Wang Fengling, Chen Jin, Dai Wenting, He Zhengmin, Zhai Dandan, Chen Weidong
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Acta Pharm. 2017 Sep 1;67(3):357-371. doi: 10.1515/acph-2017-0021.
In order to investigate the potential of nanostructured lipid carriers for efficient and targeted delivery of curcumin, the pharmacokinetic parameters of curcumin-loaded nanostructured lipid carriers (Cur-NLC) were evaluated in rats after a single intraperitoneal dose of Cur-NLC. In addition, the anticancer activity of Cur-NLC against human lung adenocarcinoma A549 cells was verified by a cellular uptake study, and a cytotoxicity and apoptosis assay. Bioavailability of Cur-NLC was better than that of native curcumin (p > 0.01), as seen from the area under the plasma concentration-time curve (AUC), maximum plasma concentration (Cmax), mean residence time (MRT) and total plasma clearance (CLz/F). Cur-NLC has a more obvious lung-targeting property in comparison with native curcumin. Cur-NLC showed higher anticancer activity in vitro against A549 cells than native curcumin (IC50 value of 5.66 vs. 9.81 mg L-1, respectively). Meanwhile, Cur-NLC treated A549 cells showed a higher apoptosis rate compared to that of native curcumin. These results indicate that NLC is a promising system for the delivery of curcumin in the treatment of lung adenocarcinoma.
为了研究纳米结构脂质载体用于姜黄素高效靶向递送的潜力,在大鼠单次腹腔注射姜黄素负载纳米结构脂质载体(Cur-NLC)后,评估了Cur-NLC的药代动力学参数。此外,通过细胞摄取研究、细胞毒性和凋亡测定,验证了Cur-NLC对人肺腺癌A549细胞的抗癌活性。从血浆浓度-时间曲线下面积(AUC)、最大血浆浓度(Cmax)、平均驻留时间(MRT)和总血浆清除率(CLz/F)来看,Cur-NLC的生物利用度优于天然姜黄素(p>0.01)。与天然姜黄素相比,Cur-NLC具有更明显的肺靶向特性。Cur-NLC在体外对A549细胞的抗癌活性高于天然姜黄素(IC50值分别为5.66和9.81 mg L-1)。同时,与天然姜黄素相比,Cur-NLC处理的A549细胞显示出更高的凋亡率。这些结果表明,纳米结构脂质载体是一种有前途的姜黄素递送系统,可用于治疗肺腺癌。