Department of Chemistry, Sam Houston State University, Huntsville, Texas 77341, USA.
AAPS PharmSciTech. 2012 Mar;13(1):112-7. doi: 10.1208/s12249-011-9728-5. Epub 2011 Dec 9.
A dendritic poly(2-alkyloxazoline)-based polymer was studied as a new carrier system for the organophosphorus-hydrolyzing recombinant enzymes, organophosphorus acid anhydrolase and organophosphorus hydrolase. Paraoxon (PO) and diisopropylfluorophosphate (DFP) were used as model organophosphorus compounds. Changes in plasma cholinesterase activity were monitored. The cholinesterase activity was proportional to the concentrations of DFP or PO. Plasma cholinesterase activity was higher in animals receiving enzyme and oxime before the organophosphates than in the oxime-only pretreated groups. These studies suggest that cholinesterase activity can serve as an indicator for the in vivo protection by the nano-intercalated organophosphorus acid anhydrolase or organophosphorus hydrolase against organophosphorus intoxications. These studies represent a practical application of polymeric nano-delivery systems as enzyme carriers in drug antidotal therapy.
一种基于树枝状聚（2-烷氧基恶唑啉）的聚合物被研究作为一种新的载体系统，用于有机磷水解重组酶、有机磷酸酐酶和有机磷水解酶。对氧磷（PO）和二异丙基氟磷酸酯（DFP）被用作模型有机磷化合物。监测血浆胆碱酯酶活性的变化。胆碱酯酶活性与 DFP 或 PO 的浓度成正比。在接受酶和肟预处理之前接受酶和肟的动物的血浆胆碱酯酶活性高于仅接受肟预处理的组。这些研究表明，胆碱酯酶活性可以作为纳米插层有机磷酸酐酶或有机磷水解酶对有机磷中毒的体内保护的指标。这些研究代表了聚合纳米递药系统作为酶载体在药物解毒治疗中的实际应用。
