Li Yingpeng, Li Xiuyan, Guan Qingxia, Zhang Chunjing, Xu Ting, Dong Yujing, Bai Xinyu, Zhang Weiping
College of Pharmacy, Tianjin University of Traditional Chinese Medicine, Tianjin.
College of Pharmacy, Heilongjiang University of Traditional Chinese Medicine, Harbin, People's Republic of China.
Int J Nanomedicine. 2017 Feb 22;12:1465-1474. doi: 10.2147/IJN.S119115. eCollection 2017.
Enhancing drug delivery is an ongoing endeavor in pharmaceutics, especially when the efficacy of chemotherapy for cancer is concerned. In this study, we prepared and evaluated nanosized HKUST-1 (nanoHKUST-1), nanosized metal-organic drug delivery framework, loaded with 5-fluorouracil (5-FU) for potential use in cancer treatment.
NanoHKUST-1 was prepared by reacting copper (II) acetate [Cu(OAc)] and benzene-1,3,5-tricarboxylic acid (HBTC) with benzoic acid (CHCOOH) at room temperature (23.7°C±2.4°C). A central composite design was used to optimize 5-FU-loaded nanoHKUST-1. Contact time, ethanol concentration, and 5-FU:material ratios were the independent variables, and the entrapment efficiency of 5-FU was the response parameter measured. Powder X-ray diffraction, scanning electron microscopy (SEM), transmission electron microscopy (TEM), and nitrogen adsorption were used to determine the morphology of nanoHKUST-1. In addition, 5-FU release studies were conducted, and the in vitro cytotoxicity was evaluated.
Entrapment efficiency and drug loading were 9.96% and 40.22%, respectively, while the small-angle X-ray diffraction patterns confirmed a regular porous structure. The SEM and TEM images of the nanoHKUST-1 confirmed the presence of round particles (diameter: approximately 100 nm) and regular polygon arrays of mesoporous channels of approximately 2-5 nm. The half-maximal lethal concentration (LC) of the 5-FU-loaded nanoHKUST-1 was approximately 10 µg/mL.
The results indicated that nanoHKUST-1 is a potential vector worth developing as a cancer chemotherapeutic drug delivery system.
提高药物递送效率是制药领域一项持续不断的工作，尤其是在关注癌症化疗疗效时。在本研究中，我们制备并评估了负载5-氟尿嘧啶（5-FU）的纳米尺寸的HKUST-1（nanoHKUST-1），一种纳米尺寸的金属有机药物递送框架，用于癌症治疗的潜在应用。
通过在室温（23.7°C±2.4°C）下使醋酸铜[Cu(OAc)]、苯-1,3,5-三羧酸（HBTC）与苯甲酸（CHCOOH）反应制备nanoHKUST-1。采用中心复合设计优化负载5-FU的nanoHKUST-1。接触时间、乙醇浓度和5-FU与材料的比例为自变量，5-FU的包封率为测量的响应参数。使用粉末X射线衍射、扫描电子显微镜（SEM）、透射电子显微镜（TEM）和氮气吸附来确定nanoHKUST-1的形态。此外，进行了5-FU释放研究，并评估了体外细胞毒性。
包封率和载药量分别为9.96%和40.22%，同时小角X射线衍射图谱证实了规则的多孔结构。nanoHKUST-1的SEM和TEM图像证实存在圆形颗粒（直径：约100 nm）以及约2-5 nm的介孔通道规则多边形阵列。负载5-FU的nanoHKUST-1的半数致死浓度（LC）约为10 µg/mL。
结果表明nanoHKUST-1作为一种癌症化疗药物递送系统是一种值得开发的潜在载体。
