Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan.
Curr Pharm Des. 2013;19(35):6246-58. doi: 10.2174/1381612811319350003.
Nano-formulation of poorly water-soluble drugs has been developed to enhance drug dissolution. In this review, we introduce nano-milling technology described in recently published papers. Factors affecting the size of drug crystals are compared based on the preparation methods and drug and excipient types. A top-down approach using the comminution process is a method conventionally used to prepare crystalline drug nanoparticles. Wet milling using media is well studied and several wet-milled drug formulations are now on the market. Several trials on drug nanosuspension preparation using different apparatuses, materials, and conditions have been reported. Wet milling using a high-pressure homogenizer is another alternative to preparing production-scale drug nanosuspensions. Dry milling is a simple method of preparing a solid-state drug nano-formulation. The effect of size on the dissolution of a drug from nanoparticles is an area of fundamental research, but it is sometimes incorrectly evaluated. Here, we discuss evaluation procedures and the associated problems. Lastly, the importance of quality control, process optimization, and physicochemical characterization are briefly discussed.
已开发出将难溶性药物制成纳米制剂的方法，以提高药物的溶解度。在本综述中，我们介绍了最近发表的论文中描述的纳米研磨技术。基于制备方法和药物及赋形剂的类型，比较了影响药物晶体大小的因素。采用粉碎工艺的自上而下方法是传统上用于制备结晶药物纳米颗粒的方法。使用介质的湿法研磨研究得比较透彻，现在已有几种湿磨药物制剂上市。已经有报道使用不同的设备、材料和条件进行了药物纳米混悬液制备的多项试验。使用高压匀浆器的湿法研磨是另一种制备生产规模药物纳米混悬液的替代方法。干法研磨是制备固态药物纳米制剂的简单方法。药物从纳米颗粒中溶解的粒径效应是基础研究的一个领域，但有时评估不正确。在这里，我们讨论了评估程序和相关问题。最后，简要讨论了质量控制、工艺优化和物理化学特性的重要性。
