摘要
环糊精和油自组装形成的beads是一种新型的药物递送系统,在油类药物固体化、改善脂溶性药物生物利用度方面具有较强的应用潜力,但beads的形成机制仍不完善。本研究利用同步辐射X射线显微成像技术,测定beads的三维结构,基于对干燥前后beads结构的定量分析,发现beads形成过程中Pickering乳滴的有序性。在添加脂溶性成分后,油相的表面张力改变,对beads的结构会产生影响。因此,在载脂溶性维生素K1的过程中beads的三维结构会发生改变,但依然可见beads形成过程中Pickering乳滴的有序性。本研究从beads内部三维结构出发,揭示了环糊精半包合形成Pickering乳滴,再有序聚集、组装形成beads的微观过程,完善了beads的形成机制,为beads的进一步研究提供了结构学基础。
Beads, a novel drug delivery system self-assembled by cyclodextrins （CDs） and oil, has potential applications in the solidification of oil drugs and improving the bioavailability of lipid-soluble drugs. However, very few researches were dedicated to the mechanism of beads formation. In this study, three-dimensional structures of beads were visualized and investigated using synchrotron radiation X-ray microcomputed tomography （SR-μCT）. The structural changes of beads attributed by drying process were analyzed and confirmed via visualization results of SR-μCT. Productively, it was proposed that Pickering emulsion droplets obtained during beads formation process were spatially localized orderly. Moreover, the effects of loading lipid soluble drug, namely, vitamin K1, on the structural changes of beads were also analyzed. It is well known that the surface tension of oil phase could be changed by the addition of lipid soluble constituents. It was reasonable that the three-dimensional structure of beads might be altered during the drug loading of vitamin K1 into the beads. However, although the morphologies of beads were changed to some extent, the ordered Pickering emulsion droplets during the process of beads formation was successfully illustrated based on the SR-μCT results. Conclusively, according to the three-dimensional structural analysis of the beads, this study revealed the organized architecture for Pickering emulsion droplet assembly and beads formation in cyclodextrin semi-inclusion complex, which significantly complements the formation mechanism of beads, and provides a structural basis for the further study of beads.
出处
《药学学报》
CAS
CSCD
北大核心
2018年第2期291-303,共13页
Acta Pharmaceutica Sinica
基金
国家科技重大专项资助项目(2017zx09101-001)
中国博士后科学基金资助项目(2017M610284)
