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Liquid Crystalline Nanostructures as PEGylated Reservoirs of Omega-3 Polyunsaturated Fatty Acids: Structural Insights toward Delivery Formulations against Neurodegenerative Disorders
ACS Omega ( IF 4.1 ) Pub Date : 2018-03-16 00:00:00 , DOI: 10.1021/acsomega.7b01935
Angelina Angelova 1 , Markus Drechsler 2 , Vasil M Garamus 3 , Borislav Angelov 4
Affiliation  

Omega-3 polyunsaturated fatty acids (ω-3 PUFAs) are bioactive lipids with considerable impact in medicine and nutrition. These compounds exert structuring effects on the cellular membrane organization, regulate the gene expression, and modulate various signaling cascades and metabolic processes. The purpose of the present work is to demonstrate the structural features of ω-3 PUFA-containing three-dimensional supramolecular lipid assemblies suitable for pharmaceutical applications that require soft porous carriers. We investigate the liquid crystalline structures formed upon mixing of eicosapentaenoic acid (EPA, 20:5) with the lyotropic nonlamellar lipid monoolein and the formation of multicompartment assemblies. Starting with the monoolein-based lipid cubic phase, double membrane vesicles, cubosome precursors, sponge-type particles (spongosomes), mixed intermediate nonlamellar structures, and multicompartment assemblies are obtained through self-assembly at different amphiphilic compositions. The dispersions containing spongosomes as well as nanocarriers with oil and vesicular compartments are stabilized by PEGylation of the lipid/water interfaces using a phospholipid with a poly(ethylene glycol) chain. The microstructures of the bulk mixtures were examined by cross-polarized light optical microscopy. The dispersed liquid crystalline structures and intermediate states were studied by small-angle X-ray scattering, cryogenic transmission electron microscopy, and quasielastic light scattering techniques. They established that PUFA influences the phase type and the sizes of the aqueous compartments of the liquid crystalline carriers. The resulting multicompartment systems and stealth nanosponges may serve as mesoporous reservoirs for coencapsulation of ω-3 PUFA (e.g., EPA) with water-insoluble drugs and hydrophilic macromolecules toward development of combination treatment strategies of neurodegenerative and other diseases.

中文翻译:

液晶纳米结构作为 Omega-3 多不饱和脂肪酸的聚乙二醇化储存库:针对神经退行性疾病递送制剂的结构见解

Omega-3 多不饱和脂肪酸 (ω-3 PUFA) 是具有生物活性的脂质,在医学和营养方面具有相当大的影响。这些化合物对细胞膜组织发挥结构化作用,调节基因表达,并调节各种信号级联和代谢过程。本工作的目的是证明含 ω-3 PUFA 的三维超分子脂质组装体的结构特征,适用于需要软多孔载体的制药应用。我们研究了二十碳五烯酸(EPA,20:5)与溶致非层状脂质单油酸酯混合时形成的液晶结构以及多室组件的形成。从基于单油酸甘油酯的脂质立方相开始,通过不同两亲性组合物的自组装获得双膜囊泡、立方体前体、海绵型颗粒(海绵体)、混合中间非层状结构和多室组件。含有海绵体以及具有油和囊泡隔室的纳米载体的分散体通过使用具有聚乙二醇链的磷脂对脂质/水界面进行聚乙二醇化来稳定。通过交叉偏振光光学显微镜检查本体混合物的微观结构。通过小角X射线散射、低温透射电子显微镜和准弹性光散射技术研究了分散液晶结构和中间态。他们确定 PUFA 影响液晶载体的相类型和水室的大小。由此产生的多室系统和隐形纳米海绵可以作为介孔储库,用于将ω-3 PUFA(例如EPA)与水不溶性药物和亲水性大分子共封装,以开发神经退行性疾病和其他疾病的联合治疗策略。
更新日期:2018-03-16
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