Uchiyama Hiromasa, Kadota Kazunori, Tozuka Yuichi
Department of Formulation Design and Pharmaceutical Technology, Faculty of Pharmacy, Osaka Medical and Pharmaceutical University, Takatsuki, Osaka, Japan.
Crit Rev Food Sci Nutr. 2023;63(32):11226-11243. doi: 10.1080/10408398.2022.2092056. Epub 2022 Jun 27.
Transglycosylation has been used to modify the physicochemical properties of original compounds. As a result, transglycosylated compounds can form molecular aggregates in size ranges of a few nanometers in an aqueous medium when their concentrations exceed a specific level. Incorporating these hydrophobic compounds has been observed to enhance the solubility of hydrophobic compounds into aggregate structures. Thus, this review introduces four transglycosylated compounds as food additives that can enhance the solubility and oral absorption of hydrophobic compounds. Here, transglycosylated hesperidin, transglycosylated rutin, transglycosylated naringin, and transglycosylated stevia are the focus as representative substances. Significantly, we observed that amorphous formations containing hydrophobic compounds with transglycosylated compounds improved solubility and oral absorption compared to untreated hydrophobic compounds. Moreover, combining transglycosylated compounds with hydrophilic polymers or surfactants enhanced the solubilizing effects on hydrophobic compounds. Furthermore, the enhanced solubility of hydrophobic compounds improved their oral absorption. Transglycosylated compounds also influenced nanoparticle preparation of hydrophobic compounds as a dispersant. This study demonstrated the benefits of transglycosylated compounds in developing supplements and nutraceuticals of hydrophobic compounds with poor aqueous solubility.
转糖基化作用已被用于改变原始化合物的物理化学性质。因此,当转糖基化化合物的浓度超过特定水平时,它们在水性介质中能够形成尺寸范围为几纳米的分子聚集体。据观察,掺入这些疏水性化合物可提高疏水性化合物在聚集体结构中的溶解度。因此,本综述介绍了四种作为食品添加剂的转糖基化化合物,它们可以提高疏水性化合物的溶解度和口服吸收。在此,转糖基化橙皮苷、转糖基化芦丁、转糖基化柚皮苷和转糖基化甜菊糖苷作为代表性物质成为焦点。值得注意的是,我们观察到,与未处理的疏水性化合物相比,含有转糖基化化合物的疏水性化合物的无定形形成提高了溶解度和口服吸收。此外,将转糖基化化合物与亲水性聚合物或表面活性剂结合可增强对疏水性化合物的增溶效果。此外,疏水性化合物溶解度的提高改善了它们的口服吸收。转糖基化化合物作为分散剂也影响了疏水性化合物的纳米颗粒制备。这项研究证明了转糖基化化合物在开发水溶性差的疏水性化合物的补充剂和营养保健品方面的益处。