Laboratory of Organic and Macromolecular Chemistry (IOMC), Friedrich Schiller University Jena, Jena, Germany.
Jena Center for Soft Matter (JCSM), Friedrich Schiller University Jena, Jena, Germany.
Handb Exp Pharmacol. 2024;284:3-26. doi: 10.1007/164_2023_649.
Conventional drug delivery systems (DDS) today still face several drawbacks and obstacles. High total doses of active pharmaceutical ingredients (API) are often difficult or impossible to deliver due to poor solubility of the API or undesired clearance from the body caused by strong interactions with plasma proteins. In addition, high doses lead to a high overall body burden, in particular if they cannot be delivered specifically to the target site. Therefore, modern DDS must not only be able to deliver a dose into the body, but should also overcome the hurdles mentioned above as examples. One of these promising devices are polymeric nanoparticles, which can encapsulate a wide range of APIs despite having different physicochemical properties. Most importantly, polymeric nanoparticles are tunable to obtain tailored systems for each application. This can already be achieved via the starting material, the polymer, by incorporating, e.g., functional groups. This enables the particle properties to be influenced not only specifically in terms of their interactions with APIs, but also in terms of their general properties such as size, degradability, and surface properties. In particular, the combination of size, shape, and surface modification allows polymeric nanoparticles to be used not only as a simple drug delivery device, but also to achieve targeting. This chapter discusses to what extent polymers can be designed to form defined nanoparticles and how their properties affect their performance.
目前,传统的药物传递系统(DDS)仍然面临着一些缺点和障碍。由于 API 的溶解度差或由于与血浆蛋白的强烈相互作用而导致的不理想的清除,高剂量的活性药物成分(API)往往难以或不可能传递。此外,高剂量会导致全身负担增加,如果不能将其专门递送到靶部位,则尤其如此。因此,现代 DDS 不仅必须能够将剂量递送到体内,而且还应该克服上述障碍,例如。一种有前途的设备是聚合物纳米粒子,尽管具有不同的物理化学性质,但它可以封装广泛的 API。最重要的是,聚合物纳米粒子可以通过起始材料(即聚合物)进行调整,例如通过引入官能团来获得针对每种应用的定制系统。这不仅可以通过与 API 的相互作用来影响颗粒特性,还可以通过其一般特性(如尺寸、可降解性和表面特性)来影响颗粒特性。特别是,尺寸、形状和表面修饰的组合使得聚合物纳米粒子不仅可以用作简单的药物传递装置,还可以实现靶向传递。本章讨论了可以在多大程度上设计聚合物以形成定义明确的纳米粒子,以及它们的性质如何影响其性能。