2017 年第 2 期 第 15 卷

载长春瑞滨红细胞载药体系的建立及其体外评价

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关键词：药物载体红细胞长春瑞滨抗肿瘤治疗

• 摘要：
• 【摘要】目的 将长春瑞滨包载于载体红细胞中，建立载长春瑞滨红细胞载药体系，并对其进行体外评价。方法 利用改良低渗预膨胀法制备载长春瑞滨红细胞载药体系，紫外分光光度计测定长春瑞滨载药量、包载率，并对其体外贮存、释药进行评估。利用MTT法评价载长春瑞滨红细胞的细胞增殖抑制作用。结果 载长春瑞滨红细胞包载率为70.92%，在体外能稳定贮存5天，包载过程中红细胞形态、性质无明显变化，载体红细胞对包载的长春瑞滨可以稳定释放，48小时释放率接近100%。载药红细胞对A549细胞作用48小时后，当长春瑞滨浓度为0.0125、0.025mg/ml 时载长春瑞滨红细胞对细胞增殖抑制率均强于裸药长春瑞滨(P<0.05)，且产生相同抑制率时，载长春瑞滨红细胞所需要的长春瑞滨剂量低于裸药长春瑞滨。结论 本实验建立的载长春瑞滨红细胞载药体系性质稳定，具有缓释作用，且在一定药物浓度条件下能提高疗效。
• Objective： To demonstrate the feasibility of establishing carrier erythrocytes by the technology and evaluate the carrier erythrocytes in vitro. Methods： Establishing carrier erythrocytes by a modified hypotonic preswelling technique. The drug loading, encapsulation efficiency of irinotecan and release in vitro were detected by ultraviolet spectrophotometer .Cell proliferation inhibition was measured by MTT to compare the cytotoxicity of vinorelbine -loaded erythrocytes and free vinorelbine. Results：The modified hypotonic preswelling technique is a effective method to establish carrier erythrocytes and vinrelbine-loaded erythrocytes with the drug loading ratio approximate 70.92%. Carrier erythrocytes can release vinorelbine sustainably, and approaching 100% vinorelbine was released from carrier erythrocytes at 48h. When the dose of vinorelbine at 0.0125,0.025 g/l, vinorelbine-loaded erythrocytes appeared better cell proliferation inhibition than free vinorelbine when incubated with A549 for 48h . Conclusion：The carrier erythrocytes in this research is stable and have sustained release.