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目的:研究胆固醇衍生物(CTBBA)脂质体的物理稳定性,细胞相容性以及药物输送。方法:CTBBA组入脂质体并测定不同pH下的zeta电位。对长期保存的脂质体进行粒径分析和含磷量分析,评价脂质体的物理稳定性。通过测定包封在脂质体内的阿霉素的体外释放,来评价CTBBA对脂质体释放药物的影响。用MTT法检测CTBBA本身以及CTBBA脂质体的细胞相容性。评估了用流式细胞仪和荧光显微镜检测脂质体细胞内药物输送能力的可行性。结果:zeta电位数据表明CTBBA脂质体带有正电荷,可以改善脂质体在长期保存过程中的物理稳定性;作为胆固醇衍生物的CTBBA能有效的降低药物的渗漏;相比某些正电荷载体,CTBBA的细胞毒性较低;流式细胞仪在反映阿霉素脂质体的细胞定位上有局限,固定液的使用会改变阿霉素荧光的细胞内分布。结论:正电荷CTBBA脂质体具有改善脂质体长期保存稳定性,且细胞毒性低的特点。流式细胞仪不能完全反映载药的CTBBA脂质体在细胞内的分布。
Objective: To study the physical stability, cell compatibility and drug delivery of cholesterol derivative (CTBBA) liposomes. Methods: The CTBBA group was injected with liposomes and the zeta potential was measured at different pH values. The long-term preservation of liposomes and particle size analysis of phosphorus content, liposomes to assess the physical stability. The effect of CTBBA on liposomal drug release was evaluated by measuring the in vitro release of doxorubicin encapsulated in liposomes. The cytocompatibility of CTBBA itself and CTBBA liposomes were determined by MTT assay. The feasibility of using flow cytometry and fluorescence microscopy to detect drug delivery in liposomes was evaluated. Results: The zeta potential data showed that the CTBBA liposomes possessed positive charge, which could improve the physical stability of the liposomes during long-term storage. As a cholesterol derivative, CTBBA could effectively reduce drug leakage. Compared with some positive Cytotoxicity of CTBBA was lower than that of CTBBA. Flow cytometry was limited in cell localization of doxorubicin liposomes. The use of fixative could change the intracellular distribution of doxorubicin fluorescence. Conclusion: The positive CTBBA liposomes have the characteristics of long-term storage stability and low cytotoxicity. Flow cytometry does not fully reflect the intracellular distribution of drug loaded CTBBA liposomes.