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目的比较能被超声击破的两种载紫杉醇超声微泡的制备方法,并评价其理化性质以及超声散射强度。方法用单纯紫杉醇法Ⅰ号和三醋酸甘油酯溶解法Ⅱ号分别制备载紫杉醇脂质超声微气泡,测定其包封率、载药量、粒径大小、分布和Zeta电位、pH值,并行超声击破试验及兔VX2皮下肿瘤显像试验。结果两种微泡显像无明显差异,可被低能量超声击破,但Ⅱ号(加入三醋酸甘油酯)脂质微泡较Ⅰ号(常规冷冻干燥法制备)载药微泡粒径显著减小[(1.07±0.38)μmvs(2.79±0.41)μm,P<0.01],表面电位增高[(19.10±0.32)mVvs(-5.90±0.21)mV,P<0.01],包封率和载药量显著增高[(95.00±1.22)%vs(36.10±4.74)%,P<0.01;(5.60±0.11)%vs(0.50±0.04)%,P<0.01]。结论三醋酸甘油酯溶解法制备的Ⅱ号微泡在局部药物释放中具有更大的应用价值。
OBJECTIVE: To compare the preparation methods of two paclitaxel-loaded ultrasound microbubbles that can be broken by ultrasound and to evaluate the physicochemical properties and the intensity of ultrasonic scattering. Methods Paclitaxel lipid microbubbles were prepared by paclitaxel method Ⅰ and glyceryl triacetate method Ⅱ, respectively. The entrapment efficiency, drug loading, particle size distribution, Zeta potential and pH value were measured. Breaking test and rabbit VX2 subcutaneous tumor imaging test. Results There was no significant difference between the two kinds of microbubble imaging, which could be ruptured by low-energy ultrasound. However, the particle size of drug-loaded microbubbles of No. Ⅱ (adding triacetin) lipid microbubbles was significantly decreased compared with that of No. 1 (routine lyophilization) (P0.01 ± 0.38) μm vs (2.79 ± 0.41) μm, P <0.01], the surface potential increased (19.10 ± 0.32) mV vs (-5.90 ± 0.21) mV, P <0.01] (95.00 ± 1.22)% vs (36.10 ± 4.74)%, P <0.01; (5.60 ± 0.11)% vs (0.50 ± 0.04)% respectively, P <0.01]. Conclusion Ⅱ microemulsion prepared by triacetin dissolution has a greater value in the local drug release.