脂蟾毒配基PLGA-TPGS纳米粒的质量评价

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 PLGA-TPGS 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 C₁₈（4.6 mm×250 mm，5 μm），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。

Quality evaluation of resibufogenin-loaded PLGA-TPGS nanoparticles

OBJECTIVE To characterize and evaluate resibufogenin (RBG)-loaded polylactide-co-glycolide-D-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles (RPTN) and RBG-loaded polylactide-co-glycolide (PLGA) nanoparticles (RPN), with RBG as model drug and PLGA-TPGS or PLGA as polymer materials.METHODS RPTN was prepared using the ultrasonic emulsification-solvent evaporation method, and characterized with RPN together in surface morphology using a transmission electron microscope, particle size and surface charge by a Nano ZS90 light scattering and laser Doppler anemometry. Drug loading (DL), entrapment efficiency (EE) and in vitro drug release of RBG in the RBG-loaded NPs were measured using a reverse phase-high performance liquid chromatography (RP-HPLC) on a Hypersil C₁₈ column (4.6×250 mm, 5 μm) with methanol and 0.05% acetic acid (90:10) as mobile phase, the detective wavelength was 298 nm.RESULTS The transmission electron microscope revealed that the nanoparticles were spherical and regular. The average particle sizes of RPTN and RPN were 152.3 nm and 331.7 nm, and their DLs were approximately 18.4% and 15.1% and EEs were approximately 79.3% and 68.6%, respectively. Both nanoparticles showed sustained drug release, and the cumulative RBG release rates of RPTN and RPN after 30 d reached 86.7% and 72.3%, respectively.CONCLUSION RPTN has smaller particle size, higher DL and EE, shows sustained drug release and releases more completely than RPN in vitro.