阿魏酸川芎嗪固体脂质纳米粒的处方优化及质量评价
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篇名: 阿魏酸川芎嗪固体脂质纳米粒的处方优化及质量评价
TITLE:
摘要: 目的:优化阿魏酸川芎嗪(FATM)固体脂质纳米粒(FATM-SLN)的处方,并进行质量评价。方法:采用乳化-超声法制备FATM-SLN。以粒径、包封率为指标,以单硬脂酸甘油酯、蛋黄卵磷脂(PC)、泊洛沙姆188(P188)、硬脂酸钠用量为因素,通过单因素试验和正交试验优化FATM-SLN处方,并进行验证试验。考察所制FATM-SLN的外观形态、粒径分布、Zeta电位、稳定性和体外释放度。结果:最优处方为FATM 10 mg、单硬脂酸甘油酯 300 mg、PC 200 mg、P188 200 mg、硬脂酸钠10 mg、纯化水20 mL。所制FATM-SLN呈类球形实体粒子,外观形态较圆整,粒径分布为40~800 nm,平均粒径为106.23 nm,多分散系数为0.254,Zate电位为-34.8 mV,包封率为73.32%,载药量为1.20%;4 ℃下10 d内外观无明显变化(RSD<2%)。其在0.5~1 h内释药最快,1 h的累积释放度达到60.47%;8 h后释药趋于平稳,累积释放度为93.46%,药物基本释放完全。结论:成功优化FATM-SLN的处方;所制FATM-SLN的粒径小、包封率高、稳定性好。
ABSTRACT: OBJECTIVE: To optimize the formulation of ferulic acid ligustrazine (FATM) solid lipid nanoparticles (FATM- SLN), and conduct the quality evaluation. METHODS: Emulsification ultrasonic method was used to prepare FATM-SLN. Using particle size and entrapment efficiency as indexes, amount of glyceryl monostearate, egg yolk lecithin (PC), poloxamer 188 (P188), and sodium stearate as factors, single factor test and orthogonal test were used to optimize the formulation; and verification test was conducted. The appearance morphology, distribution of particle size, Zeta potential, stability and in vitro release degree of prepared FATM-SLN were investigated. RESULTS: The optimal formulation was as follows as FATM of 10 mg, glyceryl monostearate of 300 mg, PC of 200 mg, P188 of 200 mg, sodium stearate of 10 mg, and purified water of 20 mL. The prepared FATM-SLN showed spherical solid particles, appearance morphology was round, distribution of particle size was 40-800 nm, particle size was 106.23 nm, polydispersity index was 0.254, Zeta potential was -34.8 mV, entrapment efficiency was 73.32%, drug loading was 1.20%; the appearance had no obvious changes within 10 d in 4 ℃ (RSD<2%). The drug-release in 0.5-1 h was the fastest, the cumulative release degree reached to 60.47%; it tended to be stable after 8 h, the cumulative release degree reached to 93.46%, and drugs were basically released completely. CONCLUSIONS: FATM-SLN formulation is successfully optimized, and the prepared FATM-SLN has small particle size, high entrapment efficiency and good stability.
期刊: 2017年第28卷第31期
作者: 孙陶利,戴智,蒋鹏程,吴柱,刘卫平,卜振军,唐靖,王建芬,马宁
AUTHORS: SUN Taoli,DAI Zhi,JIANG Pengcheng,WU Zhu,LIU Weiping,BU Zhenjun,TANG Jing,WANG Jianfen,MA Ning
关键字: 阿魏酸川芎嗪;固体脂质纳米粒;处方优化;正交试验;粒径分布;质量评价
KEYWORDS: Ferulic acid ligustrazine; Solid lipid nanoparticles; Formulation optimization; Orthogonal test; Distribution of particle size; Quality eraluation
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