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目的以脐静脉内皮细胞(HUVECs)为模型,考察其对N-三甲基壳聚糖(TMC)包衣的盐酸多柔比星脂质体的摄取情况,以评价TMC包衣盐酸多柔比星脂质体的体外血管内皮细胞靶向性。方法采用pH梯度法制备盐酸多柔比星脂质体,以不同取代度的TMC进行包衣,用DAPI定位细胞核,采用激光扫描共聚焦荧光显微镜观察不同TMC包衣盐酸多柔比星脂质体在HUVECs胞浆及胞核的转运及摄取情况。结果盐酸多柔比星脂质体性质稳定,包封率均在80%以上,粒径在100~200nm,随着TMC季铵化程度的增大,TMC包衣盐酸多柔比星脂质体的Zeta电位显著增大(P<0.05),同时HUVECs对其摄取能力增强,多柔比星能较快释放到胞浆并转运至胞核。结论TMC包衣盐酸多柔比星脂质体具有较强的体外内皮细胞靶向作用,且与TMC的季铵化程度有关,为进一步研究其体内靶向作用奠定了基础。
OBJECTIVE: To determine the uptake of doxorubicin hydrochloride liposomes coated with N-trimethyl chitosan (TMC) by using human umbilical vein endothelial cells (HUVECs) as a model to evaluate the effect of TMC-coated doxorubicin Vascular endothelial cell targeting of liposomes in vitro. Methods The pH gradient method was used to prepare doxorubicin hydrochloride liposomes and coated with TMC with different degrees of substitution. The nuclei were located by DAPI. Laser scanning confocal microscopy was used to observe the effects of different TMC-coated doxorubicin hydrochloride liposomes HUVECs in the cytoplasm and nucleus transport and uptake. Results Doxorubicin hydrochloride liposomes were stable in nature with entrapment efficiencies of over 80% and particle sizes of 100-200 nm. With the increase of the quaternization degree of TMC, TMC coated doxorubicin liposomes (P <0.05). At the same time, the uptake capacity of HUVECs was enhanced, and doxorubicin released into the cytoplasm faster and transported to the nucleus. Conclusion TMC-coated doxorubicin hydrochloride liposomes have strong endothelial cell targeting in vitro and are related to the degree of quaternization of TMC, which lays the foundation for further study of its targeting effect in vivo.