麦角甾苷固体脂质纳米粒处方筛选和理化性质研究

Research on prescription screening of Acteoside solid lipid nanoparticles

目的研究不同种类药用辅料成分对麦角甾苷固体脂质纳米粒(SLN)理化性质的影响,为研究SLN的处方筛选提供依据。方法采用乳化-固化法制备麦角甾苷-SLN,单一变量法考察山嵛酸甘油酯(Compritol ATO 888)、单硬脂酸甘油酯、大豆卵磷脂、Myrj52等辅料对麦角甾苷-SLN粒径、包封率、表征分散度(PDI)等理化性质的影响,采用透射电镜法观察麦角甾苷-SLN的形态,X-射线衍射(XRD)分析其药物晶体结构。结果随Compritol ATO 888用量增加,麦角甾苷-SLN粒径不断减小,包封率逐渐减小,PDI逐渐增加;随单硬脂酸甘油酯的用量增加,粒径明显增大,包封率略有降低,PDI减小;随卵磷脂用量增加,粒径明显增大,包封率降低,PDI减小;随Myrj52用量明显增加,粒径减小,包封率增加,PDI增大;麦角甾苷-SLN外观圆整,呈球形;麦角甾苷以分子分散状态被包裹在SLN中。结论不同辅料对麦角甾苷-SLN的理化性质均产生一定影响趋势,为制备SLN的处方筛选研究提供启示与思路。

Objective To explore the impacts of different excipients on physical and chemical properties of Acteoside solid lipidnanoparticles （Acteoside-SLN）, and make experimental evidence for the study of prescription SLN. Methods Emulsification-evaporation was appropriate for the preparation of Acteoside-SLN. Single variable method was used for fumbling the effects ofCompritol 888 ATO, glyceryl monostearate, soy lecithin, Myrj52 and other accessories on the physicochemical propertiesincluding nanoparticles particle size, encapsulation efficiency and characterization dispersity （PDI） of Acteoside-SLN.Transmission electron microscope was used to observe the morphology of Acteoside-SLN and the structure of Acteoside in SLNwas measured by XRD. Results With the increasing of the amount of Compritol 888 ATO, the particle size of nanoparticlesdecreased significantly, encapsulation efficiency decreased slightly, PDI increased; With the increasing of amount of glycerolmonostearate, particle size increased obviously, encapsulation efficiency decreased slightly, and PDI decreased; With theincreasing of the amount of lecithin, particles size increased significantly, encapsulation efficiency decreased, and PDI decreased;With the increasing of Myrj52 amount, the nanoparticles particle size decreased, encapsulation rate and PDI increased slightly.The appearance of Acteoside-SLN was presented uniform spherically. Acteoside was wrapped in SLN in a molecular dispersionstate. Conclusion Various additives have a greater impact on physicochemical properties of Acteoside-SLN, and inspiration forprescription screening of SLN is supplied by this study.