vascular branches,while the tumor angiogenesis of the other treatment groups showed more distorted shape, uneven thickness and a node with multiple vascular branches. The vascular density of liposomes coated by TMC was significantly lower than that of the free drug group and uncoated liposomes （ P 〈 0. 05 ）. Conclusion ： ADM liposomes coated by TMC not only have strong anti-tumor activity, but also have good tumor angiogenesis targeting ability.
出处
《中国药师》
CAS
2011年第7期911-914,共4页
China Pharmacist
