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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。
Objective: To investigate the antitumor activity of ADM liposomes coated with N-trimethyl chitosan (TMC) and its targeting to tumor neovascularization. Methods: Animal H22 tumor model was established. Tumor inhibition rate of TMC-coated liposome group and other groups were compared and the isothiocyanate fluorescence (FITC-Dextran) was used to analyze in vivo fluorescence in tumor tissue. The morphology of tumor neovascularization was qualitatively observed and the relative density of blood vessels in tumor tissue was quantitatively determined. Results: The tumor weight inhibition rate of TMC-coated ADM liposome group was 53.47%, significantly higher than that of the free drug group and the uncoated liposome group (8.75%, 34.88%) (P <0.05) ; Mice given TMC-coated ADM liposomes showed good morphology, uniform arrangement and fewer blood vessel branches, whereas the tumors in other administration groups were distorted and uneven in thickness, with multiple blood vessels at one node Branches, etc. The tumor vascular density in TMC-coated ADM liposomes group was significantly lower than that in free drug group and uncoated liposome group by comparing the amount of FITC-Dextran adhered to tumor tissues in different administration groups (P <0.05). CONCLUSION: TMC-coated ADM cationic liposomes not only have strong anti-tumor activity, but also have good neovascularization targeting.