多孔硅巯基化配合金属离子靶向释放阿霉素（DOX）
摘要
长久以来,癌症都是威胁人类健康的重大疾病之一。其中,化疗是一种常见癌症治疗手段,而化疗中常用的药物就有阿霉素（DOX），但由于这类抗癌药物的一些自身缺点,例如低靶向性和副作用强,其治疗结果往往差强人意。阿霉素( DOX) 为放线菌产生的蒽环类抗生素，是一种作用于 DNA 的药物，抗菌谱广，对多种肿瘤都有作用，广泛用于化学治疗。但长期使用阿霉素产生的蓄积性心脏毒性和肿瘤细胞对阿霉素产生的多药耐药性限制了阿霉素在临床上的应用。纳米载药系统具有增强肿瘤的EPR效应、减少游离药物的非特异毒性及延长药物的体循环时间,增强药物在作用部位的蓄积，提高药效等优点而成为逆转肿瘤多药耐药的有效逆转策略之一,所以找到一种良好的载体将药物精准的释放到人体病变处以解决这些缺陷是目前癌症治疗首要解决的问题。多孔硅纳米颗粒（PSiNPs）作为一种多功能纳米平台，在癌症的诊断和治疗方面表现出了优异的性能。PSiNPs具有多种外源有机分子、生物大分子、甚至纳米颗粒等的多功能负载能力，这是由于其可调的孔径和孔隙率、大的表面积和定制的表面功能化。与其他无机纳米材料相比，PSiNPs具有良好的生物相容性和生物降解性，在未来的临床应用中具有更大的潜力。但是此类药物并不能直接与多孔硅连接，需要对载体多孔硅进行表面处理，嫁接桥梁以便于和药物相结合。本实验是通过对多孔硅进行巯基化处理，再分别配位Fe等三种离子与DOX相结合，以提高多孔硅载药能力与靶向性。并测试了不同PH下药物的释放速度。
关键词：多孔硅，表面修饰，金属离子，配位，载药，DOX
Targeted release of doxorubicin (DOX) by porous silicon sulfhydrylization combined with metal ions
ABSTRACT
For a long time, cancer is one of the major diseases that threaten human health. Among them, chemotherapy is a common cancer treatment, and doxorubicin (DOX) is commonly used in chemotherapy. However, due to some of its own shortcomings, such as low targeting and strong side effects, its treatment results Often unsatisfactory. Doxorubicin (DOX) is an anthracycline antibiotic produced by actinomycetes. It is a drug that acts on DNA, has a broad antibacterial spectrum, has effects on a variety of tumors, and is widely used in chemotherapy. However, the accumulated cardiotoxicity caused by long-term use of doxorubicin and the multidrug resistance of tumor cells to doxorubicin have limited the clinical application of doxorubicin. Nano drug-loading system has the advantages of enhancing the tumor#39;s EPR effect, reducing the non-specific toxicity of free drugs, extending the systemic circulation time of drugs, enhancing the accumulation of drugs at the site of action, and improving drug efficacy, and has become an effective reversal strategy for reversing tumor multidrug resistance. One of the reasons is to find a good carrier to accurately release the drug to human lesions to solve these defects. Porous silicon nanoparticles (PSiNPs), as a multifunctional nano platform, have shown excellent performance in the diagnosis and treatment of cancer. PSiNPs have multifunctional loading capabilities for a variety of exogenous organic molecules, biological macromolecules, and even nanoparticles. This is due to their adjustable pore size and porosity, large surface area, and customized surface functionalization. Compared with other inorganic nanomaterials, PSiNPs have good biocompatibility and biodegradability, and have greater potential in future clinical applications. However, such drugs cannot be directly connected to porous silicon. Surface treatment of carrier porous silicon is required, and bridges are grafted to facilitate the combination with drugs. In this experiment, porous silicon was subjected to thiolation treatment, and then three kinds of ions, such as Fe, were combined with DOX to improve the drug-loading ability and targeting of porous silicon. The release rate of the drug at different pH was tested.
Key words: Porous silicon, surface modification, metal ion, coordination, drug loading, DOX
1.多孔硅
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