Glucosamine derivative modified nanostructured lipid carriers for targeted tumor delivery

Abstract

Stearyl-2-amino-2-deoxyglucose (2-DG) modified nanostructured lipid carriers (NLC) were developed as novel vehicles for tumor-targeted delivery. The NLC were prepared using a melted-ultrasonic method, with glyceryl monostearate (MS) as a solid lipid and oleic acid (OA) as a liquid lipid. The physical properties of the NLC, including particle size, zeta potential, surface morphology, crystal structure, and storage stability, were characterized by standard methods. 2-DG, a glucosamine derivative, serving as a broad tumor targeting ligand, was conjugated to the surface of NLC (2-DG-NLC) for targeted delivery. Fluorescent dyes (fluorescein and cypate) and anticancer drug (paclitaxel, PTX) were used as model drugs to optimize the constituents of the NLC for drug entrapment efficiency and in vitrodrug release. The dynamic behavior of 2-DG-NLC in normal mice was investigated with a near infrared (NIR) fluorescence imaging system. The in vitro and in vivo tumor targeting capabilities of 2-DG-NLC were evaluated in MCF-7 tumor cells and tumor bearing mice, respectively. Results demonstrated that 2-DG-NLC actively and efficiently accumulated at the site of the tumor. Paclitaxel encapsulated 2-DG-NLC (2-DG-PTX-NLC) had good antitumor effectiveness and low toxicity in MCF-7 tumor bearing mice. The study indicates the broad potential of this carrier for tumor diagnosis as well as for targeted chemotherapy.