尼达尼布纳米脂质体的制备及其表征研究  

Preparation and characterization of nintedanib nano-liposomes

作　　者：饶乐 郭梦雨 徐国纲[1] RAO Le;GUO Mengyu;XU Guogang(Department of Health Medicine,Second Medical Center,Chinese PLA General Hospital,Beijing 100853;Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety of Chinese Academy of Sciences,National Center for Nanoscience and Technology of China,Beijing 100190,China)

机构地区：[1]解放军总医院第二医学中心健康医学科,北京100853 [2]国家纳米科学中心,中国科学院纳米生物效应与安全性重点实验室,北京100190

出　　处：《陆军军医大学学报》2024年第14期1695-1700,F0003,共7页Journal of Army Medical University

基　　金：国家自然科学基金面上项目(82341089,82370083);国家自然科学基金青年项目(82200091)。

摘　　要：目的探讨4种不同方法制备尼达尼布脂质体的关键理化特性,筛选出尼达尼布脂质体的最佳制备方法。方法采用薄膜分散法、逆向蒸发法、乙醇注入法和改良版乙醇注入法制备尼达尼布脂质体;利用透析法测定尼达尼布脂质体的包封率,并进行粒径大小、分散性、表面电位和形貌表征,在室温放置7 d后评估其稳定性。结果薄膜分散法、逆向蒸发法、乙醇注入法和改良版乙醇注入法均制备了类圆形尼达尼布脂质体,粒径大小分别为(285.1±12.3)、(271.4±5.9)、(226.3±14.8)、(197.2±11.2)nm;包封率分别为(15.82±1.26)%、(16.71±1.35)%、(25.12±3.21)%和(32.5±3.61)%;与其他3种方法相比,改良版乙醇注入法制备尼达尼布脂质体粒径大小显著减小,包封率显著增加(P<0.05)。室温放置7 d后,薄膜分散法和逆向蒸发法粒径明显增大(P<0.01),乙醇注入法和改良版乙醇注入法粒径大小无明显差异(P>0.05)。结论改良版乙醇注入法制备的尼达尼布脂质体关键理化特性表现优异,可作为制备尼达尼布脂质体的优选方法。Objective To investigate the key physical and chemical properties of nintedanib liposomes prepared by 4 different methods in order to screen out the best preparation method of nintedanib liposomes.Methods Firstly,nintedanib liposomes were prepared by thin film dispersion,reverse evaporation,ethanol injection and modified ethanol injection,respectively.The entrapment efficiency of nintedanib liposomes was then determined by dialysis and characterized for particle size,dispersibility,surface potential,and morphology.Their stability was evaluated after being placed at room temperature for 7 d.Results Circular nintedanib liposomes were respectively prepared by thin film dispersion,reverse evaporation,ethanol injection and modified ethanol injection,with a particle size of(285.1±12.3),(271.4±5.9),(226.3±14.8)and(197.2±11.2)nm,an encapsulation rate of(15.82±1.26)%,(16.71±1.35)%,(25.12±3.21)%and(32.5±3.61)%,respectively.The nintedanib liposomes prepared by modified ethanol injection had significantly smallest particle size and highest encapsulation efficiency than the liposomes by the other 3 methods(P<0.05).In 7 d after being placed at room temperature,the particle sizes of the liposomes prepared by film dispersion and reverse evaporation were increased notably(P<0.01),but no such change was observed in the liposomes prepared by ethanol injection and modified ethanol injection(P>0.05).Conclusion Nintedanib liposomes prepared by modified ethanol injection have excellent key physical and chemical properties,and this method is an optical one for preparing nintedanib liposomes.

关 键 词：尼达尼布乙磺酸盐 脂质体 粒径大小 乙醇注入法 

分 类 号：R944[医药卫生—药剂学] R961[医药卫生—药学] R977.3