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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。
Objective: To optimize the formulation of ligustrazine ferulate (FATM) solid lipid nanoparticles (FATM-SLN) and evaluate its quality. Methods: FATM-SLN was prepared by emulsion-sonication. Using particle size and entrapment efficiency as indexes, the effects of glycerol monostearate, egg yolk lecithin (PC), poloxamer 188 (P188) and sodium stearate dosage were studied by single factor test and orthogonal test Optimize FATM-SLN prescriptions and perform validation experiments. The morphology, particle size distribution, Zeta potential, stability and in vitro release of FATM-SLN were investigated. Results: The optimal prescription was FATM 10 mg, glyceryl monostearate 300 mg, PC 200 mg, P188 200 mg, sodium stearate 10 mg and purified water 20 mL. The prepared FATM-SLN was a spherical solid particle with a round appearance with a particle size distribution of 40 to 800 nm, an average particle size of 106.23 nm, a polydispersity coefficient of 0.254 and a Zate potential of -34.8 mV with an encapsulation efficiency of 73.32% and the drug loading was 1.20%. There was no significant change in appearance within 10 days at 4 ℃ (RSD <2%). The drug release was the fastest in 0.5-1 h, and the cumulative release reached 60.47% in 1 h. After 8 h, the drug release tended to be steady with a cumulative release of 93.46%. The drug release was complete. Conclusion: The prescription of FATM-SLN is successfully optimized. The particle size of FATM-SLN is small, the entrapment efficiency is high, and the stability is good.