Sunoqrot Suhair, Hamed Rania, Abdel-Halim Heba, Tarawneh Ola
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, P.O. Box 130, Amman 11733, Jordan.
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan.
Curr Top Med Chem. 2017;17(13):1451-1468. doi: 10.2174/1568026616666161222111656.
Over the last few decades, nanotechnology has given rise to promising new therapies and diagnostic tools for a wide range of diseases, especially cancer. The unique properties of nanocarriers such as liposomes, polymeric nanoparticles, micelles, and bioconjugates have mainly been exploited to enhance drug solubility, dissolution, and bioavailability. The most important advantage offered by nanotechnology is the ability to specifically target organs, tissues, and individual cells, which ultimately reduces the systemic side effects and improves the therapeutic index of drug molecules. The contribution of medicinal chemistry to nanotechnology is evident in the abundance of new active molecules that are being discovered but are faced with tremendous delivery challenges by conventional formulation strategies. Additionally, medicinal chemistry plays a crucial role in all the steps involved in the preparation of nanocarriers, where structure-activity relationships of the drug molecule as well as the nanocarrier are harnessed to enhance the design, efficacy, and safety of nanoformulations. The aim of this review is to provide an overview of the contributions of medicinal chemistry to nanotechnology, from supplying drug candidates and inspiring high-throughput nanocarrier design strategies, to structure-activity relationship elucidation and construction of computational models for better understanding of nanocarrier physicochemical properties and biological behavior. These two fields are undoubtedly interconnected and we will continue to see the fruits of that communion for years to come.
在过去几十年里，纳米技术催生了一系列前景广阔的新疗法和诊断工具，可用于治疗多种疾病，尤其是癌症。脂质体、聚合物纳米颗粒、胶束和生物偶联物等纳米载体的独特性质主要被用于提高药物的溶解度、溶出度和生物利用度。纳米技术最重要的优势在于能够特异性地靶向器官、组织和单个细胞，这最终减少了全身副作用并提高了药物分子的治疗指数。药物化学对纳米技术的贡献体现在大量新活性分子的发现上，但这些分子面临着传统制剂策略带来的巨大递送挑战。此外，药物化学在纳米载体制备的所有步骤中都起着关键作用，在这些步骤中，药物分子以及纳米载体的构效关系被用于增强纳米制剂的设计、疗效和安全性。本综述的目的是概述药物化学对纳米技术的贡献，从提供候选药物和启发高通量纳米载体设计策略，到阐明构效关系和构建计算模型以更好地理解纳米载体的物理化学性质和生物学行为。这两个领域无疑是相互关联的，在未来的岁月里，我们将继续看到这种交融所带来的成果。
