Department of Pharmaceutical Sciences, University of North Texas Health Science Center, Fort Worth, TX, USA.
Department of Pharmaceutical Sciences, University of North Texas Health Science Center, Fort Worth, TX, USA.
Int J Pharm. 2024 Aug 15;661:124447. doi: 10.1016/j.ijpharm.2024.124447. Epub 2024 Jul 16.
None of transitional lipid-based drug delivery systems (LBDDS) includes compositions containing one lipid and one water-soluble surfactant that form stable microemulsions. The conversion of liquid LBDDS to solid LBDDS has been limited by low drug loading. Previously, we have developed drug solid microemulsions containing one lipid and TPGS (a water-soluble surfactant) that achieved high drug loading and remarkably increased oral bioavailability. This study aimed to test if binary lipid systems (BLS), composed of one lipid and one water-soluble surfactant that form stable self-emulsifying microemulsions, is not an exclusive but widely applicable type of LBDDS for other lipids and surfactants and evaluate the influences of chemical structures of lipids and surfactants on microemulsions and solid microemulsions. We systemically identified new BLS by using a library of lipids and surfactants. Propylene glycol diesters and glycerol triesters were favorable for forming stable microemulsions with Tween 80, Cremophor EL, or TPGS. To the best of our knowledge, this is the first report exploring and confirming that the BLS is a new addition to traditional LBDDS, provides a promising option for researchers, and has the potential to increase drug loading to facilitate the development of solid microemulsions.
没有一种过渡性的基于脂质的药物传递系统（LBDDS）包括含有一种脂质和一种水溶性表面活性剂的组合物，这些组合物可以形成稳定的微乳液。将液体 LBDDS 转化为固体 LBDDS 受到载药量低的限制。以前，我们已经开发了含有一种脂质和 TPGS（一种水溶性表面活性剂）的药物固体微乳液，该微乳液实现了高载药量，并显著提高了口服生物利用度。本研究旨在测试由一种脂质和一种水溶性表面活性剂组成的二元脂质系统（BLS）是否不是其他脂质和表面活性剂的 LBDDS 的唯一类型，而是广泛适用的类型，并评估脂质和表面活性剂的化学结构对微乳液和固体微乳液的影响。我们系统地使用脂质和表面活性剂库来识别新的 BLS。丙二醇二酯和甘油三酯与吐温 80、聚氧乙烯蓖麻油或 TPGS 形成稳定的微乳液。据我们所知，这是第一个探索和证实 BLS 是传统 LBDDS 的新补充的报告，为研究人员提供了一个有前途的选择，并有可能提高载药量，从而促进固体微乳液的开发。
