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
徐金转,在读博士,从事中药民族药体内递送研究,E-mail:xujinzhuan_yx@163.com
陈艺,副教授,博士生导师,从事中药活性成分体内递送与口服给药制剂研究,E-mail:chenyi_19890319@126.com;
沈祥春,教授,博士生导师,从事心血管系统药物药理及中药民族药活性研究,E-mail:shenxiangchun@126.com
收稿:2023-06-12,
网络出版:2023-08-24,
纸质出版:2024-03-05
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徐金转,张莉莉,周正莉等.艳山姜挥发油纳米乳的制备及其体内分布情况考察[J].中国实验方剂学杂志,2024,30(05):126-133.
XU Jinzhuan,ZHANG Lili,ZHOU Zhengli,et al.Preparation and in vivo Distribution of Essential Oil from Alpinia zerumbet Fructus Encapsulated Nanoemulsions[J].Chinese Journal of Experimental Traditional Medical Formulae,2024,30(05):126-133.
徐金转,张莉莉,周正莉等.艳山姜挥发油纳米乳的制备及其体内分布情况考察[J].中国实验方剂学杂志,2024,30(05):126-133. DOI: 10.13422/j.cnki.syfjx.20231349.
XU Jinzhuan,ZHANG Lili,ZHOU Zhengli,et al.Preparation and in vivo Distribution of Essential Oil from Alpinia zerumbet Fructus Encapsulated Nanoemulsions[J].Chinese Journal of Experimental Traditional Medical Formulae,2024,30(05):126-133. DOI: 10.13422/j.cnki.syfjx.20231349.
目的
2
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
2
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B
12
(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
2
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
2
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
2
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
2
The proteoglycan conjugate polysaccharides of vinegar-processed Bupleuri Radix-bovine serum albumin(VBCP-BSA) 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
2
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
2
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.
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