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AAPS PharmSciTech. 2012 Dec;13(4):1348-54. doi: 10.1208/s12249-012-9862-8. Epub 2012 Sep 28.

The improvement of the anticancer effect of a novel compound benzoic acid, 2-hydroxy-, 2-D-ribofuranosylhydrazide (BHR) loaded in solid lipid nanoparticles.

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  • 1Department of Chemistry, Tongji University, Siping Road 1239, Shanghai, 200092, People's Republic of China.


A novel drug delivery system consisting of benzoic acid, 2-hydroxy-, 2-D-ribofuranosylhydrazide (BHR)-loaded solid lipid nanoparticles (BHR-SLNs) was prepared using the emulsification-evaporation technique. The mean particle size of the BHR-SLNs measured by photon correlation spectroscopy was about 75 nm. BHR-SLN morphology was assessed by transmission electron microscopy and atomic force microscopy. The drug entrapment efficiency was 70.2%, as determined via Sephadex gel chromatography and high-performance liquid chromatography. Drug release assessment in vitro showed that BHR was gradually released from SLNs in a time-dependent manner. Furthermore, treatment of 293T and Hela cells with BHR-SLNs demonstrated that BHR-SLNs were less toxic to normal cells while more effective in antitumor potency compared with the BHR drug alone. The results imply that BHR-SLNs could be considered as a promising antitumor drug system for a range of new therapeutic applications.

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