Laboratory of Pharmaceutical Technology and Biopharmaceutics, Institute of Pharmacy, University of Bonn, Bonn, Germany; Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Int J Pharm. 2013 Nov 1;456(1):135-42. doi: 10.1016/j.ijpharm.2013.07.077. Epub 2013 Aug 16.
Solvent toxicity is one of the major drawbacks in the preparation of polymeric nanoparticles today. Here, polyethylene glycols (PEGs) are proposed as non-toxic solvents for the preparation of polymeric nanoparticles. Based on a preparation process similar to the solvent displacement technique, several process parameters were examined for their effects on the properties of the prepared nanoparticles by this method to achieve the optimum preparation conditions. The investigated parameters included polymer type and concentration, volume and temperature of the dispersing phase, methods of dispersing the solvent phase into the non-solvent phase, duration and speed of stirring and washing by dialysis. Ammonio methacrylate copolymer (Eudragit RL), poly-lactide-co-glycolide (PLGA), and PEG-PLGA were found to be successful polymer candidates for the preparation of nanoparticles by this method. Nanoparticles with diameters ranging from 80 to 400 nm can be obtained. The encapsulation efficiencies of bovine serum albumin, and lysozyme as model proteins were ranging from 7.3±2.2% to 69.3±1.8% depending on the strength of polymer-protein interaction. Biological assays confirmed a full lysozyme activity after the preparation process. PEG proved to be a suitable non-toxic solvent for the preparation of polymeric protein-loaded nanoparticles, maintaining the integrity of protein.
溶剂毒性是当今制备聚合物纳米粒子的主要缺点之一。在这里，聚乙二醇（PEGs）被提议作为制备聚合物纳米粒子的无毒溶剂。基于类似于溶剂置换技术的制备工艺，通过该方法研究了几种工艺参数对所制备纳米粒子性能的影响，以达到最佳的制备条件。研究的参数包括聚合物的类型和浓度、分散相的体积和温度、将溶剂相分散到非溶剂相中的方法、搅拌和透析洗涤的持续时间和速度。氨甲基丙烯酸共聚物（Eudragit RL）、聚乳酸-共-羟基乙酸（PLGA）和 PEG-PLGA 被发现是通过这种方法制备纳米粒子的成功聚合物候选物。可以得到直径在 80 至 400nm 之间的纳米粒子。根据聚合物-蛋白质相互作用的强度，牛血清白蛋白和溶菌酶作为模型蛋白质的包封效率在 7.3±2.2%至 69.3±1.8%之间。生物测定证实，在制备过程后，溶菌酶具有完全的活性。PEG 被证明是制备载有蛋白质的聚合物纳米粒子的合适无毒溶剂，保持蛋白质的完整性。
