研究动态
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从发现到评估和设计的结构制药学的进展。

Advances in Structure Pharmaceutics from Discovery to Evaluation and Design.

发表日期:2023 Aug 08
作者: Huipeng Xu, Li Wu, Yanling Xue, Ting Yang, Ting Xiong, Caifen Wang, Siyu He, Hongyu Sun, Zeying Cao, Jun Liu, Siwen Wang, Zhe Li, Abid Naeem, Xianzhen Yin, Jiwen Zhang
来源: MOLECULAR PHARMACEUTICS

摘要:

药物传递系统(DDSs)在以预设计的释放模式将活性药物成分(APIs)运输至目标部位中起着重要作用。对APIs和赋形剂的化学和生物性质进行了大量研究以评估DDS质量和效力,然而DDS的结构特性尚未得到充分探索。结构药学研究DDS的结构特征,尤其是三维结构,以及其与生物体的生理和病理结构的相互作用,可能影响其释放动力学和定位能力。我们提供了对多种剂型(如片剂、颗粒、小球、微球、粉末和纳米颗粒)结构的系统概述。此外,我们还讨论了结构对DDS释放和定位能力的影响,特别是不同结构颗粒的体外和体内释放相关性以及基于结构的器官和肿瘤定位能力。此外,我们还提供了关于DDS设计和评估中结构策略应用的深入讨论。此外,我们还简要描述了结构药学中一些常用的表征技术及其潜在的未来应用。
Drug delivery systems (DDSs) play an important role in delivering active pharmaceutical ingredients (APIs) to targeted sites with a predesigned release pattern. The chemical and biological properties of APIs and excipients have been extensively studied for their contribution to DDS quality and effectiveness; however, the structural characteristics of DDSs have not been adequately explored. Structure pharmaceutics involves the study of the structure of DDSs, especially the three-dimensional (3D) structures, and its interaction with the physiological and pathological structure of organisms, possibly influencing their release kinetics and targeting abilities. A systematic overview of the structures of a variety of dosage forms, such as tablets, granules, pellets, microspheres, powders, and nanoparticles, is presented. Moreover, the influence of structures on the release and targeting capability of DDSs has also been discussed, especially the in vitro and in vivo release correlation and the structure-based organ- and tumor-targeting capabilities of particles with different structures. Additionally, an in-depth discussion is provided regarding the application of structural strategies in the DDSs design and evaluation. Furthermore, some of the most frequently used characterization techniques in structure pharmaceutics are briefly described along with their potential future applications.