Garbiec Ewa, Rosiak Natalia, Sip Szymon, Zalewski Przemysław, Cielecka-Piontek Judyta
Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, Rokietnicka 3 Str., 60-806 Poznan, Poland.
Int J Mol Sci. 2025 Jan 20;26(2):855. doi: 10.3390/ijms26020855.
Curcumin, a compound known for its antioxidant and neuroprotective properties, faces challenges due to its low water solubility, which can limit its effectiveness. One effective method to address this issue is through amorphization. Incorporating curcumin into a polymeric matrix to form amorphous solid dispersions is a common approach. Another strategy involves co-amorphous systems, where low-molecular-weight components act as co-formers. A recent innovative approach combines these strategies. This study used tryptophan as a co-former and prepared systems using supercritical fluid technology. The amorphous nature of two systems was confirmed through X-ray powder diffraction: one with 10% curcumin and a polymer, and another with 10% curcumin, a polymer, and tryptophan. Fourier-transform infrared analysis demonstrated molecular interactions among all components in the systems. Scanning electron microscopy revealed that the amorphization process significantly modified the morphology of the powder particles. The ternary system with tryptophan notably increased curcumin solubility by over 300-fold. The amorphous form of curcumin in both systems exhibited significantly higher dissolution rates compared to its crystalline form. The system with tryptophan showed more than a threefold improvement in permeability according to the PAMPA test. The enhanced solubility led to over a sixfold increase in antioxidant activity and a 25-fold improvement in the inhibition of the enzyme butyrylcholinesterase.
姜黄素是一种以其抗氧化和神经保护特性而闻名的化合物，由于其低水溶性而面临挑战，这可能会限制其有效性。解决这个问题的一种有效方法是通过非晶化。将姜黄素掺入聚合物基质中以形成非晶态固体分散体是一种常见的方法。另一种策略涉及共非晶体系，其中低分子量成分作为共形成剂。最近的一种创新方法结合了这些策略。本研究使用色氨酸作为共形成剂，并使用超临界流体技术制备体系。通过X射线粉末衍射证实了两种体系的非晶性质：一种含有10%姜黄素和一种聚合物，另一种含有10%姜黄素、一种聚合物和色氨酸。傅里叶变换红外分析表明体系中所有成分之间存在分子相互作用。扫描电子显微镜显示非晶化过程显著改变了粉末颗粒的形态。含有色氨酸的三元体系使姜黄素的溶解度显著提高了300多倍。与结晶形式相比，两种体系中姜黄素的非晶形式均表现出显著更高的溶解速率。根据平行人工膜渗透试验（PAMPA），含有色氨酸的体系在渗透性方面提高了三倍多。溶解度的提高导致抗氧化活性增加了六倍多，对丁酰胆碱酯酶的抑制作用提高了25倍。
