Drug Delivery by an Enzyme-Mediated Cyclization of a Lipid Prodrug with Unique Bilayer-Formation Properties
作者:Lars Linderoth、Günther H. Peters、Robert Madsen、Thomas L. Andresen
DOI:10.1002/anie.200805241
日期:2009.2.23
Special delivery: Liposomal drug‐delivery systems in which prodrugs are activated specifically by disease‐associated enzymes have great potential for the treatment of severe diseases, such as cancer. A new type of phospholipid‐based prodrug has the ability to form stable small unilamellar vesicles (see picture). Activation of the prodrug vesicles by the enzyme sPLA2 initiates a cyclization reaction
特殊递送:脂质体药物递送系统中的前药被疾病相关的酶特异性激活,在治疗严重疾病(如癌症)方面具有巨大潜力。一种新型的磷脂基前药具有形成稳定的单层小囊泡的能力(见图)。sPLA 2酶激活前药囊泡会引发环化反应,从而导致药物释放。