Jin Gang, Wang Jie, Xu Jie, Jin Qing, Xue Jian-Fei, Li Lin-Han
School of Chemical and Pharmaceutical Engineering, Jilin Institute of Chemical Technology, Jilin 132022, PR China.
Party and Government Office, Jilin Institute of Chemical Technology, Jilin 132022, PR China.
Curr Drug Deliv. 2024 May 29. doi: 10.2174/0115672018299592240524074005.
Poor solubility of drugs leads to poor bioavailability and therapeutic efficiency. A large proportion of drugs that are not developed and marketed for use by patients are due to their extremely low solubility. Therefore, improving the solubility of poorly water-soluble drugs is one of the most important aspects of the field of drug research. With the continuous development of more and more formulation techniques and excipient applications, the solubility of poorly water-soluble drugs can be improved to a certain extent to obtain better pharmacokinetics and pharmacodynamics, including pH microenvironment regulation technology, inclusion complex, solid dispersion, nanotechnology, and application of surfactants. However, the most widely used among them is the application of surfactants. This technique can reduce the surface tension, improve wettability, and have a remarkable solubilizing ability after forming micelles. However, surfactants have also been found to possess certain limitations in solubilization. In this review, the factors affecting the solubilization of surfactants and limiting their application have been summarized from several aspects. These factors include drugs, additives, and media. Some ideas to solve these application limitations have also been put forward, which can lay a foundation for the wider application of surfactants in the future.
药物的低溶解度会导致生物利用度差和治疗效果不佳。很大一部分未被开发和推向市场供患者使用的药物是由于其极低的溶解度。因此,提高难溶性药物的溶解度是药物研究领域最重要的方面之一。随着越来越多制剂技术和辅料应用的不断发展,难溶性药物的溶解度可以在一定程度上得到提高,以获得更好的药代动力学和药效学,包括pH微环境调节技术、包合物、固体分散体、纳米技术以及表面活性剂的应用。然而,其中应用最广泛的是表面活性剂的应用。该技术可以降低表面张力,提高润湿性,并且在形成胶束后具有显著的增溶能力。然而,人们也发现表面活性剂在增溶方面存在一定的局限性。在这篇综述中,从几个方面总结了影响表面活性剂增溶作用并限制其应用的因素。这些因素包括药物、添加剂和介质。还提出了一些解决这些应用局限性的思路,可为表面活性剂在未来更广泛的应用奠定基础。