Developing cost-effective and targeted drug delivery system for antitumor therapy still remains a great challenge. We here report a facile method to modify laponite (LAP) nanodisks with polyethylene glycol-linked folic acid (PEG-FA) for targeted delivery of doxorubicin (DOX) to tumor site. In this study, LAP was first silanized to render its surface with abundant amine groups. Then PEG-FA with one end of carboxyl group was conjugated with LAP surface amines via 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) chemistry. Finally the formed LM-PEG-FA nanodisks were used to physically encapsulate DOX for in vitro and in vivo targeted therapy of cancer cells overexpressing FA receptors (FAR). We show that LM-PEG-FA is able to encapsulate DOX with a high loading efficiency of 88.6 ± 1.2 %, and the formed LM-PEG-FA/DOX complexes display a pH-dependent sustained release profile with a higher release rate at an acidic pH condition (pH 5.0) than at a physiological pH condition (pH 7.4). In vitro flow cytometry and confocal microscopic studies reveal that LM-PEG-FA/DOX complexes are able to target FAR-overexpressing human ovarian cancer cells (SK-OV-3 cells). Further cell viability assay and in vivo tumor treatment results reveal that the LM-PEG-FA/DOX complexes can exert a specific therapeutic efficacy to cancer cells in vitro and a xenografted tumor model in vivo. Therefore, the developed LM-PEG-FA nanodisks may be used as a promising platform for targeted cancer therapy.

Laponite nanodisks modified with folic acid via a PEG spacer as a platform for anticancer drug loading, release, and chemotherapy of tumors

251st National Meeting (2016)

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