姜黄素纳米粒冻干粉的反溶剂法制备工艺优化及溶出特征
发布时间：2019-04-18 18:42
【摘要】：目的优化姜黄素(Cur)纳米粒冻干粉(CNLP)制备工艺。方法以丙酮作为溶剂,去离子水作为反溶剂,聚山梨酯-80(P80)作为表面活性剂,甘露醇作为冻干保护剂通过反溶剂法制备CNLP,采用单因素分析法进行CNLP制备工艺的优化。影响CNLP粒径大小的因素有Cur质量浓度、溶剂与反溶剂体积比、表面活性剂用量、沉积时间、搅拌速率、冻干保护剂用量;得到的CNLP与原粉进行饱和溶解度和体外溶出对比实验。结果制备CNLP最优工艺为Cur质量浓度8mg/m L、溶剂与反溶剂比1∶5、表面活性剂用量0.05%、沉积时间5 min、搅拌速率400 r/min、冻干保护剂甘露醇与Cur质量比4∶1;获得的CNLP平均粒径大小为(172.2±4.6)nm;CNLP复溶液Zeta电位为(-19.7±3.7)m V;SEM图谱显示Cur原粉呈不规则的大块状,粒径在20μm左右。CNLP呈不规则的均匀块状结构,粒径在170 nm左右,与原粉相比粒径明显减小。从以上CNLP的形态来看,由激光粒度仪测得的CNLP平均粒径是基本一致的。通过饱和溶解度检测,在去离子水中,CNLP的饱和溶解度是原粉的41.32倍;在人工胃液中,CNLP饱和溶解度是原粉的1.74倍;在人工肠液中,CNLP饱和溶解度是原粉的4.11倍。通过溶出度检测,在去离子水中,CNLP的溶出速率是原粉的14.51倍;在人工胃液中,CNLP的溶出速率是原粉的2.33倍;在人工肠液中,CNLP的溶出速率是原粉的44.79倍。结论反溶剂法制备的CNLP可以改善Cur水溶性,有利于提高Cur的生物利用度。
[Abstract]:Objective to optimize the preparation of curcumin (Cur) nanoparticles freeze-dried powder (CNLP). Methods CNLP, was prepared with acetone as solvent, deionized water as anti-solvent, polysorbate-80 (P80) as surfactant and mannitol as freeze-drying protectant to prepare CNLP by anti-solvent method. The factors influencing the particle size of CNLP include the mass concentration of Cur, the volume ratio of solvent to antisolvent, the dosage of surfactant, the deposition time, the stirring rate and the dosage of freeze-dried protectant, and the saturated solubility and dissolution in vitro of the obtained CNLP are compared with that of the original powder. Results the optimum conditions for preparing CNLP were as follows: the mass concentration of Cur was 8mg/m / L, the ratio of solvent to antisolvent was 1? 5, the dosage of surfactant was 0.05%, the deposition time was 5 min, the stirring rate was 400r / min, and the mass ratio of mannitol to Cur was 4? The average particle size of CNLP was (172.2 卤4.6) nm;CNLP. The Zeta potential of complex solution was (- 19.7 卤3.7) m V;). The SEM pattern showed that the Cur powder was irregular and large, the particle size was about 20 渭 m, and the size of the raw powder was about 170 nm, which was smaller than that of the original powder. The size of the raw powder was about 20 渭 m, and the size of the powder was about 170 nm. According to the morphology of CNLP, the average particle size of CNLP measured by laser particle sizer is basically the same. The saturated solubility of CNLP in deionized water was 41.32 times that of original powder, the saturated solubility of CNLP in artificial gastric juice was 1.74 times higher than that of original powder, and the saturated solubility of CNLP in artificial intestinal fluid was 4.11 times of that of original powder. The dissolution rate of CNLP in deionized water was 14.51 times that of original powder, the dissolution rate of CNLP in artificial gastric juice was 2.33 times of that of original powder, and the dissolution rate of CNLP in artificial intestinal fluid was 44.79 times of that of original powder. Conclusion CNLP prepared by anti-solvent method can improve the water solubility of Cur and increase the bioavailability of Cur.
【作者单位】： 东北林业大学森林植物生态学教育部重点实验室;
【基金】：中央高校基本科研业务费专项资金项目(2572014AB11) 国家自然科学基金资助项目(21473023)
【分类号】：R283.6
，
本文编号：2460252
[Abstract]:Objective to optimize the preparation of curcumin (Cur) nanoparticles freeze-dried powder (CNLP). Methods CNLP, was prepared with acetone as solvent, deionized water as anti-solvent, polysorbate-80 (P80) as surfactant and mannitol as freeze-drying protectant to prepare CNLP by anti-solvent method. The factors influencing the particle size of CNLP include the mass concentration of Cur, the volume ratio of solvent to antisolvent, the dosage of surfactant, the deposition time, the stirring rate and the dosage of freeze-dried protectant, and the saturated solubility and dissolution in vitro of the obtained CNLP are compared with that of the original powder. Results the optimum conditions for preparing CNLP were as follows: the mass concentration of Cur was 8mg/m / L, the ratio of solvent to antisolvent was 1? 5, the dosage of surfactant was 0.05%, the deposition time was 5 min, the stirring rate was 400r / min, and the mass ratio of mannitol to Cur was 4? The average particle size of CNLP was (172.2 卤4.6) nm;CNLP. The Zeta potential of complex solution was (- 19.7 卤3.7) m V;). The SEM pattern showed that the Cur powder was irregular and large, the particle size was about 20 渭 m, and the size of the raw powder was about 170 nm, which was smaller than that of the original powder. The size of the raw powder was about 20 渭 m, and the size of the powder was about 170 nm. According to the morphology of CNLP, the average particle size of CNLP measured by laser particle sizer is basically the same. The saturated solubility of CNLP in deionized water was 41.32 times that of original powder, the saturated solubility of CNLP in artificial gastric juice was 1.74 times higher than that of original powder, and the saturated solubility of CNLP in artificial intestinal fluid was 4.11 times of that of original powder. The dissolution rate of CNLP in deionized water was 14.51 times that of original powder, the dissolution rate of CNLP in artificial gastric juice was 2.33 times of that of original powder, and the dissolution rate of CNLP in artificial intestinal fluid was 44.79 times of that of original powder. Conclusion CNLP prepared by anti-solvent method can improve the water solubility of Cur and increase the bioavailability of Cur.
【作者单位】： 东北林业大学森林植物生态学教育部重点实验室;
【基金】：中央高校基本科研业务费专项资金项目(2572014AB11) 国家自然科学基金资助项目(21473023)
【分类号】：R283.6
，
本文编号：2460252
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