Department of Pharmacy, Dalian Skin Disease Hospital, Dalian, China.
Anticancer Drugs. 2023 Oct 1;34(9):1010-1017. doi: 10.1097/CAD.0000000000001484. Epub 2022 Dec 23.
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).
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.
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.
Our study highlights the unique EGCG-entrapped lipid-gelatin hybrid nanoparticles, which may be a powerful strategy for further cancer therapy.
制备新型核壳型脂质-明胶-表没食子儿茶素没食子酸酯（EGCG）杂化纳米粒（LGE-N），以提高 EGCG 的稳定性和抗肿瘤疗效。
采用一步双乳液法制备 LGE-N，其中 EGCG-明胶纳米粒在内相中通过胶凝作用形成并稳定。通过标准的 3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐法评估 EGCG 溶液（EGCG-S）和 LGE-N 的细胞毒性。
所得到的 LGE-N 呈球形，具有相对较高的包封效率（92.30±1.63%）、载药量（11.09±0.62%）和控释药物释放能力。体外细胞毒性研究表明，LGE-N 在 MCF-7（乳腺癌细胞系）细胞中的半数最大抑制浓度（IC50）低于 EGCG-S。当用荧光探针 Dir 标记时，LGE-N 在肿瘤中积累更多。此外，LGE-N 在 4T1 植入小鼠中以 5mg/kg 的剂量实现了强大的抗肿瘤疗效。
本研究强调了独特的 EGCG 包封脂质-明胶杂化纳米粒，这可能是进一步癌症治疗的有力策略。
