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

作　　者：赖志昆 胡晓贞[1] 翁嘉灏[1] 冯其茂[1] 张晓嫣 LAI Zhi-kun;HU Xiao-zhen;WENG Jia-hao;FENG Qi-mao;ZHANG Xiao-yan(Department of Cardiology,Shanghai Hospital of Chinese Medicine,Shanghai,200071;Department of Internal Medicine,Tianshan Chinese Medicine Hospital,Changning District,Shanghai,200051)

机构地区：[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

出　　处：《中国中西医结合杂志》2024年第2期216-221,共6页Chinese Journal of Integrated Traditional and Western Medicine

基　　金：上海市卫生健康委员会项目(No.20204Y0260);上海市科学技术委员会项目(No.21Y11920700);国家自然科学青年基金资助项目(No.82104758)。

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。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 

分 类 号：R283.6[医药卫生—中药学]