Controlled Systemic Release of Therapeutic Peptides from PEGylated Prodrugs by Serum Proteases
Controlled Systemic Release of Therapeutic Peptides from PEGylated Prodrugs by Serum Proteases
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DOI：
10.1002/anie.201301533
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发表时间：
2013-07-15
影响因子：
16.6
通讯作者：
Hoffmann, Ralf
中科院分区：
文献类型：
--
作者：
Nollmann, Friederike Inga;Goldbach, Tina;Hoffmann, Ralf
一种新的概念，即通过聚乙二醇化前体的血清蛋白酶系统地释放多肽药物，使得调节释放动力学以满足医学需要成为可能。药物释放取决于聚乙二醇聚合物的大小以及多肽连接物的序列和长度。前药的抗菌活性甚至强于游离肽，而直接聚乙二醇化使其失去了抗菌活性。
A novel concept to release peptidic drugs systemically by serum proteases from a PEGylated precursor makes it possible to tune release kinetics to fit the medical needs. Drug release depends on the size of the PEG polymer and the sequence and length of the peptide linker. The antimicrobial activities of the prodrugs were even better than those of the free peptides, whereas direct PEGylation abolished the peptide activity.