Abstract
AbstractAs the direct entrapment of camptothecin (CPT) into conventionally used polymeric materials is extremely difficult due to its high crystallization property, CPT‐derived prodrugs are widely used to increase drug‐polymer compatibility. However, the rapid CPT conversion from prodrugs is still a challenge due to the high steric hindrance around the hydroxyl of CPT. To address this, we reported here a fragile lactyl carbonate (LC) linker, which could be instantly cleaved to release CPT from LC‐linked lipophilic prodrugs under physiological conditions. Furthermore, such instantly‐cleaved CPT prodrugs could be stably encapsulated in methoxy poly(ethylene glycol)‐block‐poly(actic acid) (mPEG‐PLA) micelles, thus to achieve indirect CPT entrapment with a potent in vitro cytotoxicity as a result of the rapid CPT conversion. The strategy of entrapping instantly‐cleaved prodrugs in polymeric micelles displayed an excellent potential to broaden the scope of application of polymeric materials in drug delivery.
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