[关键词]
[摘要]
目的 构建姜黄素纳米递药系统(H-PtNP-Cur),旨在解决姜黄素水溶性差、生物利用度低的难题,使其发挥更好的抗肿瘤作用。方法 通过粒度电位分析仪和透射电子显微镜考察载体的粒度、电位和形态;稳定性实验考察了载体的稳定性;紫外可见分光光度法验证姜黄素对铂颗粒的吸附;透析法分析载药量及释放率;流式细胞仪分析HepG2细胞对纳米载体的摄取;MTT法考察纳米载体对HepG2细胞的毒性;细胞成像实验考察纳米载体对HepG2细胞的抑制情况。结果 成功合成了H-PtNP-Cur载体,其形态规整、大小均匀,测得粒径为(146.2±1.5)nm,电位(−;10.5±0.6)mV,载药量为 (12.4±2.7)%,包封率为(81.4±1.3)%,制备的载体稳定性较好,体外释放表明该载体可以控制姜黄素缓慢释放;细胞摄取结果表明纳米载体的构建有利于HepG2细胞的摄取;MTT实验说明纳米载体能够抑制HepG2细胞的生长;细胞成像实验证明H-PtNP-Cur对HepG2细胞的抑制率是最高的。结论 H-PtNP-Cur纳米递药系统可以有效抑制HepG2细胞生长,为肝癌的治疗提供新的思路。
[Key word]
[Abstract]
Objective To construct drug delivery system loaded with curcumin (H-PtNP-Cur) to solve weak solubility and low bioavailability of curcumin, achieving more effectively anti-tumor responses. Methods The particle size, Zeta potential, and morphology of the nanocarrier were investigated by Zetasizer (Nano ZS 90, Malvern) and transmission electron microscopy (TEM). The stability of the nanocarrier was investigated by stability experiments. UV-visible spectrophotometry was used to verify the adsorption of curcumin (Cur) on the Pt nanoparticles. The drug loading amount and release rate were analyzed by dialysis method using HPLC. The uptake of nanocarriers by HepG2 cells was analyzed by flow cytometry. The toxicity of nanocarriers to HepG2 cells was investigated by MTT assay. The inhibitory effect of nanocarriers on HepG2 cells was studied by cell imaging. Results The H-PtNP-Cur carrier was successfully prepared. The morphology of particles was regular and uniform. The particle size, Zeta potential, the drug loading amount, and entrapment efficiency were (146.2 ±1.5) nm, (−10.5 ±0.6) mV, (12.4 ±2.7)%, and (81.4 ±1.3)%, respectively. The prepared nanocarrier had good stability. The in vitro release results showed that the carrier could sustain the slow release of curcumin. The results of cellular uptake indicated that the nanocarriers promoted the uptake of HepG2 cells. The MTT assay indicated that the nanocarriers could significantly inhibit the growth of HepG2 cells than free curcumin. The cell imaging experiments showed that the inhibition rate of H-PtNP-Cur on HepG2 cells was the highest. Conclusion The H-PtNP-Cur has obvious inhibiting effects on the growth of HepG2 cells, which provides a new way for the treatment of liver cancer.
[中图分类号]
[基金项目]
抗体介导靶向缺血心肌的给药系统研究(QC2015130)