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在水相环境中从十六烷酸十六酯/辛酸三甘油酯/聚山梨酯 80 混合物中系统地表征纳米结构脂质载体。

Systematic Characterization of Nanostructured Lipid Carriers from Cetyl Palmitate/Caprylic Triglyceride/Tween 80 Mixtures in an Aqueous Environment.

机构信息

Division of Chemical Engineering, Graduate School of Engineering Science, Osaka University, 1-3 Machikaneyamacho, Toyonaka 560-8531, Osaka, Japan.

Bioprocess Engineering Study Program, Faculty of Agricultural Technology, Universitas Brawijaya, Jalan Veteran, Malang 65145 East Java, Indonesia.

出版信息

Langmuir. 2021 Apr 13;37(14):4284-4293. doi: 10.1021/acs.langmuir.1c00270. Epub 2021 Apr 2.

Abstract

Nanostructured lipid carriers (NLCs) are gaining attention as the new generation of lipid vehicles. These carriers consist of saturated lipids with small drops of liquid oil dispersed into the inner lipid matrix and are stabilized by a surfactant. Conventionally, NLC-based drug delivery systems have been widely studied, and many researchers are looking into the composition of NLC properties to improve the performance of NLCs. The membrane fluidity and polarity of self-assembling lipids are also essential properties that must be affected by membrane compositions; however, such fundamental characteristics have not been studied yet. In this study, NLCs were prepared from cetyl palmitate (CP), caprylic triglyceride (CaTG), and Tween 80 (T80). Structural properties, such as particle size and ζ-potential of the CP/CaTG/T80 ternary mixtures, were investigated. Then, the systematic characterization of self-assembly properties using fluorescence-based analysis was applied for the first time to the NLC system. As a final step, the ternary diagram was developed based on the self-assembly properties to summarize the possible structures formed at different compositions. The results showed four states: micelle-like, oil-in-water (O/W) emulsion-like, solid lipid nanoparticle-like, and intermediate (solid-liquid coexistence). For the purpose of making the lipid matrix more liquified, the heterogeneous state and the disordered state of the O/W emulsion-like structure might fulfill the criteria of NLCs. Finally, the ternary diagram provides new information about the assembly state of NLC constituents that could become an important reference for developing high-performance NLCs.

摘要

纳米结构脂质载体(NLC)作为新一代脂质载体备受关注。这些载体由饱和脂质组成,小液滴状的液态油分散在内部脂质基质中,并由表面活性剂稳定。传统上,基于 NLC 的药物传递系统已经得到了广泛的研究,许多研究人员正在研究 NLC 特性的组成,以提高 NLC 的性能。自组装脂质的膜流动性和极性也是必须受膜组成影响的重要性质;然而,这些基本特性尚未得到研究。在这项研究中,NLC 是由十六烷酸肉豆蔻酯(CP)、辛酸三甘油酯(CaTG)和吐温 80(T80)制备的。研究了 CP/CaTG/T80 三元混合物的结构性质,如粒径和 ζ-电位。然后,首次应用基于荧光的分析方法对自组装性质进行系统表征,应用于 NLC 系统。最后,根据自组装性质开发了三元相图,以总结不同组成下可能形成的结构。结果表明存在四种状态:胶束状、油包水乳状(O/W)、固体脂质纳米颗粒状和中间态(固液共存)。为了使脂质基质更加液化,O/W 乳状结构的非均相状态和无序状态可能符合 NLC 的标准。最后,三元相图提供了有关 NLC 成分组装状态的新信息,这可能成为开发高性能 NLC 的重要参考。

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