Single-step assembly of lipid-gelatin-epigallocatechin-3-gallate hybrid nanoparticles for cancer therapy.

OBJECTIVE

Novel core-shell lipid-gelatin-epigallocatechin-3-gallate hybrid nanoparticles (LGE-N) were prepared to increase the stability and antitumor efficacy of epigallocatechin-3-gallate (EGCG).

METHODS

The LGE-N was prepared by a single-step double-emulsion method, in which EGCG-gelatin nanoparticles were formed and stabilized in the inner phase by gelatinization. The cytotoxicity of EGCG solution (EGCG-S) and LGE-N were assessed by a standard 3-(4, 5-dimethylthiazol- 2-yl)-2, 5-diphenyltetrazolium bromide assay.

RESULTS

The obtained LGE-N had a spherical shape, with relatively high encapsulation efficiency (92.30 ± 1.63%), drug loading capacity (11.09 ± 0.62%) and controlled drug release. In-vitro cytotoxicity studies revealed that LGE-N exhibited a lower half maximal inhibitory concentration compared with EGCG-S in MCF-7 (a breast carcinoma cell line) cells. When labeled with a fluorescent probe, Dir, LGE-N was shown to accumulate much more in tumor. In addition, the LGE-N achieved potent antitumor efficacy at a dose of 5 mg/kg in 4T1-implanted mice.

CONCLUSION

Our study highlights the unique EGCG-entrapped lipid-gelatin hybrid nanoparticles, which may be a powerful strategy for further cancer therapy.