艳山姜挥发油纳米乳的制备及其体内分布情况考察  

Preparation and in vivo Distribution of Essential Oil from Alpinia zerumbet Fructus Encapsulated Nanoemulsions

作　　者：徐金转 张莉莉 周正莉 徐珊 周翔 黄磊 巩仔鹏 陈艺 沈祥春 XU Jinzhuan;ZHANG Lili;ZHOU Zhengli;XU Shan;ZHOU Xiang;HUANG Lei;GONG Zipeng;CHEN Yi;SHEN Xiangchun(Guizhou Provincial Engineering Center for Efficient Utilization of Natural Pharmaceutical Resources,Key Laboratory of Optimal Utilization of Natural Medicinal Resources,Guizhou Provincial Key Laboratory of Pharmaceutics,School of Pharmaceutical Sciences,Guizhou Medical University,Guiyang 550025,China)

机构地区：[1]贵州医科大学药学院,贵州省天然药物资源高效利用工程中心,天然药物资源优效利用重点实验室,贵州省药物制剂重点实验室,贵阳550025

出　　处：《中国实验方剂学杂志》2024年第5期126-133,共8页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(82104537,82260827);中央引导地方基金项目(黔科合中引地[2023]003);贵州省教育厅自然科学研究项目(黔教技[2023]066号);贵州省高层次创新型人才项目(黔科合平台人才-GCC[2023]048);国家大学生创新创业训练计划项目(S202210660140);贵州省优秀青年科技人才项目(黔科合平台人才[2021]5632号)。

摘　　要：目的:制备包载艳山姜挥发油(EOFAZ)的口服纳米乳,考察其体外促吸收效果和体内分布情况。方法:将醋柴胡多糖(VBCP)和牛血清白蛋白(BSA)通过Maillard反应进行偶联,制备多糖-蛋白偶联物VBCP-BSA。以VBCP-BSA为乳化剂,维生素B12(VB_(12))为吸收促进剂,中链甘油三酯与EOFAZ混合作为油相,通过高能外力乳化法制备负载EOFAZ的纳米乳,对该纳米乳的粒径及粒径分布、表面Zeta电位、EOFAZ含量、外观形态等进行表征,并利用荧光素示踪法考察荧光素标记的EOFAZ纳米乳在体外的吸收效果及体内的分布情况。结果:VBCP与BSA通过Maillard反应48 h后形成偶联物VBCP-BSA,并具有较高的接枝度。以VBCP-BSA为乳化剂,制备得到均一的粉色纳米乳液EOFAZ@VBCP-BSA/VB_(12)。该纳米乳的粒径<100 nm,粒径分布均匀,表面弱负电荷,呈圆球形,对EOFAZ的包封率>80%,其具有良好的体外吸收效果,口服后能增强肝脏蓄积。结论:设计的蛋白多糖纳米乳能够有效负载EOFAZ,促进口服吸收,增强肝脏分布,可为口服EOFAZ保肝制剂的开发提供实验依据。Objective:To prepare oral nanoemulsions encapsulating essential oil from Alpinia zerumbet fructus(EOFAZ)and to investigate its pro-absorption effect in vitro and distribution in vivo.Method:The proteoglycan conjugate polysaccharides of vinegar-processed Bupleuri Radix-bovine serum albumin(VBCPBSA)was prepared by Maillard reaction of VBCP and BSA.Taking VBCP-BSA as emulsifier,vitamin B_(12)(VB_(12))as absorption enhancer,and medium chain triglycerides mixed with EOFAZ as oil phase,the nanoemulsions loaded with EOFAZ was prepared by high energy emulsification method.The particle size,particle size distribution,surface Zeta potential,EOFAZ content and appearance and morphology of the nanoemulsions were characterized,and fluorescein tracer method was used to investigate the absorption effect of fluorescein-labeled EOFAZ nanoemulsions in vitro and their distribution in vivo.Result:VBCP-BSA was formed by Maillard reaction for 48 h with high grafting rate.Using VBCP-BSA as emulsifier,the homogeneous pink nanoemulsions was prepared and denoted as EOFAZ@VBCP-BSA/VB_(12).The particle size of the nanoemulsions was less than 100 nm and the particle size distribution was uniform.The surface of the nanoemulsions was a weak negative charge,and the shape was spherical.The encapsulation rate of the nanoemulsions for EOFAZ was greater than 80%,which had a good absorption effect in vitro and could enhance liver accumulation after oral administration.Conclusion:The designed proteoglycan nanoemulsions can effectively load EOFAZ,promote oral absorption and enhance liver distribution,which can provide experimental basis for the development of oral EOFAZ liver protection preparations.

关 键 词：纳米乳 多糖-蛋白偶联物 维生素B_(12)(VB_(12)) 艳山姜挥发油(EOFAZ) 口服制剂 体内分布 肝靶向 

分 类 号：R22[医药卫生—中医基础理论] R28[医药卫生—中医学] R943R969.1