槲皮素固体脂质纳米粒的制备及理化性质的评价

Preparation of quercetin solid lipid nanoparticles and evaluation of their physical and chemical properties

目的制备槲皮素固体脂质纳米粒并对其理化性质进行评价。方法通过熔融超声法制备Que-SLN,以槲皮素的投药量、单硬脂酸甘油酯-蛋黄卵磷脂的质量比,、泊洛沙姆188的含量、超声时间为影响要素,包封率和载药量为评价指标,正交试验优化制备工艺;透析法考察体外释放特性。结果最优处方为槲皮素5.0mg, GMS质量分数为50%,P188百分含量为1%,超声时间为5min。制备的Que-SLN外观呈球形,形态较圆整,大小均一,粒径(191.2 3±3.25)nm, PDI为(0.19±0.04),电位(-24.40±1.24)mV,包封率为(90.54±1.36)%,载药量(4.33±0.06)%,槲皮素药物浓度为452.7 0mg/L,72h内具有缓释作用,累计释放率为(87.60±0.66)%。结论熔融超声法适用于Que-SLN的制备,可增加槲皮素在水中的溶解度,Que-SLN在72h内具有缓释作用。

Objective To prepare quercetin solid lipid nanoparticles and evaluate their properties. Methods Que-SLN were prepared by melt ultrasound. The formulation and preparation process was optimized by orthogonal test with the dosage of quercetin, the mass fraction of glycerol monostearate, the percentage of poloxamer 188, the ultrasonic time as the influencing factors, the encapsulation efficiency and drug loading as the evaluation indexes. The release characteristic in vitro was investigated by dialysis method. Results The optimum formulation was quercetin dosage of 5.0 mg, glycerin monostearate percentage of 50%, P188 percentage of 1%, ultrasound time of 5 min. The particle size was(191.2 3±3.25)nm, PDI was(0.19±0.04), the zeta potential was(-24.4±1.24) mV, the encapsulation efficiency was(90.54±1.36)%, the drug loading content was(4.33±0.06)%. The Que content was 452.70 mg· L^(-1).The drug showed a sustained release up to 87.60% within 72 hours. Conclusion The melt ultrasound method is suitable for the preparation of Que-SLN, which increases the solubility of quercetin and Que-SLN has sustained-release effect in 72 h.