Department of Materials Science and Engineering, University of Central Florida, 12760 Pegasus Dr, Orlando, FL-32816, USA.
NanoScience Technology Center, University of Central Florida, 12424 Research Pkwy #400, Orlando, FL-32826, USA.
Chembiochem. 2024 Jan 2;25(1):e202300440. doi: 10.1002/cbic.202300440. Epub 2023 Nov 20.
Peptide-based polyelectrolyte complexes are biocompatible materials that can encapsulate molecules with different polarities due to their ability to be precisely designed. Here we use UV-Vis spectroscopy, fluorescence microscopy, and infrared spectroscopy to investigate the encapsulation of model drugs, doxorubicin (DOX) and methylene blue (MB) using a series of rationally designed polypeptides. For both drugs, we find an overall higher encapsulation efficiency with sequences that have higher charge density, highlighting the importance of ionic interactions between the small molecules and the peptides. However, comparing molecules with the same charge density, illustrated that the most hydrophobic sequence pairs had the highest encapsulation of both DOX and MB molecules. The phase behavior and stability of DOX-containing complexes did not change compared to the complexes without drugs. However, MB encapsulation caused changes in the stabilities of the complexes. The sequence pair with the highest charge density and hydrophobicity had the most dramatic increase in stability, which coincided with a phase change from liquid to solid. This study illustrates how multiple types of molecular interactions are required for efficient encapsulation of poorly soluble drugs and provides insights into the molecular design of delivery carriers.
基于肽的聚电解质复合物是生物相容性材料，由于其能够精确设计，因此可以封装具有不同极性的分子。在这里，我们使用紫外可见光谱、荧光显微镜和红外光谱研究了一系列合理设计的多肽对模型药物阿霉素（DOX）和亚甲蓝（MB）的包封。对于这两种药物，我们发现电荷密度较高的序列的总体包封效率更高，这突出了小分子和多肽之间离子相互作用的重要性。然而，比较具有相同电荷密度的分子表明，最疏水的序列对同时对 DOX 和 MB 分子具有最高的包封率。与不含药物的复合物相比，含 DOX 的复合物的相行为和稳定性没有变化。然而，MB 的包封导致复合物的稳定性发生变化。电荷密度和疏水性最高的序列对的稳定性增加最为显著，这与从液相到固相的相转变相吻合。这项研究说明了多种类型的分子相互作用对于有效包封疏水性药物的必要性，并为递药载体的分子设计提供了思路。
