Abstract

A cationic anticancer drug, doxorubicin (DOX), was intercalated into layered double hydroxide (LDH) with an anionic polymer (polyacrylic acid (PAA)) to introduce the advantages of LDH as a drug carrier to DOX. Through X-ray diffraction patterns, Fourier-transform-infrared spectra, zeta-potential and X-ray photoelectron spectra showed that, PAA and DOX were intercalated in LDH interlayers through electrostatic stabilization between the carboxylate of PAA and LDH layer and between the carboxylate PAA backbone and DOX. Scanning electron microscopic images and dynamic light scattering results revealed that the DOX-PAA-LDH hybrid showed a favorable size for cellular uptake and enhanced permeability and retention, with a ~ 300 nm hydrodynamic radius and ~ 160 nm primary particle size. According to the bio-transmission electron microscopic images and confocal microscopic images, the DOX-PAA-LDH hybrid continuously provides drugs to endosomal cells during endocytosis and exocytosis. In accordance with these results, DOX-PAA-LDH showed improved anticancer activity against human osteosarcoma cells (MG-63) and human lung adenocarcinoma epithelial cells (A549) due to the advantages of LDH as a drug carrier.

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