Natural prodrugs derived from different natural origins (e.g., medicinal plants, microbes, animals) have a long history in traditional medicine. They exhibit a broad range of pharmacological activities, including anticancer effects in vitro and in vivo. They have potential as safe, cost-effective treatments with few side effects, but are lacking in solubility, bioavailability, specific targeting and have short half-lives. These are barriers to clinical application. Nanomedicine has the potential to offer solutions to circumvent these limitations and allow the use of natural pro-drugs in cancer therapy. Mesoporous silica nanoparticles (MSNs) of various morphology have attracted considerable attention in the search for targeted drug delivery systems. MSNs are characterized by chemical stability, easy synthesis and functionalization, large surface area, tunable pore sizes and volumes, good biocompatibility, controlled drug release under different conditions, and high drug-loading capacity, enabling multifunctional purposes. In vivo pre-clinical evaluations, a significant majority of results indicate the safety profile of MSNs if they are synthesized in an optimized way. Here, we present an overview of synthesis methods, possible surface functionalization, cellular uptake, biodistribution, toxicity, loading strategies, delivery designs with controlled release, and cancer targeting and discuss the future of anticancer nanotechnology-based natural prodrug delivery systems.

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通过介孔二氧化硅纳米球递送天然药物作为有希望的抗癌策略

来自不同自然起源的天然前药（例如，药用植物，微生物，动物）在传统医学中历史悠久。它们表现出广泛的药理活性，包括体外和体内的抗癌作用。它们具有作为安全，具有成本效益的治疗方法且几乎没有副作用的潜力，但缺乏溶解性，生物利用度，特异性靶向性且半衰期短。这些是临床应用的障碍。纳米医学有潜力提供解决这些局限性的解决方案，并允许在癌症治疗中使用天然的前药。在寻找靶向药物递送系统时，各种形态的中孔二氧化硅纳米粒子（MSN）引起了相当大的关注。MSN具有化学稳定性，易于合成和功能化的特点，大表面积，可调节的孔径和体积，良好的生物相容性，在不同条件下可控制的药物释放以及高载药量，可实现多种用途。在体内临床前评估中，绝大部分结果表明，如果以优化的方式合成MSN，则它们的安全性。在这里，我们概述了合成方法，可能的表面功能化，细胞摄取，生物分布，毒性，负载策略，具有控释的递送设计和靶向癌症，并讨论了基于抗癌纳米技术的天然前药递送系统的未来。绝大多数结果表明，如果MSN以优化方式合成，它们的安全性。在这里，我们概述了合成方法，可能的表面功能化，细胞摄取，生物分布，毒性，负载策略，具有控释的递送设计和靶向癌症，并讨论了基于抗癌纳米技术的天然前药递送系统的未来。绝大多数结果表明，如果MSN以优化方式合成，它们的安全性。在这里，我们概述了合成方法，可能的表面功能化，细胞摄取，生物分布，毒性，负载策略，具有控释的递送设计和靶向癌症，并讨论了基于抗癌纳米技术的天然前药递送系统的未来。