Abstract
This study describes the effect of the core crosslinking degree on drug release from block copolymer crosslinked nanoassemblies (CNAs) to which an anticancer drug (doxorubicin: DOX) was conjugated through an acid-sensitive hydrazone linker. The CNAs were synthesized from poly(ethylene glycol)-poly(aspartate hydrazide) (PEG-Hyd) block copolymers comprising 5 kDa PEG and 33 repeating units of Hyd. Three types of CNAs were prepared at a core crosslinking degree of 13, 21, and 41%, entrapping 39, 37, and 30 wt% of DOX, respectively. CNAs were 30 - 34 nm in diameter and retained the particle size after drug entrapment. A monophasic curve fitting showed that CNAs accelerated drug release at pH 5.0 by 1.78 - 3.91 fold with respect to pH 7.4 depending on the core crosslinking degree. Further kinetic analysis revealed that drug release from the CNAs was biphasic, combining fast and slow drug release stages, and suggested that drug molecules interact with the CNA core as they escape from the particle. The core crosslinking degree was confirmed to modulate drug release rates mainly in the slow release stage in an acidic condition. Taken together, this study provides a better understanding of pH-controlled drug release from block copolymer nanoassemblies with a crosslinked core. © Global Scientific Publishers 2013.
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