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星点设计-响应面法优化积雪草苷阳离子脂质体的处方
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| 篇名： | 星点设计-响应面法优化积雪草苷阳离子脂质体的处方 |
| TITLE： | |
| 摘要： | 目的：优化积雪草苷阳离子脂质体的处方，并对其体外释药特性进行考察。方法：采用薄膜分散法制备脂质体；以包封率、载药量为指标，以积雪草苷与磷脂质量比（药脂比，X1）、胆固醇与磷脂质量比（X2）、D-甘露糖质量浓度（X3）为因素，采用星点设计-响应面法优化处方；以十二烷基硫酸钠为介质，采用透析袋法考察加入1％十八胺所制阳离子脂质体的体外释药特性，并与积雪草苷的溶液及普通脂质体进行比较。结果：最优处方为X1 0.07、X2 0.17、X3 0.03 g/ml，所得积雪草苷脂质体的包封率为（75.529±1.071）％、载药量为（2.539±0.029）％（n＝3），与预测值的偏差分别为－0.217％与0.205％；脂质体加入1％十八胺后其电位由 －5.6 mV变为20.8 mV，证实形成阳离子脂质体。积雪草苷溶液、普通脂质体、阳离子脂质体的体外累积释药率分别为89.13％（12 h）、87.58％（72 h）、94.46％（72 h），后者释药符合Weibull模型。结论：所得积雪草苷阳离子脂质体包封率较高，可持续72 h释药。 |
| ABSTRACT： | OBJECTIVE： To optimize the formulation of Asiaticoside cationic liposomes， and to investigate the characteristics of drug release in vitro. METHODS： The thin film dispersion method was used to prepare liposome； using encapsulation efficiency and drug-loading amount as index， the formulation of Asiaticoside liposomes was optimized by central composite design-response surface method with the ratio of drug to lipid （X1）， the ratio of cholesterol to lipid （X2） and the concentration of D-mannose （X3） as factors. Using sodium lauryl sulfate as medium， in vitro release characteristics of cationic liposomes prepared with 1％ octadecylamine was investigated by bag filter method， and compared with those of Asiaticoside solution and common liposome. RESULTS： The optimal formulation was X1 0.07， X2 0.17 and X3 0.03 g/ml. The encapsulation efficiency was （75.529±1.071）％， and drug-loading amount was （2.539±0.029）％ （n＝3）； the deviation from the predicted values were －0.217％ and 0.205％； 1％ octadecylamine was add into formulation to obtain cationic liposomes， and the Zeta potential had changed from －5.6 mV to 20.8 mV. in vitro accumulative release rates of Asiaticoside solution， common liposomes and cationic liposomes were 89.13％（12 h）， 87.58％（72 h） and 94.46％（72 h）， and the latter was in line with Weibull model. CONCLUSIONS： Asiaticoside cationic liposomes have high encapsulation efficiency， and can releases for 72 h. |
| 期刊： | 2016年第27卷第16期 |
| 作者： | 任翔，刘琨，张莉 |
| AUTHORS： | REN Xiang，LIU Kun，ZHANG Li |
| 关键字： | 积雪草苷；阳离子脂质体；处方优化；星点设计-响应面法；体外释药 |
| KEYWORDS： | Asiaticoside； Cationic liposomes； Formulation optimization； Central composite design-response surface method； Drug release in vitro |
| 阅读数： | 461 次 |
| 本月下载数： | 1 次 |
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