摘要
目的考察复方葡配甘露聚糖水凝胶(专利号:ZL202010787982.9)处方中蛇床子挥发油纳米粒(Cnidii Fructus volatile oil nano-particulates,CVOP)在双骨架复合凝胶基质中的稳定性,以及CVOP对处方中积雪草总苷透黏膜吸收的影响。方法通过冷冻电子显微镜(cryo-electron microsocopy,Cryo-EM)、扫描电子显微镜(SEM)、透射电子显微镜(TEM)对凝胶基质结构以及其中的CVOP进行观察,以CVOP的外观形态、粒径为评价指标,结合GS-MS法,以CVOP的组成成分谱图及含量变化为判断依据,评价CVOP的稳定性;采用体外透黏膜试验考察CVOP对处方中积雪草总苷透阴道黏膜吸收的影响。结果蛇床子挥发油(Cnidii Fructus volatile oil,CO)在双骨架复合凝胶基质中能够形成圆整的球形粒子结构,平均粒径为(185±26)nm;CVOP在凝胶基质中稳定性良好,6个月加速试验后其形态结构、粒径与组成成分基本不变;CVOP对大鼠阴道黏膜不产生刺激性;在不含CVOP的空白水凝胶(B)中,积雪草苷(asiaticoside,AS)和羟基积雪草苷(madecassoside,MAS)的黏膜渗透性始终低于含有CVOP的水凝胶(A)组;在6.0 h时,水凝胶A中AS和MAS的累积渗透量分别是水凝胶B中AS和MAS的4.68倍与2.01倍,表明CVOP能够提高水溶性积雪草总苷的阴道黏膜渗透性。结论CO在双骨架复合凝胶基质中能够形成稳定的球形纳米粒,并可提高积雪草总苷的黏膜渗透性而有利于发挥多成分间的协同治疗作用。
Objective To investigate the stability of Shechuangzi(Cnidii Fructus)volatile oil nano-particulates(CVOP)in the double skeleton composite hydrogel matrix and the effect of CVOP on the transmucosal absorption of Jixuecao Zonggan(Centella Total Glucosides)in the prescription of compound glucomannan hydrogel(ZL.202010787982.9).Methods The structure of the hydrogel matrix and the CVOP in the double skeleton composite hydrogel matrix were observed by cryo-electron microscopy(Cryo-EM),scanning electron microscope(SEM)and transmission electron microscope(TEM).The appearance and particle size of CVOP were used as evaluation indexes,and the stability of CVOP was evaluated by combining with the GS-MS method based on the spectrogram of the components and content change of CVOP.The effect of CVOP on the transvaginal mucosal absorption of Centella Total Glucosides in the prescription was investigated by in vitro transmucosal test.Results The Cnidii Fructus volatile oil(CO)could form a spherical nano-particulates with round appearance in the double skeleton composite hydrogel matrix,and the CVOP with an average size of(185±26)nm.The CVOP had good stability in the hydrogel matrix,and its morphology,particle size and composition were basically unchanged after six months of accelerated test,and it did not cause irritation to the rat vaginal mucosa.In the hydrogel without CVOP(B),the mucosal permeability of asiaticoside(AS)and madecassoside(MAS)was always lower than that of the hydrogel containing CVOP(A).At 6.0 h,the cumulative permeability of AS and MAS in hydrogel A was 4.68 times and 2.01 times of AS and MAS in hydrogel B,respectively.It was shown that CVOP could improve the vaginal mucosal permeability of water-soluble Centella Total Glucosides.Conclusion The CO could form stable spherical nano-particulates in the double skeleton composite hydrogel matrix,and the CVOP could exert synergistic therapeutic effects of the multi-components by promoting the mucosal permeability of Centella Total Glucosides.
作者
赵宁
王军栋
关丽
张育珍
付丽娜
李伟泽
杨黎彬
ZHAO Ning;WANG Jundong;GUAN Li;ZHANG Yuzhen;FU Lina;LI Weize;YANG Libin(Xi’an Medical University,Xi’an 710021,China;Yantai Food and Drug Testing Center,Yantai 264000,China)
出处
《中草药》
CAS
CSCD
北大核心
2024年第15期5061-5069,共9页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金项目(82004075)
陕西省教育厅项目(23JP154)
西安医学院科研能力提升计划项目(2022NLTS059)
西安医学院科研能力提升计划项目(2022NLTS062)
江苏省扬中市“江雁计划”产业领军人才项目([2021]26号)。
关键词
双骨架复合凝胶
蛇床子挥发油
纳米粒
积雪草总苷
黏膜渗透性
积雪草苷
羟基积雪草苷
double skeleton composite hydrogel
Cnidii Fructus volatile oil
nano-particulates
Centella Total Glucosides
mucosal permeability
asiaticoside
madecassoside
