脂蟾毒配基PLGA-TPGS纳米粒的质量评价

发布时间：2018-11-23 08:49

【摘要】：目的:以自制材料乙交酯丙交酯共聚物-维生素E聚乙二醇1000琥珀酸酯(polylactide-co-glycolide-D-α-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS)为载体制备脂蟾毒配基PLGA-TPGS纳米粒(Resibufogenin-loaded PLGATPGS nanoparticles,RPTN),并以市售材料乙交酯丙交酯共聚物(PLGA)为载体制备脂蟾毒配基PLGA纳米粒(RBG-loaded PLGA nanoparticles,RPN),体外评价和比较2种纳米粒的质量。方法:采用超声乳化-溶剂挥发法制备RPTN和RPN,用透射电子显微镜和激光粒度仪分别测定二者的外观、粒径、表面电荷。采用反相高效液相色谱法,色谱柱为Hypersil C_(18)(4.6mm×250 mm,5μm),甲醇和0.05%冰醋酸溶液(9∶1)为流动相,检测波长为298 nm,测定RBG在RPTN和RPN中的载药量、包封率和体外释放度。结果:RPTN和RPN的粒径分别为152.3 nm和331.7 nm,载药量和包封率分别为18.4%、79.3%和15.1%、68.6%。体外药物释放30 d时RPTN和RPN的体外累积释放率分别为86.7%和72.3%,RPTN释放较完全。结论:自制载体制备的RPTN比RPN粒径更小,载药量和包封率更大,体外有明显的缓释作用,释放更完全。
[Abstract]:Objective: to prepare PLGA-TPGS nanoparticles (Resibufogenin-loaded PLGATPGS nanoparticles, 伪-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS) using polylactide-co-glycolide-D- 伪-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS as the carrier of glycolide copolymers and vitamin E polyethylene glycol 1000. The ligands of PLGA nanoparticles (RBG-loaded PLGA nanoparticles,RPN) were prepared by using (PLGA) as the carrier, and the quality of the two nanoparticles was evaluated and compared in vitro. Methods: RPTN and RPN, were prepared by phacoemulsification and solvent volatilization. The appearance, particle size and surface charge of RPTN and RPN, were measured by transmission electron microscope (TEM) and laser particle size analyzer respectively. Hypersil C18 column (4.6mm 脳 250 mm,5 渭 m), methanol and 0.05% glacial acetic acid solution (9:1) was used as mobile phase by RP-HPLC. The detection wavelength was 298 nm, to determine the drug loading of RBG in RPTN and RPN. Encapsulation efficiency and in vitro release. Results: the particle sizes of RPTN and RPN were 152.3 nm and 331.7 nm, respectively, and the entrapment efficiency were 18.4% and 15.1%, respectively. The cumulative release rates of RPTN and RPN were 86.7% and 72.3% respectively. Conclusion: compared with RPN, the RPTN prepared by self-made carrier has smaller particle size, larger drug loading and encapsulation efficiency, and has obvious slow-release effect and more complete release in vitro.
【作者单位】： 大连医科大学基础医学院;大连医科大学药学院;大连医科大学;
【基金】：辽宁省自然科学基金项目(编号:2015020308)
【分类号】：R94
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本文编号：2350963