Department of Chemical Engineering, Isfahan University of Technology, Isfahan, Iran.
Department of Biomedical Engineering, Neda Habibi, University of North Texas, Denton, Texas, United States.
Protein Pept Lett. 2022;29(1):80-88. doi: 10.2174/0929866528666211126160432.
Due to their solid-like porous structure, molecular organogel and microcrystal structures have the capabilities of loading drug molecules, encapsulation, and extended release, all considered as essential properties in drug delivery applications. Phases of these structures, however, depend on the solvent used during the gelation process.
Understanding the phase transition between organogel and microcrystal structures through adjusting the mixture ratio of different co-solvents.
Short peptide Diphenylalanine as the gelation building block was used due to its amino acid sequences that can be exactly selected at its molecular levels. Ethanol as a polar solvent was used in combination with four other co-solvents with different polarity levels, namely Xylene, Toluene, Acetone, and Dimethyl Sulfoxide. The morphology of molecular structures of each co-solvent combination at each ratio level was examined as well as the loading and release properties for a non-polar Flufenamic Acid drug.
The resultant structure was affected by the polarity of the co-solvents; in particular, in the sample containing 25 μg/ml of the drug, 94% of the drug amount was loaded inside the organogel. By increasing the drug concentration to 50, 75, and 100 μg/ml, the loading capability decreased to 76%, 47%, and 33%, respectively.
Molecular organogels have excellent capabilities of loading drug molecules, while microcrystal structures have higher release capacity. The findings of this study reveal how to best design a gelation method to obtain maximum loading or release properties for a particular peptide- based drug delivery application.
由于其类似固体的多孔结构，分子有机凝胶和微晶结构具有负载药物分子、封装和缓释的能力，这些都是药物输送应用中必不可少的特性。然而，这些结构的相态取决于凝胶化过程中使用的溶剂。
通过调整不同共溶剂的混合比，了解有机凝胶和微晶结构之间的相转变。
使用短肽二苯丙氨酸作为凝胶化构建块，因为其氨基酸序列可以在分子水平上精确选择。使用极性溶剂乙醇，并与四种不同极性水平的其他共溶剂（二甲苯、甲苯、丙酮和二甲基亚砜）组合使用。检查了每种共溶剂组合在每个比例水平下的分子结构形态以及非极性氟芬那酸药物的负载和释放性能。
所得结构受共溶剂极性的影响；特别是在含有 25μg/ml 药物的样品中，94%的药物量被负载到有机凝胶中。将药物浓度增加到 50、75 和 100μg/ml 时，载药量分别降低至 76%、47%和 33%。
分子有机凝胶具有优异的负载药物分子的能力，而微晶结构具有更高的释放能力。本研究的结果揭示了如何设计最佳的凝胶化方法，以获得特定基于肽的药物输送应用的最大负载或释放性能。
