a Faculty of Pharmacy and Biochemistry, Department of Pharmacognosy , University of Zagreb , Zagreb , Croatia.
b Department of Laboratory Diagnostics , University Hospital Centre Zagreb , Zagreb , Croatia.
J Microencapsul. 2018 Jan;35(1):1-12. doi: 10.1080/02652048.2017.1409819. Epub 2017 Dec 4.
This work aimed to investigate the potential effect of cyclodextrin encapsulation on intrinsic ability of daidzein (DAD) and genistein (GEN) to inhibit the glycosaminoglycan (GAG) synthesis in fibroblasts originating from patients with mucopolysaccharidosis (MPS), type II and III. DAD or GEN encapsulation with either 2-hydroxypropyl-β-cyclodextrin or sulphobuthylether-β-cyclodextrin were achieved by neat grinding and were characterised by thermal analysis, X-ray powder diffraction, scanning electron microscopy and solubility testing which confirmed the complexes formation with increased solubility with respect to starting compounds. Both isoflavones, as well as their co-ground cyclodextrin complexes reduced GAG levels in the fibroblasts of MPS II and MPS III patients from 54.8-77.5%, in a dose dependent manner, without any significant cytotoxic effect. Cyclodextrin encapsulation did not change the intrinsically high effect of both DAD and GEN on the GAG level reduction in the treated cells, thus could be considered as a part of combination therapies of MPS.
本研究旨在探究环糊精包合是否会影响大豆苷元(DAD)和染料木黄酮(GEN)抑制黏多糖贮积症(MPS)Ⅱ型和Ⅲ型成纤维细胞糖胺聚糖(GAG)合成的内在能力。通过干法研磨实现了 DAD 或 GEN 与 2-羟丙基-β-环糊精或磺丁基醚-β-环糊精的包合,并通过热分析、X 射线粉末衍射、扫描电子显微镜和溶解度测试对其进行了表征,证实了复合物的形成,与起始化合物相比,其溶解度有所提高。两种异黄酮及其共研磨的环糊精复合物均能剂量依赖性地降低 MPS II 和 MPS III 患者成纤维细胞中的 GAG 水平,降幅为 54.8-77.5%,且无明显细胞毒性作用。环糊精包合并未改变 DAD 和 GEN 对治疗细胞中 GAG 水平降低的固有高作用,因此可被视为 MPS 联合治疗的一部分。