超临界流体强化溶液快速分散技术制备三七皂苷脂质体性质研究
Properties Study of Panax Notoginseng Saponins Liposome Prepared by Solution Enhanced Dispersion by Supercritical Fluid
赖志昆 1胡晓贞 1翁嘉灏 1冯其茂 1张晓嫣2
作者信息
- 1. 上海市中医医院心病科(上海 200071)
- 2. 上海市长宁区天山中医医院内科(上海 200051)
- 折叠
摘要
目的 观察超临界流体强化溶液快速分散技术(SEDS)制备三七皂苷脂质体(PNS-Lip)的药剂学特征,并与常规脂质体制备方法进行比较.方法 采用超临界流体强化溶液快速分散技术(SEDS)、薄膜分散法(TFD)、逆向蒸发法(RPE)制备PNS-Lip.透射电镜观察不同PNS-Lip外观形态;检测粒径与电位;超滤法测定包封率(EE)和载药量(DL);以药物泄漏率(LR)评价制剂稳定性;进行体外溶出实验检测.结果 不同制备方法制得的PNS-Lip呈现出淡蓝色乳光,表面光滑,形态圆整,具有双层膜结构.与PNS-Lip-RPE比较,PNS-Lip-TFD及PNS-Lip-SEDS粒径、多分散系数(PDI)、Zeta电位降低,60、120、180、240、300、360 s LR 降低,EE 和 DL 升高(P＜0.05,P＜0.01);PNS-Lip-SEDS 在420s LR 降低(P＜0.05).与 PNS-Lip-TFD 比较,PNS-Lip-SEDS 的粒径、PDI 及 Zeta 电位降低,180、240、300、360、420 s LR 降低,EE 和 DL 升高(P＜0.05,P＜0.01).PNS-Lip-RPE 及 PNS-Lip-TFD在初始阶段存在突释作用,随后持续缓慢释放;PNS-Lip-SEDS未发生突释现象,缓释作用更加明显,在48 h后达到溶解平衡.结论 SEDS作为新型的制粒技术,与常规的脂质体制备方法相比具有一定的优势,该技术在纳米给药系统领域具有广阔的应用前景.
Abstract
Objective To observe the pharmaceutical characteristics of Panax notoginseng saponins liposome(PNS-Lip)prepared by solution enhanced dispersion by supercritical fluid(SEDS),and compare with conventional liposome preparation methods.Methods PNS-Lip was prepared by SEDS,thin-film dispersion method(TFD)and reversed-phase evaporation method(RPE).The appearance and morphology of different PNS-Lip were observed by transmission electron microscope;The particle size and potential of PNS-Lip were detected.The encapsulation rate(EE)and drug load(DL)were determined by ultrafiltration method.Leakage rate(LR)was used to evaluate the stability of the preparation.The dissolution test was performed in vitro.Results The PNS-Lip prepared by different preparation methods showed light blue opalescence,smooth surface,round shape and double-layer film structure.Compared with PNS-Lip-RPE,the particle size,polydispersity index(PDI)and Zeta potential of PNS-Lip-TFD and PNS-Lip-SEDS significantly decreased,and the LR at 60,120,180,240,300 and 360 s also significantly decreased,the EE and DL significantly increased(P＜0.05,P＜0.01).In addition,the DR of PNS-Lip-SEDS significantly decreased in 420 s(P＜0.05).Compared with PNS-Lip-TFD,the particle size,PDI and Zeta potential of PNS-Lip-SEDS significantly decreased,and LR also significantly decreased at 180,240,300,360 and 420 s,while EE and DL increased(P＜0.05,P＜0.01).PNS-Lip-RPE and PNS-Lip-TFD had sudden release in the initial stage,and then continued to release slowly.However,there was no sudden release of PNS-Lip-SEDS with a more obvious sustained release effect which reached dissolution equilibrium after 48 h.Conclusion As a new granulating technology,SEDS has certain advantages compared with the conventional liposome preparation method,and it has broad application prospects in the field of nano-drug delivery system.
关键词
三七皂苷/脂质体/超临界流体强化溶液快速分散技术/体外溶出/中药单体Key words
Panax notoginseng saponins/liposome/solution enhanced dispersion by supercritical fluid/in vitro dissolution/Chinese medicine monomers引用本文复制引用
基金项目
上海市卫生健康委员会项目(20204Y0260)
上海市科学技术委员会项目(21Y11920700)
国家自然科学青年基金资助项目(82104758)
出版年
2024
国家科技期刊平台
NSTL
万方数据