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植物素是否是抗氧化芦丁的优越纳米递药系统?

Are phytosomes a superior nanodelivery system for the antioxidant rutin?

机构信息

School of Pharmacy, University of Otago, Dunedin, New Zealand.

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

出版信息

Int J Pharm. 2018 Sep 5;548(1):82-91. doi: 10.1016/j.ijpharm.2018.06.042. Epub 2018 Jun 19.

Abstract

Rutin, a strong antioxidant, has been implicated in the prevention of liver inflammation. However, low solubility and permeability through the gut wall limit development of rutin as a therapeutic agent for oral administration. Phytosomes are described as lipid nanocarriers with a complexation between the phospholipid headgroups and entrapped phytochemicals. The aim of this research was to compare the structure of rutin liposomes to rutin phytosomes. FT-IR, DSC and NMR were employed to investigate the presence of any molecular interactions between the formulation components. The FT-IR spectra showed that a new -OH bond had formed in the rutin phytosomes, suggesting the formation of a molecular complex. P NMR experiments revealed that the DPPC molecule is altered when formulated as liposomes but that these changes were greater for samples from the phytosome formulation. DSC data revealed that when rutin was added to DPPC there was a significant shift in the transition temperature of DPPC. Further, the shift was greater in the THF solvent used to produce phytosomes compared to CHCl used to produce liposomes. H NMR spectra of the phytosome samples indicated three additional peaks that were greater than in the liposome formulation. ROESY NMR spectra provided evidence supporting the interaction between rutin and DPPC in both liposomes and phytosomes. The apparent differences in molecular interaction between liposomes and phytosomes did not however impact rutin release in biorelevant media or during in vitro small intestinal lipolysis.

摘要

芦丁是一种强抗氧化剂,已被证实可预防肝脏炎症。然而,其在肠道壁中的低溶解度和通透性限制了其作为口服治疗剂的发展。植物生化素被描述为磷脂头部基团与包封的植物化学物质之间形成复合物的脂质纳米载体。本研究旨在比较芦丁脂质体和芦丁植物生化素的结构。傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)和核磁共振(NMR)用于研究配方成分之间是否存在任何分子相互作用。FT-IR 光谱表明,芦丁植物生化素中形成了新的-OH 键,表明形成了分子复合物。31P NMR 实验表明,当 DPPC 被配方制成脂质体时,DPPC 分子会发生变化,但这种变化在植物生化素配方的样品中更大。DSC 数据显示,当芦丁添加到 DPPC 中时,DPPC 的相变温度有明显的偏移。此外,在用于制备植物生化素的 THF 溶剂中,偏移大于用于制备脂质体的 CHCl3。植物生化素样品的 1H NMR 谱表明,有三个额外的峰大于脂质体配方。ROESY NMR 谱提供了证据支持芦丁与 DPPC 之间在脂质体和植物生化素中的相互作用。然而,脂质体和植物生化素之间分子相互作用的明显差异并未影响生物相关介质中的芦丁释放或体外小肠脂肪酶解过程中的释放。

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