Drug Delivery 2011-01-01

Anti-inflammatory activity of injectable dexamethasone acetate-loaded nanostructured lipid carriers.

Xuefan Xu, Chunyan Zhao, Hongyun Yang, Yanlin Jian, Zhirong Zhang, Yuan Huang

Index: Drug Deliv. 18(7) , 485-92, (2011)

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Abstract

This work studied the intravenous injection formulation of nanostructured lipid carriers (NLCs) loaded with dexamethasone acetate (DA), a poorly water-soluble drug. The goal of this study was to design nanoparticles which could improve therapeutic efficacy of DA on inflammations. Based on the optimized results of single-factor screening experiment, DA-loaded NLCs (DA-NLCs) prepared by an emulsification-ultrasound method were found to be relatively uniform in size (178 ± 4 nm) with a negative zeta potential (-38 ± 4 mV). The average drug entrapment efficiency was 91 ± 3 %. In vitro release tests indicated DA-NLCs possessed a sustained release characteristic and the accumulative release percentage was near 80 % at 23 h. DA-NLCs exhibited an average peak concentration of DA (7.6 μg/ml) in the pleural exudate after intravenous administration to an experimental model of γ-carrageenan-induced pleuritis rats, which was 8.3 times higher than that of free DA (0.9 μg/ml). The γ-carrageenan-induced edema test showed that the anti-acute inflammatory activity of DA-NLCs was stronger than that of free drug at the same drug concentration (P<0.05). In addition, biodistribution results clearly indicated that DA-NLCs preferentially accumulated in mice livers and lungs after intravenous injection. These results revealed that injectable NLCs may serve as a promising carrier for DA, greatly enhancing the selective effect on inflammatory sites, reducing systematic side effects and may be a potential carrier to increase therapeutic efficacy on inflammatory diseases.