pH-Responsive nanoparticles based on cholesterol/imidazole modified oxidized-starch for targeted anticancer drug delivery.

Various nanoparticles have been developed for tumor-targeted drug delivery. However, nanoparticles with effective targeting and intelligent release capacity are still deficient. Herein, we present new pH-responsive and neutral charged nanoparticles for tumor-targeted anticancer drug delivery. Oxidized starch was synthesized and simultaneously modified by cholesterol and imidazole to obtain amphiphilic cholesterol/imidazole modified oxidized-starch (Cho-Imi-OS). Cho-Imi-OS easily self-assembled into nanoparticles by dialysis. Curcumin was selected as model drug to be encapsulated into the hydrophobic core of nanoparticles. The results showed that curcumin would effectively accumulate in cancer cells by encapsulating into the nanoparticles owing to the nano-sized structure and near neutral charged property of nanoparticles. Curcumin was released faster at pH 5.5 than that at pH 7.4 from the curcumin-loaded nanoparticles (Cur-NPs), indicating the pH-triggered release capacity of Cur-NPs after endocytosis by endosomes since the pH is low to 5.0∼6.0 in endosomes. Naturally, Cur-NPs showed significantly strong inhibitory effect on cancer cells.