摘要
目的采用Box-Behnken效应面法筛选壳聚糖/海藻酸钠自组装制备葛根素纳米粒(Pur-NPs)的最优处方。方法采用自组装法制备葛根素壳聚糖/海藻酸钠纳米粒(Pur-CS/SA-NPs),以壳聚糖质量浓度、壳聚糖pH值、海藻酸钠质量浓度、搅拌速度、搅拌时间、超声功率、投药量为考察因素,以包封率、载药量、粒径、多分散指数(PDI)为评价指标,进行单因素考察,利用Box-Behnken效应面设计法筛选最优处方,将最优处方进行表征及体外释放实验。结果得到优化后自组装法最优的处方为壳聚糖质量浓度0.45 mg/mL,海藻酸钠质量浓度为0.07 mg/mL,壳聚糖pH值4.33,转速316.49 r/min。为了实验操作方便,将最优处方定为壳聚糖质量浓度0.45 mg/mL,海藻酸钠质量浓度为0.07 mg/mL,壳聚糖pH值为4.3,转速300r/min,平行3次实验进行验证,所得纳米粒包封率(89.056±1.680)%、载药量(44.528±0.840)%、平均粒径(208.327±1.870)nm、PDI 0.131±0.006。经过表征,纳米粒形态完好,由体外释放实验可知,纳米粒经过拟合所符合的方程为Higuchi模型,且在释放过程中无突释现象,表明纳米粒在体外释放良好。结论采用Box-Behnken效应面法优化了Pur-CS/SA-NPs的处方,以平均粒径、PDI、包封率、载药量为指标评价该模型,且经过表征及体外释放实验,表明该模型预测性良好。
Objective To screen the optimal formulation of puerarin nanoparticles(Pur-NPs)by self-assembly of chitosan/alginate by Box-Behnken response surface method.Methods Puerarin chitosan/sodium alginate nanoparticles(Pur-CS/SA-NPs)were prepared by self-assembly method.Taking chitosan concentration,chitosan pH,sodium alginate concentration,stirring speed,stirring time,ultrasonic power,and dosage as investigation factors,the encapsulation rate,drug loading,particle size,and polydispersity index(PDI)were used as evaluation index to investigate the optimal prescriptions using the Box-Behnken response surface design method,and the optimal formulation was characterized and released in in vitro experiments.Results The optimal formulation from the optimized self-assembly method was as following:chitosan concentration of 0.45 mg/mL,sodium alginate concentration of 0.07 mg/mL,chitosan pH of 4.33,and rotation speed of 316.49 r/min.For the convenience of experimental operation,the most optimal prescription was determined to be chitosan concentration of 0.45 mg/mL,sodium alginate concentration of 0.07 mg/mL,chitosan pH of 4.3,and rotation speed of 300 r/min.The results were verified by three parallel experiments,and the encapsulation efficiency,drug loading,average particle diameter,and PDI of obtained nanoparticles were(89.056±1.680)%,(44.528±0.840)%,(208.327±1.870)nm and 0.131±0.006,respectively.After characterization,the morphology of the nanoparticles was intact.It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles was Higuchi model,and there was no burst release during the release process,indicating that the nanoparticles were released well in vitro.Conclusion The prescription of puerarin chitosan/sodium alginate nanoparticles was optimized by Box-Behnken response surface method.The model was evaluated by average particle size,PDI,encapsulation efficiency and drug loading,and the characterization results and in vitro release test showed that the model had good predictability.
作者
颜洁
关志宇
朱卫丰
钟凌云
吴文婷
邹斌
李娜
陈鸿
YAN Jie;GUAN Zhi-yu;ZHU Wei-feng;ZHONG Ling-yun;WU Wen-ting;ZOU Bin;LI Na;CHEN Hong(School of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China)
出处
《中草药》
CAS
CSCD
北大核心
2019年第23期5706-5713,共8页
Chinese Traditional and Herbal Drugs
基金
国家重点研发计划中医药现代化研究重点专项（2017YFC1702904）
江西省教育厅科技计划项目（GJJ170718）
江西省2018年度研究生创新专项（YC2018-S287、YC2018-S285）
中药学一流学科科研项目（JXSYLXK-ZHYAO049）
