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苦豆子总碱二元醇脂质体制备及体外透皮特性研究

Preparation and in Vitro Transdermal Properties of Sophora Alopecuroides Total Alkaloid Diol Liposome
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摘要 目的在制备苦豆子总碱脂质体的过程中,加入两种水相混溶渗透促进剂:乙醇和丙二醇,以获得新的、稳定的透皮给药系统,增强苦豆子总碱(SATA)的皮肤传递。方法注入法制备二元醇脂质体,并对其形态,大小,Zeta电位进行表征,包封率、囊泡稳定性和皮肤渗透特性为优化乙醇和丙二醇配比的重要考察因素,采用Franz扩散池对小鼠皮肤进行体外皮肤渗透实验,比较小鼠皮肤的累积渗透量。用激光共聚焦扫描电镜观察含有荧光素罗丹明B的苦豆子总碱二元醇脂质体在离体小鼠皮肤中的穿透深度及荧光强度。结果当乙醇∶丙二醇=7∶3(w/w)时,二元醇脂质体的稳定性最好、包封率最高(89.13±0.42)%,粒径最小(103.00±16.15)nm,透皮深度(170μm)最大和最强的荧光强度(Max FI=160 AU)。结论制备的苦豆子总碱二元醇脂质体(乙醇∶丙二醇=7∶3,w/w)是一种高效且稳定的经皮传递载体。 Objective In the process of preparing Sophora alopecuroides total alkaloids liposomes,two water-soluble permeation enhancers,ethanol and propylene glycol,were added to obtain a new and stable transdermal delivery system,enhancing the skin transmission of Sophora alopecuroides total alkaloids(SATA).Methods Injecting method was used to prepare diol liposomes,and their morphology,size,and Zeta potential were characterized.The encapsulation efficiency,vesicle stability,and skin permeation characteristics were important factors for optimizing the ratio of ethanol and propylene glycol.In vitro skin permeation experiments were conducted on mouse skin using Franz diffusion cell to compare the cumulative permeation amount of mouse skin.The penetration depth and fluorescence intensity of sophora alopecuroides total alkaloid diols liposomes containing fluorescein rhodamine B in isolated mouse skin were observed by laser confocal scanning electron microscopy.Results The results showed that when ethanol:propylene glycol=7∶3(w/w),the stability of diol liposomes was the best,the encapsulation efficiency was the highest(89.13±0.42)%,the particle size was the smallest(103.00±16.15)nm,and the transdermal depth was(170μm).Maximum and strongest fluorescence intensity(MaxFI=160 AU).Conclusion The prepared bitter bean seed total alkaloid diol liposome(ethanol:propylene glycol=7∶3,w/w)is an efficient and stable transdermal delivery carrier.
作者 王慧 邵青 张燕 王文杰 杨苗苗 胡婕雯 张玲 WANG Hui;SHAO Qing;ZHANG Yan;WANG Wenjie;YANG Miaomiao;HU Jiewen;ZHANG Ling(Xi'an Mental Health Center,Xi'an 710061,China;Xi'an Jiaotong University Affiliated Red Society Hospital,Xi'an 710000,China)
出处 《陕西中医药大学学报》 2023年第3期71-75,共5页 Journal of Shaanxi University of Chinese Medicine
基金 国家自然科学基金项目(81202938) 西安市科学技术局重点实验室(201805051ZD2CG35)。
关键词 苦豆子总碱(SATA) 二元醇脂质体 乙醇 丙二醇 经皮传递载体 共聚焦激光扫描电镜 Total alkaloids of Sophora alopecuroides(SATA) Diol liposomes Ethanol Propylene glycol Transdermal delivery carrier Confocal laser scanning electron microscopy
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