论文部分内容阅读
目的研究心肌特异性靶向肽PCM和穿膜肽TAT双修饰的载荧光探针香豆素-6脂质体的制备工艺,并初步考察其心肌靶向性。方法采用薄膜分散-超声法,以PCM和TAT为靶头,制备以大豆磷脂、胆固醇、DSPE-m PEG_(2000)为载体材料的载香豆素-6的双修饰脂质体;优化香豆素-6用量、靶头连接方法及靶头用量,以形态、粒径分布、电位、包封率及体外稳定性对脂质体进行表征;考察心肌细胞H_9C_2对双修饰脂质体的摄取能力,表征其心肌靶向性。结果 PCM和TAT通过插入法连接,当PCM的用量为脂质的3%、TAT的用量为脂质的1%、香豆素-6的用量为20μg时,所制得的双修饰脂质体的形态圆整,粒径分布为115.7±2.91 nm,Zeta电位为-13.1±1.81 m V,包封率为83.2%±3.1%,具有良好的体外稳定性,双修饰脂质体的心肌细胞摄取率明显高于未修饰和单修饰的脂质体。结论双修饰脂质体的制备工艺简单,PCM和TAT双修饰可提高脂质体的心肌细胞靶向性。
OBJECTIVE: To study the preparation of coumarin-6 liposomes loaded with both cardiac-specific targeting peptide (PCM) and transmembrane peptide (TAT) double-modified liposomes. Methods The modified liposomes containing coumarin-6 with soybean lecithin, cholesterol and DSPE-m PEG 2000 as the carrier material were prepared by membrane dispersion-sonication with PCM and TAT as the targets. The amount of urea-6, the method of target attachment and the amount of target were used to characterize the morphology, size distribution, potential, entrapment efficiency and in vitro stability of liposomes. , Characterizing its myocardial targeting. Results PCM and TAT were connected by insert method. When the amount of PCM was 3% of lipids, the amount of TAT was 1% of lipids and the amount of coumarin-6 was 20μg, the prepared double modified liposomes The particle size distribution was 115.7 ± 2.91 nm, the Zeta potential was -13.1 ± 1.81 mV and the entrapment efficiency was 83.2% ± 3.1%, which showed good in vitro stability. The uptake of double-modified liposomes into cardiomyocytes The rates were significantly higher than the unmodified and unmodified liposomes. Conclusion The preparation method of double-modified liposomes is simple, and double modification of PCM and TAT can enhance the cardiomyocyte targeting of liposomes.