自组装多肽在新型药物制剂研发领域中的应用

Utility of the Self-assembling Peptides as Novel Drug Formulations

自组装多肽是一类具有特殊结构和功能的多肽分子,可以通过自组装的方式形成带有空腔的聚合物。利用这种特性,自组装多肽可以作为释药载体来改善药物的药学性质,例如提高药物的生物利用度,降低药物的毒性,增加药物的靶向性以及透膜性等,使药物更加适合临床需求。自组装多肽主要有两种,一种是基于多肽的空间结构进行自组装,另外一种是基于多肽的两亲性。主要就两亲性多肽自组装的特点及其在药物制剂研发领域中的应用进行阐述,并展望其在本领域的发展前景。

Self-assembled peptides possess distinct structural characterizations, inducing the formation of a stable supermolecule with a cavity. This central cavity was employed as drug carrier in last decade. The wide range utilities of self-assembled peptides covered the improved bioavailability, drug targeting release, cytotoxie alleviation, cell penetration activity and so on. There are two kinds of self-assembled peptide generally. One is based on the spatial structure of the peptide, and the other one is based on pepfide amphiphile. Amphiphilic peptide has four rationally designed chemical entities. By reasonable controlling the chemical structure, amphiphilic peptides can self-assemble into a variety of nanostructures, such as nanofiber, nanotube, nanoparticles and hydrogel. It is highlighted a kind of peptide that is cellular penetration peptide （CPP）. The mechanism of supermolecule formation and drug loading procedures was summarized. The remarkable functions of self-assembled peptides spread a prosperous scene in drug controlled release and drug sustained release.