青藤碱聚乳酸羟基乙酸共聚物-水溶性维生素E纳米粒的质量评价

发布时间：2018-01-22 02:24

  本文关键词： 青藤碱 聚乳酸羟基乙酸共聚物-水溶性维生素E 纳米粒 质量评价 体外释放度 稳定性　出处：《中国药房》2015年07期 　论文类型：期刊论文

【摘要】：目的:对青藤碱聚乳酸羟基乙酸共聚物-水溶性维生素E(PLGA-TPGS)纳米粒(SPTN)的质量进行评价。方法:以PLGATPGS为载体,采用超声乳化-溶剂挥发法制备SPTN;另以PLGA为载体制备青藤碱PLGA纳米粒(SPN)作为对照。采用激光粒度仪测定2种纳米粒的粒径和Zeta电位;采用高效液相色谱法测定2种纳米粒中药物含量,计算其载药量、包封率、体外释放度和考察SPTN的体外稳定性,色谱柱为Hypersil C18,流动相为甲醇-10 mmol/L磷酸二氢钠(38∶62,V/V),流速为1.0 ml/min,检测波长为262 nm,进样量为20μl。结果:SPTN和SPN的平均粒径分别为(194.6±2.8)、(382.4±3.2)nm,Zeta电位分别为(-21.3±1.7)、(-13.9±2.3)m V;载药量分别为(9.5±0.7)%、(6.2±0.8)%,包封率分别为(41.3±1.6)%、(32.8±1.8)%;体外药物释放二者均呈两相释放,30 d时累积释放度分别为92.8%、71.3%;与0 d时比较,高温(40℃)、强光[(4 500±500)lx]、高湿[(90±5)%]条件下10 d内SPTN的外观性状、粒径、载药量均无明显变化,6个月的加速试验和12个月的长期试验中SPTN的外观性状、粒径、载药量也均无明显变化。结论:SPTN具有比SPN更小的粒径、更大的载药量和包封率,体外释放更完全,具有明显的缓释作用,体外稳定性好。
[Abstract]:Objective: to evaluate the quality of sinomenine poly (lactic acid glycolic acid) copolymers, water-soluble vitamin E (PLGA-TPGS) nanoparticles. Methods: PLGATPGS was used as the carrier. SPTNs were prepared by phacoemulsification and solvent volatilization. In addition, sinomenine PLGA nanoparticles were prepared with PLGA as the carrier. The particle size and Zeta potential of the two kinds of nanoparticles were measured by laser particle size analyzer. High performance liquid chromatography (HPLC) was used to determine the drug content in the two nanoparticles. The drug loading, encapsulation efficiency, release in vitro and the stability of SPTN in vitro were calculated. The chromatographic column was Hypersil C18. The mobile phase consisted of methanol-10 mmol/L sodium dihydrogen phosphate (38: 62 V / V), the flow rate was 1.0 ml / min, and the detection wavelength was 262 nm. Results the average particle size of SPN was 194.6 卤2.8 渭 l and 382.4 卤3.2 nm, respectively. The Zeta potentials were -21.3 卤1.7mV and 13.9 卤2.3mV, respectively. The drug loading rate was 9.5 卤0.7 and the entrapment rate was 41.3 卤1.6 and 32.8 卤1.8 respectively. The cumulative release rates of both drugs in vitro were 92.8% and 71.3% respectively at 30 days after release. Compared with 0 d, high temperature 40 鈩，

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