蟾皮提取物固体脂质纳米粒的质量评价

Quality Evaluation of Solid Lipid Nanoparticle of the Skin Extract of Bufobufo gargarizans

目的:对蟾皮提取物固体脂质纳米粒进行质量评价。方法:采用透射电子显微镜观察蟾皮提取物固体脂质纳米粒的形态,激光散射粒度分析仪测定其粒径,高效液相色谱法测定其中有效成分华蟾酥毒基和酯蟾毒配基的含量、包封率、载药量及华蟾酥毒基的累积释放率,另对纳米粒进行60、25、4℃3个温度下放置24 d内的稳定性考察。结果:蟾皮提取物固体脂质纳米粒大小均匀,呈球形或椭球形,平均粒径为(138.5±4.2)nm;华蟾酥毒基与酯蟾毒配基的包封率分别为90.60%、91.51%,载药量分别为35.82%、44.15%;蟾皮提取物固体脂质纳米粒中华蟾酥毒基在体外释放4 h时累积释放率约为50%,48 h时约为88%,符合Weibull方程模型(r=0.943 8);在3种考察温度下,纳米粒随放置时间的延长包封率逐渐下降,但以4℃时降低程度最小。结论:制备的蟾皮提取物固体脂质纳米粒质量评价结果均符合要求,并具有缓释性能,但建议在低温下保存。

OBJECTIVE：To evaluate the quality of solid lipid nanoparticle of the skin extract of Bufobufo gargarzans. METHODS：The morphology of solid lipid nanoparticle of the skin extract of B. gargarzans was observed by TEM. The particle size was determined by laser scattering particle size analyzer. The contents of cinobufagin and resibufogenin,encapsulation efficiency,drug-loading amount and accumulative release rate of cinobufagin were determined by HPLC. The stability of nanoparticle was investigated within 24 h at 60,25 and 4 ℃. RESULTS：The solid lipid nanoparticle of the skin extract of B. gargarzans were uniform in particle size and showed round and spheroidicity shape;average particle size was（138.5±4.2）nm,The encapsulation efficiency of cinobufagin and resibufogenin were 90.60% and 91.51%,and drug-loading amount were 35.82% and 44.15%. The accumulative release rate of cinobufagin was 50% at 4 h and reached 88% at 48 h,which was in line with Weibull equation（r=0.943 8）.Under 3 kinds of temperature conditions,encapsulation efficiency decreased gradually as the holding time of nanoparticle prolonged;the decrease degree was the smallest at 4 ℃.CONCLUSIONS：The quality evaluation results of solid lipid nanoparticle of the skin extract of B. gargarzans are in line with the standard,and prepared nanoparticles show sustained-release effects and should be kept under low temperature.