AbouAitah Khaled, Lojkowski Witold
Laboratory of Nanostructures and Nanomedicine, Institute of High Pressure Physics, Polish Academy of Sciences, Sokolowska 29/37, 01-142 Warsaw, Poland.
Medicinal and Aromatic Plants Research Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), 33 El-Behouth St., Dokki, Giza 12622, Egypt.
Pharmaceutics. 2021 Jan 22;13(2):143. doi: 10.3390/pharmaceutics13020143.
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.
源自不同天然来源（如药用植物、微生物、动物）的天然前药在传统医学中有着悠久的历史。它们具有广泛的药理活性，包括在体外和体内的抗癌作用。它们有潜力成为安全、经济有效且副作用少的治疗方法，但存在溶解度、生物利用度、特异性靶向性不足以及半衰期短的问题。这些都是临床应用的障碍。纳米医学有潜力提供解决方案来规避这些限制，并使天然前药能够用于癌症治疗。各种形态的介孔二氧化硅纳米颗粒（MSN）在寻找靶向药物递送系统方面引起了相当大的关注。MSN的特点是化学稳定性好、易于合成和功能化、比表面积大、孔径和孔体积可调、生物相容性好、在不同条件下可控药物释放以及载药量高，可实现多功能用途。在体内临床前评估中，绝大多数结果表明，如果以优化方式合成，MSN具有安全性。在此，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、控释递送设计以及癌症靶向，并讨论基于抗癌纳米技术的天然前药递送系统的未来。
