【摘要】 为拓展和推动丝素蛋白材料在医药领域的临床应用，综述了近年来丝素蛋白在药物递送系统中的最新研究进展，重点阐述了丝素蛋白药物递送载体的种类、制备方法、主要的药物负载类型及其应用性能。通过分析发现：丝素蛋白除具有出色的生物相容性和可控降解性外，其大分子独特的亲疏水链结构还赋予丝素蛋白聚集态结构自组装的调控基础；以丝素蛋白为基材所构建的微球、水凝胶和微针等多种形貌的药物载体表现出高效的药物负载能力和可控的释放速率，从而达到患者减少服药次数和提高治疗效率的目的。除负载小分子化学药物，丝素蛋白载体还可改善蛋白和基因类药物易降解和半衰期短的缺点。由于丝素蛋白的这些优异特性，将其用于研制靶向与特异性药物载体可实现对不同类型疾病的针对性治疗，从而提高药物利用度和降低副作用。最后指出使用丝素蛋白作为药物载体存在的问题和重要的发展方向。更多还原

【Abstract】 Significance With the increasing incidence of chronic noncommunicable diseases(e.g. cancer), inflammation and diabetes, drug delivery systems with controlled release are developed and applied in clinical practice. Silk fibroin was studied widely for applications in the fields of tissue engineering and medicine because of its good biocompatibility and biodegradability. The research on the application of silk fibroin as drug carriers attracted much global attention. In order to expand and promote the clinical applications of silk fibroin materials in pharmaceutical field, this paper reviews the latest research progress of silk fibroin in drug delivery systems, with highlights on carrier types, preparation methods, drug loading types and application properties of silk fibroin drug delivery systems.Progress As a controlled drug carrier, silk fibroin is an ideal candidate because of its unique chemical structure and aggregated structure, and its excellent biocompatibility and controllable degradation. Silk fibroin materials can be prepared into various forms, among which silk fibroin materials in the form of microspheres, hydrogels and microneedles exhibit efficient drug loading capacity and controllable release rate when used as drug carriers, resulting in the decrease of dosing frequency and improvement of the therapeutic efficiency. Silk fibroin-based drug delivery system not only can stably encapsulate various small molecule compounds, but also deliver biological macromolecules such as proteins and nucleic acids. Composite drug carriers developed by combining other materials can reduce the degradation of silk fibroin drug carriers in vivo and improve the drug availability. Furthermore, the alternating arrangement of hydrophilic and hydrophobic chains of the silk fibroin macromolecule provides a structure basis for regulating the molecular conformation and aggregation structure of silk fibroin materials. The crystal form and crystallinity of silk fibroin can be regulated by physical or chemical modification to control drug release or endow targeting ability to diseased cells, which can effectively improve the therapeutic efficiency of serious diseases and reduce the damage to normal tissue cells.Conclusion and Prospect With the continuous exploration of the biological function of silk fibroin, some progress in silk fibroin-based drug release materials has been made in association with drug delivery forms, targeted therapy and drug availability. Silk fibroin as a drug carrier has been found to prolong the circulation time of drugs in the blood, reduce the frequency of drug use and alleviate adverse drug reactions of patients. These advantages provide important guidance for in-depth and sustainable development of silk fibroin in drug delivery application. However, there are still problems in the stability of the preparation of silk fibroin drug carriers and their drug loading capacity. The quality of silk fibroin varies greatly due to the different sources, such as varieties, seasons and regions. It is necessary to standardize the characteristics and extraction method of silk fibroin. Although silk fibroin drug carriers can be endowed with the capability of targeted drug delivery by physical or chemical modification, it may be attacked by the immune system at the initial stage of entering the body, leading to failure of targeted release. The accuracy and effectiveness of silk fibroin used as drug carriers still need long-term exploration and clinical trials. With the development of material science, chemical science and pharmacy, the research and application of silk fibroin-based drug delivery systems will be further continued.更多还原