纳米悬浮液(NS),它们是纳米大小的胶体颗粒系统,最近已成为纳米药物中最有趣的物质之一。NS具有高的商业潜力,因为它们通过其小的粒径和大的表面积提供低水溶性药物的增强的溶解度和溶解。此外,它们可以改变药物的药代动力学,因此,提高其疗效和安全性。这些优点可用于提高口服难溶性药物的生物利用度,真皮,肠胃外,肺,眼,或全身或局部影响的鼻途径。尽管NS通常主要由水介质中的纯药物组成,它们还可以含有稳定剂,有机溶剂,表面活性剂,助表面活性剂,冷冻保护剂,渗透剂,和其他组件。稳定器类型的选择,如表面活性剂或/和聚合物,它们的比例是NS配方中最关键的因素。NS可以用自上而下的方法制备(湿磨,干磨,高压均质化,和共研磨)和自下而上的方法(反溶剂沉淀,液体乳液,和声波沉淀)由研究实验室和制药专业人员提供。如今,结合这两种技术的技术也经常遇到。NS可以液体剂型提供给患者,或后期生产过程(冷冻干燥,喷雾干燥,或喷雾冷冻)也可以用于将液态转化为固态,以制备不同的剂型,例如粉末,颗粒,片剂,胶囊,电影,或凝胶。因此,在NS配方的开发中,成分/金额,制备方法,工艺参数/水平,管理路线,和剂型必须定义。此外,应确定和优化对预期用途最有效的因素。这篇综述讨论了配方和工艺参数对NSs性能的影响,并强调了最新进展,新颖的策略,以及与将NS应用于各种给药途径有关的实际考虑。
Nanosuspensions (NSs), which are nanosized colloidal particle systems, have recently become one of the most interesting substances in nanopharmaceuticals. NSs have high commercial potential because they provide the enhanced solubility and dissolution of low-water-soluble drugs by means of their small particle sizes and large surface areas. In addition, they can alter the pharmacokinetics of the drug and, thus, improve its efficacy and safety. These advantages can be used to enhance the bioavailability of poorly soluble drugs in oral, dermal, parenteral, pulmonary, ocular, or nasal routes for systemic or local effects. Although NSs often consist mainly of pure drugs in aqueous media, they can also contain stabilizers, organic solvents, surfactants, co-surfactants, cryoprotectants, osmogents, and other components. The selection of stabilizer types, such as surfactants or/and polymers, and their ratio are the most critical factors in NS formulations. NSs can be prepared both with top-down methods (wet milling, dry milling, high-pressure homogenization, and co-grinding) and with bottom-up methods (anti-solvent precipitation, liquid emulsion, and sono-precipitation) by research laboratories and pharmaceutical professionals. Nowadays, techniques combining these two technologies are also frequently encountered. NSs can be presented to patients in liquid dosage forms, or post-production processes (freeze drying, spray drying, or spray freezing) can also be applied to transform the liquid state into the solid state for the preparation of different dosage forms such as powders, pellets, tablets, capsules, films, or gels. Thus, in the development of NS formulations, the components/amounts, preparation methods, process parameters/levels, administration routes, and dosage forms must be defined. Moreover, those factors that are the most effective for the intended use should be determined and optimized. This review discusses the effect of the formulation and process parameters on the properties of NSs and highlights the recent advances, novel strategies, and practical considerations relevant to the application of NSs to various administration routes.