Liao Jie, Liu Bo, Liu Jun, Zhang Jiani, Chen Ke, Liu Huixia
Central South University, Xiang Ya Hospital , Changsha , China.
Expert Opin Drug Deliv. 2015 Mar;12(3):493-506. doi: 10.1517/17425247.2015.966681. Epub 2014 Nov 28.
Aptamers are short, single-stranded DNA or RNA sequences that can fold into complex secondary and tertiary structures and bind to various target molecules with high affinity and specificity. These properties, as well as rapid tissue penetration and ease of chemical modification, make aptamers ideal recognition elements for in vivo targeted drug delivery and attractive molecules for use in disease diagnosis and therapy.
The general properties of aptamers as well as advantages over their counterpart antibodies are briefly discussed. Next, aptamer selection by cell- systematic evolution of ligands by exponential enrichment is described in detail. Finally, the review summarizes recent progress in the field of targeted drug delivery based on aptamers and their conjugation to liposomes, micelles and other nanomaterials.
Advances in nanotechnology have led to new and improved nanomaterials for biomedical applications. Conjugation of nanoparticles (NPs) with aptamers exploits both technologies, making aptamer-NP conjugates ideal agents for drug delivery with proven therapeutic effects and the reduction of toxicity to normal tissue. The use of multivalent aptamer-conjugated nanomaterials represents one of the new directions for drug development in the future; as such, continuing studies of these multivalent aptamers and bioconjugates should result in important clinical applications in targeted drug delivery.
适配体是短的单链DNA或RNA序列，能够折叠成复杂的二级和三级结构，并以高亲和力和特异性与各种靶分子结合。这些特性，以及快速的组织穿透性和易于化学修饰的特点，使适配体成为体内靶向药物递送的理想识别元件，以及用于疾病诊断和治疗的有吸引力的分子。
简要讨论了适配体的一般特性及其相对于对应抗体的优势。接下来，详细描述了通过指数富集的配体细胞系统进化来选择适配体。最后，本综述总结了基于适配体及其与脂质体、胶束和其他纳米材料偶联的靶向药物递送领域的最新进展。
纳米技术的进步带来了用于生物医学应用的新型和改进的纳米材料。纳米颗粒（NPs）与适配体的偶联利用了这两种技术，使适配体-NP偶联物成为具有已证实治疗效果和降低对正常组织毒性的理想药物递送剂。使用多价适配体偶联的纳米材料代表了未来药物开发的新方向之一；因此，对这些多价适配体和生物偶联物的持续研究应会在靶向药物递送中产生重要的临床应用。
