<br>大豆磷脂酰胆碱和甘油二油酸酯的高度结构立方胶束脂质纳米颗粒的形成及其三酰甘油脂肪酶的降解,ACS Applied Materials & Interfaces

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大豆磷脂酰胆碱和甘油二油酸酯的高度结构立方胶束脂质纳米颗粒的形成及其三酰甘油脂肪酶的降解
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2014-05-07 00:00:00 , DOI: 10.1021/am501489e
Maria Wadsäter ₁ , Justas Barauskas , Tommy Nylander , Fredrik Tiberg

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立方胶束(I ₂ )等反相内相结构的脂质纳米粒对肽、蛋白质以及一些小分子表现出良好的载药能力。由于其可控的小尺寸和内部形态，此类纳米颗粒适合使用几种不同的给药途径进行药物递送，包括静脉注射、肌内注射和皮下注射。在这方面，一个非常有趣的系统是双组分大豆磷脂酰胆碱（SPC）/甘油二油酸酯（GDO）系统，它根据脂质组分的比例形成一系列反向液晶相。对于过量水中的 50/50 (w/w) 比例，这些脂质已被证明可形成Fd 3 m结构的反立方胶束 (I ₂ ) 相。在这里，我们证明，在少量（5-10 wt%）聚山梨醇酯 80 (P80) 存在的情况下，这种 SPC/GDO 相可以分散成纳米颗粒，且仍具有明确的Fd 3 m结构。所得纳米颗粒分散体具有窄的尺寸分布并表现出良好的长期稳定性。在制药应用中，药物输送载体及其成分的生物降解途径是重要的考虑因素。在研究的第二部分中，我们展示了在类似生理的温度和 pH 值下暴露于三酰甘油脂肪酶 (TGL) 时颗粒的结构如何演变。 TGL 催化酰基甘油酯（例如 GDO）脂解降解为单酸甘油酯、甘油和游离脂肪酸。在降解过程中，颗粒的内相经历了从反向 I ₂结构到负曲率较小的结构（二维六边形、双连续立方和海绵）的连续相变，最终导致多层囊泡的形成。

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Formation of Highly Structured Cubic Micellar Lipid Nanoparticles of Soy Phosphatidylcholine and Glycerol Dioleate and Their Degradation by Triacylglycerol Lipase

Lipid nanoparticles of reversed internal phase structures, such as cubic micellar (I₂) structure show good drug loading ability of peptides and proteins as well as some small molecules. Due to their controllable small size and inner morphology, such nanoparticles are suitable for drug delivery using several different administration routes, including intravenous, intramuscular, and subcutaneous injection. A very interesting system in this regard, is the two component soy phosphatidylcholine (SPC)/glycerol dioleate (GDO) system, which depending on the ratio of the lipid components form a range of reversed liquid crystalline phases. For a 50/50 (w/w) ratio in excess water, these lipids have been shown to form a reversed cubic micellar (I₂) phase of the Fd3m structure. Here, we demonstrate that this SPC/GDO phase, in the presence of small quantities (5–10 wt %) of Polysorbate 80 (P80), can be dispersed into nanoparticles, still with well-defined Fd3m structure. The resulting nanoparticle dispersion has a narrow size distribution and exhibit good long-term stability. In pharmaceutical applications, biodegradation pathways of the drug delivery vehicles and their components are important considerations. In the second part of the study we show how the structure of the particles evolves during exposure to a triacylglycerol lipase (TGL) under physiological-like temperature and pH. TGL catalyzes the lipolytic degradation of acylglycerides, such as GDO, to monoglycerides, glycerol, and free fatty acids. During the degradation, the interior phase of the particles is shown to undergo continuous phase transitions from the reversed I₂ structure to structures of less negative curvature (2D hexagonal, bicontinuous cubic, and sponge), ultimately resulting in the formation of multilamellar vesicles.

更新日期：2014-05-07

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