基于水溶性杯芳烃的超分子体系在药物传递中的应用

Application of Water-soluble Calixarene-based Supramolecular Macrocycles in Drug Delivery

杯芳烃是第三代超分子大环主体,具有合成简单,易于功能化修饰,空腔大小可调控等优势,其与客体分子基于非共价键作用的结合具有改善疏水性药物溶解度,提高生物利用度,降低毒性和刺激性等作用。分子组装的特性赋予了杯芳烃在一定条件下形成不同形态纳米聚集体的能力,为药物传递提供了新的思路。本文基于超分子大环的2种核心作用,即主客体络合和分子组装,对水溶性杯芳烃构筑的药物传递系统进行介绍,综述了近10年来该类药物传递系统在改善难溶性药物溶解度,增加药物生物利用度、靶向性、减少不良反应发生率及其他方面的应用。

As the representative supramolecular macrocycles of third generation,calixarene has the advantages of simple synthesis,easy functional modification and adjustable cavity size.The noncovalent interactions of host and guest exhibited several advantages in improving solubility of hydrophobic drugs,improving bioavailability,and decreasing toxicity or irritation.The characteristics of molecular assembly supply the calixarene with the ability to form different nano aggregates,which provides a new idea for drug delivery.Based on the two core functions of supramolecular macrocycles,host guest complexation and molecular assembly,the review elaborates on the research progress of water-soluble calixarene-based drug delivery system with nano structures and the applications,et al,in improving the solubility,increasing the bioavailability and targeting of antitumor drugs,reducing the rate of adverse reaction,et al,in recent 10 years.