阿德福韦酯纳米脂质载体的制备及处方优化
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篇名: | 阿德福韦酯纳米脂质载体的制备及处方优化 |
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摘要: | 目的:制备阿德福韦酯纳米脂质载体(ADV-NLC),并优化其处方。方法:以硬脂酸和单硬脂酸甘油酯为固体脂质,油酸为液体脂质,双子(Gemini)表面活性剂、聚山梨酯80为乳化剂,十二烷基硫酸钠(SDS)为稳定剂,采用溶剂分散-超声法制备ADV-NLC。以粒径、多分散指数、Zeta电位和包封率为指标,单因素试验筛选Gemini表面活性剂-聚山梨酯80比例、乳化剂用量(乳化剂与水相之比)、药脂比、固-液脂质比。结果:处方为乳化剂(双子表面活性剂-聚山梨酯80比例1 ∶ 2)用量3%、药脂比4.5%,固-液脂质比6 ∶ 5。所制ADV-NLC的平均粒径为(48.83±2.65) nm,多分散指数<0.3,Zeta电位为(-28.7±1.8) mV,包封率为(77.65±0.03)%(n=3)。结论:成功制得ADV-NLC,且处方合理、可行。 |
ABSTRACT: | OBJECTIVE: To prepare nanostructured lipid carrier of adefovir dipivoxil (ADV-NLC), and optimize the formulation. METHODS: Using stearic acid and glycerin monostearate as solid lipid, oleic acid as liquid lipid, Gemini surfactant and polysorbate 80 as emulsifier, sodium dodecyl sulfate (SDS) as stabilizer, solvent dispersion ultrasonic method was used to prepare ADV-NLC. And using particle size, polydispersity index, Zeta potential, encapsulation efficiency as indexes, single factor test was conducted to screen Gemini surfactant-polysorbate 80 ratio, emulsifier dosage (ratio of emulsifier to water phase), drug-lipid ratio, solid-liquid lipid ratio. RESULTS: The formula was as follow as 3% emulsifier (Gemini surfactant-polysorbate 80 ratio of 1 ∶ 2), 4.5% drug-lipid ratio, solid-liquid lipid ratio of 6 ∶ 5. The average particle size of the prepared ADV-NLC was (48.83±2.65) nm, polydispersity index<0.3, Zeta potential was (-28.7±1.8) mV, encapsulation efficiency was (77.65±0.03)% (n=3). CONCLUSIONS: ADV-NLC is successfully prepared, and the formulation is reasonable and feasible. |
期刊: | 2017年第28卷第16期 |
作者: | 孙珊珊,王慧云,王飞飞,丁林 |
AUTHORS: | SUN Shanshan,WANG Huiyun,WANG Feifei,DING Lin |
关键字: | 阿德福韦酯;纳米脂质载体;双子表面活性剂;处方优化 |
KEYWORDS: | Adefovir dipivoxil; Nanostructured lipid carrier; Gemini surfactant; Formulation optimization |
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