Most current strategies of drug delivery systems face momentous challenges owing to obvious biological barriers. It is urgently necessary to develop artificial nanocarriers with biological and physical properties to reduce the severe system cytotoxicity of chemical drugs. Herein, triggered by the stiffness and amphiphilicity of the triple helix β-glucan (LNT), we developed a novel nanocarrier with the hydrophobic cavity for delivering the anti-cancer drug of doxorubicin. In our findings, based on the law of minimum surface energy, LNT with considerable chain stiffness self-assembled into nanotubes (LNT-NT) with the controlled hydrophobic nanotube diameter at the nanometer level positively depending on the molecular weight through hydrogen bonding and hydrophobic interaction in manners of "shoulder-to-shoulder" and "head-to-head" arrangements. The hydrophobic drug of doxorubicin was then demonstrated to be entrapped into LNT-NT through hydrophobic interaction. Doxorubicin loaded into LNT-NT nanocarriers significantly inhibited tumor growth in vitro and in vivo by promoting tumor cell apoptosis and blocking cell proliferation, showing a higher therapeutic efficacy of 74.5 % and less adverse effects than the free doxorubicin, which was ascribed to the enhanced targetability by LNT-NT. In conclusion, this work proposes an alternative strategy for delivering hydrophobic drugs to reduce cytotoxicity and enhance therapeutic effectiveness by constructing β-glucan-based nanotubes as a promising nanocarrier.
Keywords: Anti-cancer; Nanocarrier; Nanotube; Self-assemble; Triple helix β-glucan.
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