Abstract：
Proteins have recently caught attention as potential excipients for amorphous solid dispersions (ASDs) to improve oral bioavailability of poorly water-soluble drugs. Notably, the studies have highlighted whey protein isolates, particularly β-lactoglobulin (BLG), as promising candidates in amorphous stabilization, dissolution and solubility enhancement, achieving drug loadings of 50 wt% and higher. Consequently, investigations into the mechanisms underlying the solid-state stabilization of amorphous drugs and the enhancement of drug solubility in solution have been conducted. This graphical review provides a comprehensive overview of recent findings concerning BLG-based ASDs. Firstly, the dissolution performance of BLG-based ASDs is compared to more traditional polymer-based ASDs. Secondly, the drug loading onto BLG and the resulting amorphous stabilization mechanisms is summarized. Thirdly, interactions between BLG and drug molecules in solution are described as the mechanisms governing the improvement of drug solubility. Lastly, we outline the impact of the spray drying process on the secondary structure of BLG, and the resulting differences in amorphous stabilization and drug dissolution performance between α-helix-rich and β-sheet-rich BLG-based ASDs.
摘要：
蛋白质最近作为无定形固体分散体（ASD）的潜在赋形剂引起了人们的注意，以改善水溶性差的药物的口服生物利用度。值得注意的是,这些研究强调了乳清蛋白分离物，特别是β-乳球蛋白（BLG），作为无定形稳定的有希望的候选者，溶解和溶解度增强，实现50重量%和更高的药物负载。因此,已对无定形药物的固态稳定和药物在溶液中溶解度的增强进行了研究。此图形评论提供了有关基于BLG的ASD的最新发现的全面概述。首先,将基于BLG的ASD的溶解性能与更传统的基于聚合物的ASD进行比较。其次,总结了药物在BLG上的负载以及由此产生的无定形稳定机制。第三，BLG与溶液中药物分子之间的相互作用被描述为控制药物溶解度提高的机制。最后,我们概述了喷雾干燥过程对BLG二级结构的影响，以及由此产生的富含α-螺旋和富含β-折叠的BLG的基于ASD之间的无定形稳定性和药物溶出性能的差异。
