丁香苦苷固体脂质纳米粒的制备及表征
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篇名: 丁香苦苷固体脂质纳米粒的制备及表征
TITLE:
摘要: 目的:制备丁香苦苷固体脂质纳米粒(SYR-SLN),优化处方,并对其进行表征。方法:采用乳化蒸发法制备SYR-SLN,以包封率为指标,在单因素试验考察基础上,通过正交试验设计对处方中卵磷脂-单甘酯质量比、有机相-水相体积比、泊洛沙姆188(F68)浓度、投药量进行优化,确定最优处方工艺,考察所制纳米粒的包封率、载药量、形态、粒径、Zeta电位、稳定性等。结果:卵磷脂-单甘酯质量比为3 ∶ 1,有机相-水相体积比为1 ∶ 2,F68的浓度为0.4%,投药量为10 mg,最优处方工艺为单甘酯80 mg、卵磷脂240 mg、F68浓度0.4%、SYR 10 mg、无水乙醇5 mL、蒸馏水10 mL,乳化温度为65 ℃,搅拌速度为600 r/min。所得SYR-SLN的包封率为(42.35±0.60)%(n=3),载药量为(5.33±0.03)%(n=3),其外观圆整,分布均匀,平均粒径为(180.30±5.31) nm,Zeta电位为   (-41.9±0.8) mV,4 ℃条件下贮存15 d稳定性良好。结论:本方法成功制得SYR-SLN,且处方工艺简单,包封率高。
ABSTRACT: OBJECTIVE: To prepare Syringopicroside solid lipid nanoparticles (SYR-SLN), and optimize the formula and characterize SYR-SLN. METHODS: SYR-SLN were prepared by emulsion evaporation method. Using entrapment efficiency as index, based on single factor, orthogonal design was adopted to optimize the mass ratio of lecithin-monoglyceride, volume ratio of organ phase to water phase, poloxamer 188 (F68) concentration and drug dosage. The optimal formula technology was established to investigate entrapment efficiency, drug-loading amount, morphology, particle size, Zeta potential, stability, etc. RESULTS: The mass ratio of lecithin-monoglyceride was 3 ∶ 1; the volume ratio of organic phase to water phase was 1 ∶ 2; the concentration of F68 was 0.4%; drug dosage was 10 mg. The optimal formula included that monoglyceride 80 mg, lecithin 240 mg, 0.4% F68, syringopicroside 10 mg, absolute ethyl alcohol 5 mL, distilled water 10 mL, emulsification temperature at 65℃ and stirring at 600 r/min. Encapsulation efficiency of SYR-SLN was (42.35±0.60)% (n=3); drug-loading amount was (5.33±0.03)% (n=3); SYR-SLN had a spherical morphology and was evenly distributed. The average particle size was (180.30±5.31) nm with Zeta potential of (-41.9±0.8) mV, and the SYR-SLN could maintain stable for 15 days at 4℃. CONCLUSIONS: SYR-SLN is prepared successfully, and the technology is simple with high encapsulation efficiency.
期刊: 2019年第30卷第9期
作者: 张喜武,李秋晗,李英鹏,李永吉,徐坐帝,窦金金
AUTHORS: ZHANG Xiwu,LI Qiuhan,LI Yingpeng,LI Yongji,XU Zuodi,DOU Jinjin
关键字: 丁香苦苷;固体脂质纳米粒;制备;处方工艺;表征
KEYWORDS: Syringopicroside; Solid lipid nanoparticle; Preparation; Formula technology; Characterization
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