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Development of the cholestosome, a novel delivery system made exclusively from cholesteryl esters
European Journal of Lipid Science and Technology ( IF 1.8 ) Pub Date : 2023-12-06 , DOI: 10.1002/ejlt.202300087 Lawrence Mielnicki 1 , Julie Hughes 1 , Jerome Schentag 2 , Mary Irving 2 , Victoria Monetti 1 , John Fraser MacArthur 1 , David Cordone 1 , Mary McCourt 1
European Journal of Lipid Science and Technology ( IF 1.8 ) Pub Date : 2023-12-06 , DOI: 10.1002/ejlt.202300087 Lawrence Mielnicki 1 , Julie Hughes 1 , Jerome Schentag 2 , Mary Irving 2 , Victoria Monetti 1 , John Fraser MacArthur 1 , David Cordone 1 , Mary McCourt 1
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A novel vesicular drug delivery system has been created using only cholesteryl esters. The uncharged nature of the esters requires a formulation process that uses energy, in the form of sonication, to facilitate the cholesteryl esters formation into vesicles. The nature of the material choices renders the vesicles resistant to pH degradation between a pH of 2 and 10. Storage condition at 4°C for 9 months shows a stability of encapsulated materials as well as vesicles. The formulation process is a modified reverse phase method in which the esters are dissolved in an organic solvent, which is then removed and the aqueous component is then added with sonication in a temperature-controlled water bath. A wide variety of materials can be encapsulated in these vesicles, which are called cholestosomes. Delivery of the cholestosome-encapsulated materials is a function of the ester component structure and not the encapsulated molecule. Once encapsulated, the vesicles deliver the materials into cells. The potential for oral availability was explored using chylomicrons. Successful delivery of the cholestosome encapsulated into chylomicrons has enhanced the effectiveness of delivery to cells. Analytical methods have been developed to analyze the materials chosen from the cholesteryl esters as well as the encapsulated materials.
中文翻译：
胆甾醇体的开发，一种完全由胆固醇酯制成的新型输送系统
仅使用胆固醇酯创建了一种新型囊泡药物递送系统。酯的不带电性质需要使用超声处理形式的能量的配制过程，以促进胆固醇酯形成囊泡。材料选择的性质使得囊泡能够抵抗 pH 值为 2 至 10 之间的 pH 降解。在 4°C 的储存条件下保存 9 个月显示了封装材料和囊泡的稳定性。配制过程是一种改进的反相方法，其中将酯溶解在有机溶剂中，然后除去有机溶剂，然后在温控水浴中超声处理后添加水性组分。这些囊泡中可以封装多种材料，这些囊泡称为胆汁小体。胆囊体封装材料的递送是酯组分结构的函数，而不是封装分子的函数。一旦被封装，囊泡就会将材料输送到细胞中。使用乳糜微粒探索了口服利用的潜力。成功递送封装在乳糜微粒中的胆囊体增强了递送至细胞的有效性。已经开发出分析方法来分析选自胆固醇酯的材料以及封装材料。
更新日期：2023-12-06
中文翻译：
胆甾醇体的开发，一种完全由胆固醇酯制成的新型输送系统
仅使用胆固醇酯创建了一种新型囊泡药物递送系统。酯的不带电性质需要使用超声处理形式的能量的配制过程，以促进胆固醇酯形成囊泡。材料选择的性质使得囊泡能够抵抗 pH 值为 2 至 10 之间的 pH 降解。在 4°C 的储存条件下保存 9 个月显示了封装材料和囊泡的稳定性。配制过程是一种改进的反相方法，其中将酯溶解在有机溶剂中，然后除去有机溶剂，然后在温控水浴中超声处理后添加水性组分。这些囊泡中可以封装多种材料，这些囊泡称为胆汁小体。胆囊体封装材料的递送是酯组分结构的函数，而不是封装分子的函数。一旦被封装，囊泡就会将材料输送到细胞中。使用乳糜微粒探索了口服利用的潜力。成功递送封装在乳糜微粒中的胆囊体增强了递送至细胞的有效性。已经开发出分析方法来分析选自胆固醇酯的材料以及封装材料。
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