A modified spontaneous emulsification solvent diffusion method for the preparation of curcumin-loaded PLGA nanoparticles with enhanced in vitro anti-tumor activity

Abstract

To improve the anti-tumor activity of hydrophobic drug curcumin, we prepared curcumin-loaded PLGA nanoparticles (PLGA-Cur NPs) through a modified spontaneous emulsification solvent diffusion (modified-SESD) method. The influence of main preparation parameters was investigated, such as the volume ratio of binary organic solvents and the concentration of surfactant. Results indicated that the synthesized regular spherical PLGA NPs with the average diameter of 189.7 nm exhibited relatively higher yield (58.9%), drug loading (11.0% (w/w)) and encapsulation efficiency (33.5%), and also a controllable drug release profile. In order to evaluate the in vitro cytotoxicity of the prepared NPs, MTT assay was conducted, and results showed that the NPs could effectively inhibit HL60 and HepG2 cells with lower IC₅₀ values compared with free curcumin. Furthermore, confocal microscopy together with flow cytometry analysis proved the enhanced apoptosis-inducing ability of PLGA-Cur NPs. Polymeric NP formulations are potential to be used for hydrophobic drug delivery systems in cancer therapy.

Keywords

curcumin / PLGA nanoparticle / modified spontaneous emulsification solvent diffusion (modified-SESD) / anti-tumor

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Acknowledgements

This work was supported by the National Natural Science Foundation of China (Grant Nos. 51272236 and 51002139), the Science Foundation of Zhejiang Sci-Tech University (Grant Nos. 13042158-Y, 0716687-Y and 0816833-Y), and the Zhejiang Provincial Top Key Discipline of Biology.

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2014 Higher Education Press and Springer-Verlag Berlin Heidelberg