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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。
OBJECTIVE: To prepare lipopolysaccharide from Tolactone-lactide-co-glycolide-D-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) PLGA-TPGS nanoparticles (RPTN) were synthesized and the PLGA nanoparticles (RBG-loaded PLGA nanoparticles were prepared by using PLGA as the commercial material) nanoparticles, RPN), in vitro evaluation and comparison of the quality of two kinds of nanoparticles. Methods: RPTN and RPN were prepared by ultrasonic emulsification - solvent evaporation method. The appearance, particle size and surface charge of the two materials were measured by transmission electron microscopy and laser particle sizer respectively. The mobile phase consisted of Hypersil C 18 (4.6 mm × 250 mm, 5 μm), methanol and 0.05% glacial acetic acid (9:1) with a detection wavelength of 298 nm by reversed-phase high performance liquid chromatography RBG in RPTN and RPN drug loading, entrapment efficiency and in vitro release. Results: The particle sizes of RPTN and RPN were 152.3 nm and 331.7 nm, respectively. The drug loading and encapsulation efficiency were 18.4%, 79.3% and 15.1%, 68.6%, respectively. The cumulative release rates of RPTN and RPN were 86.7% and 72.3% respectively after 30 days of drug release in vitro, and the release of RPTN was more complete. CONCLUSION: RPTN prepared by self-made carrier is smaller than RPN, its drug loading and entrapment efficiency are larger, and it has obvious sustained-release effect in vitro and release more completely.