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目的制备携载PSMA单克隆抗体的载阿霉素纳米泡,观察其基本特性和体内显影能力。方法机械震荡法制备靶向载药纳米泡,观察其形态、大小、载阿霉素和偶联PSMA单克隆抗体的情况。检测粒径和电位,检测载药浓度,并在超声波治疗仪辐照下检测药物释放率。将靶向载药纳米泡与临床用微米级声学造影剂对比研究,观察二者在小鼠肝肾的增强造影效果。结果靶向载药纳米泡大小、分布均匀。荧光显微镜显示阿霉素和PSMA单克隆抗体与纳米泡结合。纳米泡粒径(793.80±92.05)nm,电位(8.74±2.41)mV,载药浓度(1.18±0.11)mg/ml。辐照下,阿霉素释放率(48.65±3.99)%。靶向载药纳米泡在小白鼠肝肾显影的达峰时间、上升时间和持续显影时间均长于临床用微米级声学造影剂,且有统计学差异(P<0.05),而峰值强度无统计学差异(P>0.05)。结论本实验成功制备了性质稳定的携载PSMA单克隆抗体载药纳米泡,且在体内有较好的显影效果,为今后应用靶向纳米泡作为化疗药物载体靶向治疗前列腺癌的研究提供了基础。
OBJECTIVE: To prepare doxorubicin-loaded nanobubbles carrying PSMA monoclonal antibody and observe its basic characteristics and in vivo imaging ability. Methods Targeted drug-loaded nanobubbles were prepared by mechanical shaking method. Morphology, size, doxorubicin-loaded and conjugated PSMA monoclonal antibodies were observed. Detection of particle size and potential, detection of drug concentration, and ultrasonic testing instrument to detect drug release rate. Targeted drug-loaded nanobubbles and clinical contrast with micron-level contrast agent to study the two in mice liver and kidney enhanced contrast imaging. Results Targeted drug-loaded nanobubble size, uniform distribution. Fluorescence microscopy showed that doxorubicin and PSMA monoclonal antibodies bind to the nanobubbles. The nanobubble size (793.80 ± 92.05) nm, potential (8.74 ± 2.41) mV and drug loading concentration (1.18 ± 0.11) mg / ml, respectively. Under irradiation, doxorubicin release rate (48.65 ± 3.99)%. Targeted drug-loaded nanobubbles in the rat liver and kidney development peak time, rise time and duration of development were longer than clinical micron-level contrast agent, and there was a significant difference (P <0.05), while the peak intensity was not statistically significant Difference (P> 0.05). CONCLUSIONS: The stable nanocapsules loaded with monoclonal antibody against PSMA were successfully prepared in this study and have good imaging results in vivo. These results provide the basis for the future research of targeting nanobubbles as a chemotherapeutic drug carrier for the treatment of prostate cancer basis.