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无载油和载油液晶颗粒的特性由带负电荷的稳定剂柠檬酸三乙酯稳定。

Characterization of oil-free and oil-loaded liquid-crystalline particles stabilized by negatively charged stabilizer citrem.

机构信息

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.

出版信息

Langmuir. 2012 Aug 14;28(32):11755-66. doi: 10.1021/la3021244. Epub 2012 Aug 3.

Abstract

The present study was designed to evaluate the effect of the negatively charged food-grade emulsifier citrem on the internal nanostructures of oil-free and oil-loaded aqueous dispersions of phytantriol (PHYT) and glyceryl monooleate (GMO). To our knowledge, this is the first report in the literature on the utilization of this charged stabilizing agent in the formation of aqueous dispersions consisting of well-ordered interiors (either inverted-type hexagonal (H(2)) phases or inverted-type microemulsion systems). Synchrotron small-angle X-ray scattering (SAXS) and cryogenic transmission electron microscopy (cryo-TEM) were used to characterize the dispersed and the corresponding nondispersed phases of inverted-type nonlamellar liquid-crystalline phases and microemulsions. The results suggest a transition between different internal nanostructures of the aqueous dispersions after the addition of the stabilizer. In addition to the main function of citrem as a stabilizer that adheres to the surface of the dispersed particles, it has a significant impact on the internal nanostructures, which is governed by the following factors: (1) its penetration between the hydrophobic tails of the lipid molecules and (2) its degree of incorporation into the lipid-water interfacial area. In the presence of citrem, the formation of aqueous dispersions with functionalized hydrophilic domains by the enlargement of the hydrophilic nanochannels of the internal H(2) phase in hexosomes and the hydrophilic core of the L(2) phase in emulsified microemulsions (EMEs) could be particularly attractive for solubilizing and controlling the release of positively charged drugs.

摘要

本研究旨在评估带负电荷的食品级乳化剂柠檬酸酯(citrem)对植醇(PHYT)和甘油单油酸酯(GMO)无油和含油水性分散体内部纳米结构的影响。据我们所知,这是文献中首次报道在由有序内部(反相六方(H(2))相或反相微乳液体系)组成的水性分散体形成中利用这种带电稳定剂。同步加速器小角 X 射线散射(SAXS)和低温透射电子显微镜(cryo-TEM)用于表征反相非层状液晶相和微乳液的分散相和相应的未分散相。结果表明,在加入稳定剂后,水性分散体的内部纳米结构发生转变。除了 citrem 作为粘附在分散颗粒表面上的稳定剂的主要功能外,它还对内部纳米结构有重大影响,这受以下因素控制:(1)其在脂质分子疏水尾部之间的渗透;和(2)其进入脂质-水界面区域的程度。在 citrem 的存在下,通过扩大六方囊体内部 H(2)相的亲水性纳米通道和乳化微乳液(EME)中亲水性核心,可以形成具有功能化亲水区的水性分散体,这对于溶解和控制带正电荷的药物的释放可能特别有吸引力。

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