In this study, a novel micellar
drug carrier was fabricated from an amphiphilic diblock copolymer containing poly (
ethylene glycol) monomethyl ether (
mPEG) and stearic moiety (C18) with a linkage of
valine-
citrulline (VC), which can be cleaved by
cathepsin B (CB) enriched in lysosome of
tumor cell. Moreover, the self-assembled
micelles were observed as ellipsoid shape with major and minor axis of ca. 169 and 103nm, respectively. Such
drug carrier was used to encapsulate anti-
cancer drug doxorubicin (DOX), and hence showed a faster drug release behavior in a mimic lysosome condition containing
cathepsin B. It was ascribed to the lysosome-sensitivity of the
valine-
citrulline linkage, which was verified by the size distribution curve shifted to greater size under the same mimic lysosome condition. Furthermore, in comparison with pristine
doxorubicin, the encapsulation strategy of as-fabricated micellar carrier resulted in a predominant decrease of cytotoxicity. On the whole, a micellar
drug carrier, which can be disassembled by
cathepsin B, has been emerging as a potential of specific drug release in lysosome. Additionally, the controlled nanoscale together with elongated structure of such assembled ellipsoid
micelles might contribute passive targeting function to
tumor tissue and faster cellular uptake behavior (Zhou et al.).