适配体是一类能够与靶标特异性结合的DNA、RNA或多肽片段。具有相对分子质量小、生物相容性好、可化学合成等优点,目前适配体修饰技术逐步在基础医学研究、药物研发及临床肿瘤诊断与治疗领域得到应用。不少抗肿瘤药物水溶性差、生物利用度低以及非特异性的细胞毒性所产生的副作用严重阻碍癌症化疗。适配体具有高特异性、高亲和力的固有性质,纳米载体可增强药物的水溶性,提高生物利用度,大量适配体介导的纳米载体被开发用于肿瘤靶向治疗。本文主要介绍了适配体的起源、发展及其在肿瘤靶向中对纳米粒子的修饰。
Aptamers are a class of DNA, RNA and polypeptide fragments binding to different target specifically. Aptamers with small molecular weight, good biocompatibility and easy to synthesize have been extensively used in basic medical research, pharmaceutical study and clinical tumor diagnosis and treatment. The majority of anticancer drugs pos- sess the side effects of poor aqueous solubility, low bioavailability and nonspecific cytotoxicity, which poses a challenge to cancer chemotherapy. A large number of aptamer-modified nanocarriers have been developed for targeted cancer therapy not only because nanocarriers enhance the water-solubility as well as bioavailability, but also the inherent properties of high specificity and high affinity of aptamers. In this review, we will discuss the origin and development of aptamers and focus on the modification of aptamers to nanoparticles in targeting drug delivery system.