目的 制备槲皮素纳米胶束,用以改善其溶解度。方法 以磷脂/胆盐/聚乙烯吡咯烷酮为载体材料,采用薄膜分散法制备槲皮素三元纳米胶束,对其处方及制备工艺进行筛选优化,并对制备的纳米胶束进行表征与评价。结果 优选出的最佳制备处方及工艺为槲皮素37.5 mg,大豆磷脂150 mg,脱氧胆酸钠225 mg,聚乙烯吡咯烷酮K30 60 mg置于圆底烧瓶中,加入适量体积分数95%乙醇,超声溶解,45 ℃减压旋转蒸发25 min去除有机溶剂,加入生理盐水15 mL,超声120 s匀速振摇水化脱膜,12 000 r·min-1离心5 min去除未包封药物,即得澄清槲皮素胶束溶液。槲皮素纳米胶束呈类球形,粒径为(8.0±0.5)nm,PDI为(0.153±0.06),Zeta电位为(-32.4±0.155)mV,药物包封率为(82.83±7.34)%,含量为(2.07±0.03)mg·mL-1。槲皮素纳米胶束具有良好稳定性,6个月内外观、粒径、含量无明显变化。72 h药物体外释放达到67%左右。结论 本研究的优选处方及工艺可以用于槲皮素纳米胶束的制备,其溶解度提高约750倍。
Abstract
OBJECTIVE To prepare quercetin nanomicelles and improve its solubility. METHODS Using phospholipid,bile salt and polyvinylpyrrolidone as carrier materials, quercetin ternary nanomicelles were prepared by thin film dispersion method.The formulation and preparation process were screened and optimized, and the prepared nanomicelles were characterized and evaluated. RESULTS The optimal preparation formula and process were as follows: firstly, put quercetin 37.5 mg, soybean phospholipids 150 mg, Sodium deoxycholate 225 mg, and polyvinylpyrrolidone K30 60 mg in a round-bottom flask.Secondly,It has been added an appropriate amount of 95% ethanol and dissolved by ultrasound.Thirdly, the solution was evaporated at 45 ℃ for 25 min to remove the organic solvent.At last, 15 mL of normal saline was added, and the membrane was decoated by ultrasonic 120 s shaking at a constant speed. The unencapsulated drug was removed by centrifugation at 12 000 r·min-1 for 5 min, and the quercetin micellar solution was clarified.Quercetin micelles showed regular spherical shapes.The particle size was(8.0±0.5)nm, the polydispersity index(PDI) was (0.153±0.06), the Zeta potential was (-32.4±0.155)mV, the encapsulation efficiency was(82.83±7.34)%,the content of the drug was(2.07±0.03) mg·mL-1 and the drug release in vitro reached about 67% after 72 h. Quercetin nanomicelles had good stability and no obvious change in appearance, particle size and content within 6 months. CONCLUSION The process can be used for the preparation of quercetin nanomicelles, and the solubility of quercetin is increased by about 750 times.
关键词
槲皮素 /
纳米胶束 /
溶解度 /
薄膜分散法
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Key words
quercetin /
nanomicelle /
solubility /
thin film dispersion method
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中图分类号：
R944
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参考文献
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脚注
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基金
河北省自然科学基金项目资助(H2018206052,H2020206451);河北省2021年度医学科学研究课题资助(20211108)
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