Kioomars Sajedeh, Heidari Somayeh, Malaekeh-Nikouei Bizhan, Shayani Rad Maryam, Khameneh Bahman, Mohajeri Seyed Ahmad
a Students Research Committee, Department of Food and Drug Control, School of Pharmacy , Mashhad University of Medical Sciences , Mashhad , Iran.
b Nanotechnology Research Center, School of Pharmacy , Mashhad University of Medical Sciences , Mashhad , Iran.
Pharm Dev Technol. 2017 Feb;22(1):122-129. doi: 10.1080/10837450.2016.1230131. Epub 2016 Sep 21.
In this study several ciprofloxacin (CFX) imprinted and non-imprinted hydrogels were prepared and evaluated as ocular drug delivery systems in aqueous media. 2-Hydroxyethyl methacrylate (HEMA) was used as a solvent and backbone monomer, ethylene glycol dimethacrylate (EGDMA) as a cross-linker, methacrylic acid (MAA) as a functional monomer and CFX as the template molecule. CFX-imprinted hydrogels (MIPs) were prepared applying different CFX:MAA molar ratios (1:16, 1:20 and 1:32) in feed composition of monomer solutions. Thermal polymerization was applied and hydrogels were synthesized in a polypropylene mold (0.4 mm thickness). Swelling and binding properties of hydrogels were evaluated in water. Release profile of the MIPs was evaluated in NaCl (0.9%) and artificial tears. The data showed that enhancing the MAA concentration, as a co-monomer, and using molecular imprinting improved binding properties of the synthesized hydrogels. The optimized MIPs with 400 mM MAA and CFX: MAA molar ratio of 1:20 and 1:16 showed the greatest affinity for CFX and the highest ability to control drug release. In vitro antibacterial activity of hydrogels was studied and demonstrated the effect of CFX-loaded hydrogels against Pseudomonas aeruginosa (P. aeruginosa) and Staphylococcus aureus (S. aureus) isolated from patients' eyes. This study indicated antibacterial efficacy of CFX-loaded MIP hydrogels.
在本研究中，制备了几种环丙沙星（CFX）印迹和非印迹水凝胶，并将其作为水性介质中的眼部给药系统进行评估。甲基丙烯酸2-羟乙酯（HEMA）用作溶剂和主链单体，乙二醇二甲基丙烯酸酯（EGDMA）用作交联剂，甲基丙烯酸（MAA）用作功能单体，CFX用作模板分子。在单体溶液的进料组成中应用不同的CFX:MAA摩尔比（1:16、1:20和1:32）制备CFX印迹水凝胶（MIPs）。采用热聚合，在聚丙烯模具（厚度0.4毫米）中合成水凝胶。在水中评估水凝胶的溶胀和结合性能。在NaCl（0.9%）和人工泪液中评估MIPs的释放曲线。数据表明，提高作为共聚单体的MAA浓度以及使用分子印迹可改善合成水凝胶的结合性能。具有400 mM MAA且CFX:MAA摩尔比为1:20和1:16的优化MIPs对CFX表现出最大亲和力和最高的药物释放控制能力。研究了水凝胶的体外抗菌活性，并证明了负载CFX的水凝胶对从患者眼中分离出的铜绿假单胞菌（P. aeruginosa）和金黄色葡萄球菌（S. aureus）的作用。本研究表明负载CFX的MIP水凝胶具有抗菌功效。
