Amphiphilic hexadecyl-quaternized chitin micelles for doxorubicin delivery

A series of amphiphilic chitin derivatives were synthesized by conjugating hexadecyl groups (degree of substitute of hexadecyl groups (DS_H) = 0.11, 0.18, and 0.24) onto the backbone of quaternized chitins (degree of substitute of quaternary ammonium groups (DS_Q) = 0.36). The amphiphilic chitin derivatives could self-assemble into cationic micelles with hydrophobic alkyl side chain as core and hydrophilic quaternary ammonium groups as shell in deionized water. The biocompatible cationic micelles with an average particle size of 332.4-385.0 nm showed a drug loading content (DLC) of 10.2%-15.1%. The release behavior of DOX from micelles strongly depended on the DS_H values of chitin derivatives. DOX-loaded micelles effectively inhibited the growth of HepG2 cells through being internalized into HepG2 cells, and releasing DOX into the cytoplasm and nucleus. This work presented a novel chitin-based nanocarrier for potential chemotherapy.