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固体脂质纳米粒的结构。

On the Structure of Solid Lipid Nanoparticles.

机构信息

Department of Physics, King's College London, London, WC2R 2LS, UK.

Pharmaceutical Biophysics Group, Institute of Pharmaceutical Science, King's College London, London, SW1 9NH, UK.

出版信息

Small. 2019 Nov;15(45):e1903156. doi: 10.1002/smll.201903156. Epub 2019 Sep 18.

Abstract

Solid lipid nanoparticles (SLNs) have a crystalline lipid core which is stabilized by interfacial surfactants. SLNs are considered favorable candidates for drug delivery vehicles since their ability to store and release organic molecules can be tailored through the identity of the lipids and surfactants used. When stored, polymorphic transitions in the core of drug-loaded SLNs lead to the premature release of drug molecules. Significant experimental studies have been conducted with the aim of investigating the physicochemical properties of SLNs, however, no molecular scale investigations have been reported on the behaviors that drive SLN formation and their polymorphic transitions. A combination of small angle neutron scattering and all-atom molecular dynamics simulations is therefore used to yield a detailed atomistic description of the internal structure of an SLN comprising triglyceride, tripalmitin, and the nonionic surfactant, Brij O10 (C E ). The molecular scale mechanisms by which the surfactants stabilize the crystalline structure of the SLN lipid core are uncovered. By comparing these results to simulated liquid and solid aggregates of tripalmitin lipids, how the morphology of the lipids vary between these systems is demonstrated providing further insight into the mechanisms that control drug encapsulation and release from SLNs.

摘要

固体脂质纳米粒 (SLN) 具有结晶性脂质核心,由界面活性剂稳定。SLN 被认为是药物传递载体的理想候选物,因为它们存储和释放有机分子的能力可以通过所使用的脂质和表面活性剂的特性来调整。当储存时,载药 SLN 核心中的多晶型转变会导致药物分子过早释放。已经进行了大量的实验研究来研究 SLN 的物理化学性质,但是,没有报道关于驱动 SLN 形成及其多晶型转变的行为的分子尺度研究。因此,结合小角中子散射和全原子分子动力学模拟,对包含甘油三酯、三棕榈酸甘油酯和非离子表面活性剂 Brij O10 (C E ) 的 SLN 的内部结构进行了详细的原子描述。揭示了表面活性剂稳定 SLN 脂质核心结晶结构的分子尺度机制。通过将这些结果与三棕榈酸甘油酯脂质的模拟液体和固体聚集体进行比较,展示了这些系统之间脂质形态的变化,从而进一步深入了解控制 SLN 中药物包封和释放的机制。

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