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达那唑-酪蛋白酸钠复合纳米粒的制备及其形成机制研究
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| 篇名： | 达那唑-酪蛋白酸钠复合纳米粒的制备及其形成机制研究 |
| TITLE： | Study on preparation and formation mechanism of danazol-sodium caseinate composite nanoparticles |
| 摘要： | 目的 制备并表征达那唑（DAZ）-酪蛋白酸钠（SC）复合纳米粒，探讨“自下而上（bottom-up）”工艺中纳米粒形成的机制。方法以SC作为调控纳米粒的稳定剂，通过反溶剂沉淀法制备DAZ-SC复合纳米粒，对其粒径、Zeta电位、微观形态、稳定性、包封率、载药量、体外溶出度等进行表征，进一步利用荧光光谱、红外光谱和在线粒子监测等方法分析DAZ与SC的相互作用机制。结果DAZ-SC复合纳米粒的粒径为（223.7±12.5）nm，多分散性指数为0.274±0.012，Zeta电位为－（17.81±1.63）mV（n＝3）；纳米混悬液的稳定性良好，DAZ的固态性质明显改善，溶出度显著提高。SC在DAZ的作用下发生静态淬灭，二级结构有所改变；在SC的作用下，DAZ的结晶过程得到控制；DAZ与SC之间的相互作用主要为氢键和范德华力。结论本研究成功制备了DAZ-SC复合纳米粒；在“bottom-up”工艺中，因SC与DAZ之间氢键和范德华力引起的相互作用抑制了药物晶体的生长与团聚。 |
| ABSTRACT： | OBJECT IVE To prepar e and characterize danazol （DAZ）-sodium caseinate （SC）composite nanoparticles ，and to study the mechanism of preparing nanoparticles in “bottom-up”technology. METHODS SC was used as a stabilizer for regulating nanoparticles，so that DAZ-SC composite nanoparticles were prepared by anti-solvent precipitation method. The particle size ， Zeta-potential，micro-morphology，stability，encapsulation efficiency ，drug loading and in vitro dissolution rate were characterized. Fluorescence spectra ，IR spectra ，FBRM and other methods were used to analyze the interaction mechanism between DAZ and SC. RESULTS The particle size of DAZ-SC composite nanoparticles was （223.7±12.5）nm，and the polydispersity index was 0.274± 0.012. Zeta-potential was －（17.81±1.63）mV（n＝3）. The stability of nano-suspension was good ，the solid properties of DAZ were greatly improved ，and the dissolution rate was significantly increased. SC was statically quenched under the action of DAZ and the secondary structures of SC were changed. The crystallization process of DAZ was controlled under the action of SC ，and the interaction between DAZ and SC was mainly hydrogen bond and van der Waals force. CONCLUSIONS In this study ，DAZ-SC composite nanoparticles are successfully prepared. In the “bottom-up”technology，the interaction between SC and DAZ caused by hydrogen bond and van der Waals force inhibits the growth and agglomeration of drug crystals . |
| 期刊： | 2022年第33卷第10期 |
| 作者： | 李佳雯，曹文峰，徐浩，冯予涵，冷钰婷，景秋芳，任福正 |
| AUTHORS： | LI Jiawen ，CAO Wenfeng ，XU Hao，FENG Yuhan ，LENG Yuting ，JING Qiufang ，REN Fuzheng |
| 关键字： | 达那唑；酪蛋白酸钠；稳定剂；形成机制；纳米粒 |
| KEYWORDS： | danazol；sodium caseina te；stabilizer；formation mechanism ；nanoparticles |
| 阅读数： | 248 次 |
| 本月下载数： | 5 次 |
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