Sun Yi-Wei, Wang Li-Hong, Meng Da-Li, Che Xin
School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Shenyang 110016, PR China.
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Oncotarget. 2017 Nov 11;8(62):105673-105681. doi: 10.18632/oncotarget.22387. eCollection 2017 Dec 1.
This study described a valuable drug delivery system for poorly water-soluble anticancer naturalproduct, licochalcone A, isolated from , loaded on hollow gold nanoparticles by green method to improve solubility and dissolution and maintain its natural pharmacological property. Briefly, the formation of hollow gold nanoparticles involves three steps: preparing of silica nanospheres by Stober method, forming of a thick gold shell around the silica templates and etching of silica particles by HF solution. Hollow gold nanoparticles (HGNPs) and drug loaded hollow gold nanoparticles (L-HGNPs) displayed spherical structure and approximately 200nm in size observed by SEM, XRD, EDS and DSC analysis showed that HGNPs were gold hollow structure and crystalline form. The solubility in aqueous solution of licochalcone A was increased obviously to 488.9 μg/ml, compared with free drugs of 136.1 μg/ml. Another interesting finding is that near-infrared (NIR) irradiation increased the speed of solubility of licochalcone A in aqueous solutions, rather than quantity. In short, the method of nano-delivery system combined with poorly water-soluble drug to improve its solubility and dissolution is worth applying to other natural products in order to increase their opportunities in clinical applications.
本研究描述了一种用于水溶性差的抗癌天然产物甘草查尔酮A的有价值的药物递送系统，该天然产物从[具体来源未译出]中分离得到，通过绿色方法负载于中空金纳米颗粒上，以提高其溶解度和溶出度，并保持其天然药理特性。简而言之，中空金纳米颗粒的形成涉及三个步骤：通过斯托伯方法制备二氧化硅纳米球，在二氧化硅模板周围形成厚金壳，以及用氢氟酸溶液蚀刻二氧化硅颗粒。通过扫描电子显微镜（SEM）观察，中空金纳米颗粒（HGNPs）和载药中空金纳米颗粒（L-HGNPs）呈现球形结构，尺寸约为200nm，X射线衍射（XRD）、能谱分析（EDS）和差示扫描量热法（DSC）分析表明，HGNPs为金中空结构且为晶型。与游离药物的136.1μg/ml相比，甘草查尔酮A在水溶液中的溶解度明显提高至488.9μg/ml。另一个有趣的发现是，近红外（NIR）照射提高了甘草查尔酮A在水溶液中的溶解速度，而非溶解量。总之，纳米递送系统与水溶性差的药物相结合以提高其溶解度和溶出度的方法值得应用于其他天然产物，以增加它们在临床应用中的机会。
