目的制备载硫酸长春新碱的聚乳酸-乙醇酸-聚乙二醇共聚物(PLGA-PEG)超声微泡造影剂,观察微泡的一般特性及体内、外显影效果。方法采用W/O/W复乳-溶剂挥干法制备超声微泡造影剂,正交实验设计获得最佳制备工艺,采用紫外分光光度法测定微泡的包封率和载药量,光学显微镜观察微泡形态,以马尔文激光粒径测量仪测定微泡造影剂的粒径、Zeta电位,并观察微泡在兔心腔的显影效果。结果获得的微泡造影剂为球形,平均粒径约为1·27μm,包封率为(37·63±0·61)%,Zeta电位为-24·88mV,静脉注射载药微泡后,能增强兔心腔超声显影效果。结论采用复乳-溶剂挥干法成功制备超声微泡造影剂,能增强体内外超声显影效果。
Objective To prepare vincristine-loaded PLGA-PEG ultrasound microbubbles contrast agent(VCR-PLGA-PEG-UMCA),and to evaluate its characteristics and imaging effect in vivo and in vitro.Methods A water-in-oil-in-water double-emulsion/solvent evaporation method was used to prepare microbubbles.Orthogonal experimental design was used to select the optimal formulation.Ultraviolet spectrophotometry was applied to determine the entrapment efficiency of microbubbles,the morphology of microbubbles was observed with optical microscopy and particle size,Zeta potential was measured with Malvern laser particle size measuring instrument.Then the imaging effect of VCR-PLGA-PEG-UCMA was evaluated in 2 rabbits in vivo.Results Acquired microbubbles were spherical,the mean diameter was 1.27 μm,the drug entrapment efficiency was(37.63±0.61)% and Zeta potential was-24.88 mV.VCR-PLGA-PEG-UMCA enhanced the heart imaging effect of the rabbits in vivo.Conclusion VCR-PLGA-PEG-UMCA is successfully prepared with the above methods,and can enhance the imaging effect in vitro and in vivo.