丁香苦苷固体脂质纳米粒的制备及表征

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∶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。

Preparation and Characterization of Syringopicroside Solid Lipid Nanoparticles

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.