Université de Lyon, F-69622, Lyon, France.
J Biomed Nanotechnol. 2011 Apr;7(2):255-62. doi: 10.1166/jbn.2011.1279.
Preparation of biodegradable nanoparticles containing active molecule is now taking much attention of researchers. The aim of the present work is to achieve the nanosize particles for the first time by double emulsion (W1/O/W2,) evaporation method to encapsulate hydrophilic substance using high performance stirring apparatus. A fluorescent stable hydrophilic agent (Stilbene derivative) was used as a model drug to be encapsulated. For this purpose, PCL (polycaprolactone) was chosen as polymer in this study. Several kinds of stabilizers [triton-405, tween 80, poloxamer, PVP (polyvinylpyrrolidone), PEG (poly ethylene glycol) & PVA (poly vinyl alcohol)] were investigated and the results indicate that the PVA (0.5% concentration) leads to the most stable double emulsion with the particle size in nano range. Different parameters affecting the size of particles have been studied such as stirring time (for 1st and 2nd emulsion), stirring speed (for 1st and 2nd emulsion), polymer and stabilizer concentrations etc. After duration of one month, the encapsulation efficiency of obtained particles was estimated using U.V. analysis. Transmission Electron Microscopy (TEM) showed that the prepared particles were spherical in shape. The size and size distribution were found to be submicron and ranging from 150 to 400 nm.
制备含有活性分子的可生物降解纳米粒子现在引起了研究人员的极大关注。本工作的目的是首次通过双乳液(W1/O/W2)蒸发法,使用高性能搅拌装置将亲水性物质封装到纳米颗粒中。荧光稳定的亲水性试剂(芪衍生物)被用作被包封的模型药物。为此,在本研究中选择了 PCL(聚己内酯)作为聚合物。研究了几种稳定剂[曲通 405、吐温 80、泊洛沙姆、PVP(聚乙烯吡咯烷酮)、PEG(聚乙二醇)和 PVA(聚乙烯醇)],结果表明 PVA(0.5%浓度)导致具有纳米级粒径的最稳定的双乳液。研究了影响颗粒尺寸的不同参数,如搅拌时间(第 1 和第 2 乳液)、搅拌速度(第 1 和第 2 乳液)、聚合物和稳定剂浓度等。一个月后,使用 U.V.分析估计了获得的颗粒的包封效率。透射电子显微镜(TEM)显示,所制备的颗粒呈球形。发现粒径和粒径分布为亚微米级,范围为 150 至 400nm。