中文摘要：

癌症等恶性增殖疾病的靶向治疗有赖于靶向药物传递系统（targeteddrugdeliverysystem，TDDS）的开发。环糊精具有低毒、易修饰等优良性质，并可通过与药物分子形成包合物而提高药物的溶解性、稳定性、安全性和生物利用度等，因而具有成为优秀药物载体的潜力。环糊精不仅可以以其本身或修饰环糊精的形式充当载体，还可通过聚轮烷、阳离子聚合物或纳米粒等形式构建有效的药物载体。肿瘤或人体某些病变部位的细胞表面存在过度表达的生物受体如叶酸受体、去唾液酸糖蛋白受体、透明质酸受体、转铁蛋白受体和整合素受体等，可以与其相应的配体产生特异性识别。用适当的化学方法将配体分子如叶酸、单糖或寡糖、透明质酸、转铁蛋白及RGD肽等键接在基于环糊精的载体上，可形成具有靶向性质的药物载体，进而与药物分子一起构筑靶向药物传递系统。这种药物传递系统不仅针对于化学治疗药物，在核酸传递中也得到了丰富的应用。本文综述了基于环糊精的靶向药物传递系统的靶向机理及最新研究进展，并对其发展前景作了展望。

英文摘要：

Targeted drug delivery system （TDDS） nowadays has been adopted as a superb approach to the therapies of cancer and other mortal diseases. Cyclodextrins （CDs） are chosen to take the part of a promising drug carrier due to its low toxicity and high flexibility of structure modification. They are commonly used to enhance the aqueous solubility, chemical stability, safety and bioavailability of drugs in virtue of their peculiar ability to form CD/drug inclusion complexes. Not only native and chemically modified cyclodextrins were employed as drug carriers, but also sorts of CD-based more sophisticated carrier systems such as polyrotaxanes/ polypseudorotaxanes, polycations and nanoparticles emerged in recent years. Considering the fact that lots of biological receptors such as folate receptor, asialoglycoprotein receptor, hyaluronic receptor, transferrin receptor, integrin receptor are overexpressed on the surface of most cancer cells and other focal ceils, design of TDDS containing matching targeting ligands （TLs） could help realize targeted therapy for those focal cells or tissues. Targeting ligands such as folic acid （FA）, mono- and oligosaccharides, hyaluronic acid （HA）, transferrin, RGD sequence are consequently chemically bound to CD-based carriers to form targeted carrier systems whichfurther furnished TDDS via non-covalent complexation or bio-cleavable conjugation to drug molecules. Such TDDS are also widely applied on nucleic acid delivery in addition to chemotherapeutical drugs. As to depict the important developments, basic targeting principles and the latest progress on targeted drug delivery systems based on CDs are summarized, and also a brief prospect is given in this review.