Vandervoort J, Ludwig A
Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Antwerp (Wilrijk), Belgium.
Int J Pharm. 2002 May 15;238(1-2):77-92. doi: 10.1016/s0378-5173(02)00058-3.
Poly(lactic-co-glycolic-acid) nanoparticles are often produced using the w/o/w emulsification solvent evaporation method. In most cases poly(vinyl alcohol) (PVA) is used as stabilizer of the emulsion. The goal of this study was to compare a series of polymers to PVA in a 2(2) full factorial design study. The influence of the concentration of PVA and the polymers tested on particle size and zeta potential value was evaluated before and after freeze-drying of the prepared particles. Nanoparticles were obtained with most polymers when they were used in combination with PVA. Leaving PVA out of the formulation, however, increased the size of the particles over 1 microm. Two exceptions are poloxamer and carbopol, which can be considered as valuable alternatives to PVA. Zeta potential values were usually slightly negative, the most extreme zeta potential values were measured when poloxamer and carbopol were employed. The use of gelatin type A made it possible to achieve positive values. The original 2(2) full factorial design study was further expanded to a central composite design for poloxamer and carbopol, in order to fit the measured data to a quadratic model and to calculate response surfaces.
聚乳酸-乙醇酸共聚物纳米颗粒通常采用水包油包水乳化溶剂蒸发法制备。在大多数情况下,聚乙烯醇(PVA)用作乳液的稳定剂。本研究的目的是在一项2(2)全因子设计研究中,将一系列聚合物与PVA进行比较。在制备的颗粒冻干前后,评估PVA和测试聚合物的浓度对粒径和zeta电位值的影响。当大多数聚合物与PVA联合使用时,可获得纳米颗粒。然而,在配方中不使用PVA会使颗粒尺寸增加到1微米以上。泊洛沙姆和卡波姆是两个例外,它们可被视为PVA的有价值替代品。zeta电位值通常略为负值,使用泊洛沙姆和卡波姆时测得的zeta电位值最为极端。使用A型明胶可实现正值。最初的2(2)全因子设计研究进一步扩展为泊洛沙姆和卡波姆的中心复合设计,以便将测量数据拟合到二次模型并计算响应面。