Rafati H, Mirzajani F
Department of Chemical Engineering, Medicinal Plants and Drugs Research Institute, Shahid Beheshti Univ., G.C., Evin, Tehran, Iran.
Pharmazie. 2011 Jan;66(1):31-6.
The therapeutic effects of anticancer drugs would highly improve if problems with low water solubility and toxic adverse reactions could be solved. In this work, a full factorial experimental design was used to develop a polymeric nanoparticulate delivery system as an alternative technique for anticancer drug delivery. Nanoparticles containing tamoxifen citrate were prepared and characterized using an O/W emulsification-solvent evaporation technique and different analytical methods. Scanning Electron Microscopy (SEM), particle size analysis and High Pressure Liquid Chromatography (HPLC) were used for characterization of nanoparticles. Nanoparticles' characteristics including size, size distribution, drug loading and the efficiency of encapsulation were optimized by means of a full factorial experimental design over the influence of four different independent variables and desirability function using Design-Expert software. The resulting tamoxifen loaded nanoparticles showed the best response with particle sizes less than 200 nm, improved encapsulation efficiency of more than 80% and the optimum loading of above 30%. The overall results demonstrate the implication of desirability functionin experimental design as a beneficial approach in nanoparticle drug delivery design.
如果能够解决抗癌药物水溶性低和毒性不良反应的问题，其治疗效果将得到显著提高。在这项工作中，采用全因子实验设计来开发一种聚合物纳米颗粒递送系统，作为抗癌药物递送的替代技术。使用O/W乳化-溶剂蒸发技术和不同的分析方法制备并表征了含柠檬酸他莫昔芬的纳米颗粒。扫描电子显微镜（SEM）、粒度分析和高压液相色谱（HPLC）用于纳米颗粒的表征。通过全因子实验设计，利用Design-Expert软件，在四个不同自变量的影响下，通过合意函数对纳米颗粒的特性（包括尺寸、尺寸分布、载药量和包封效率）进行了优化。所得载有他莫昔芬的纳米颗粒表现出最佳响应，粒径小于200nm，包封效率提高到80%以上，最佳载药量超过30%。总体结果表明，合意函数在实验设计中的应用是纳米颗粒药物递送设计中的一种有益方法。
