School of Pharmaceutical Sciences, Zhengzhou University , Zhengzhou , PR China.
Drug Deliv. 2019 Dec;26(1):1017-1026. doi: 10.1080/10717544.2019.1672829.
Curcumin, a commonly used natural product for antitumor therapy, is unable to achieve full potential due to poor bioavailability. Based on our previous report of a novel delivery system for curcumin using functionalized single-walled carbon nanotubes by phosphatidylcholine and polyvinylpyrrolidone (SWCNT-Cur), we further evaluated SWCNT-Cur's performance and characteristics . SWCNT-Cur significantly increased the blood concentration of curcumin, up to 18-fold, in mice. And in a murine S180 tumor model, SWCNT-Cur exhibited significantly higher inhibition efficacy on tumor growth and no obvious toxicity in main organs. Moreover, photothermal therapy induced by SWCNT under near-infrared radiation further facilitated SWCNT-Cur to inhibit the tumor growth . In addition, solvent residue is negligible in SWCNT-Cur formulation, and hydrogen bonding was formed between void carriers and curcumin, as demonstrated by GC chromatograph and IR spectra. Furthermore, experiments of confocal microscopy and spectrofluorometer showed that SWCNT-Cur gave a six-fold higher uptake for curcumin compared to native curcumin in human prostate cancer PC-3 cells. In conclusion, curcumin delivery with functionalized SWCNT is a promising strategy to enhance anticancer activity by enhancing cell uptake and blood concentration, changing physicochemical properties of curcumin and combining phototherapeutic with chemotherapeutic effects.
姜黄素是一种常用于抗肿瘤治疗的天然产物,但由于生物利用度差,其尚未能充分发挥作用。基于我们之前关于使用磷脂酰胆碱和聚乙烯吡咯烷酮(SWCNT-Cur)对姜黄素进行新型递药系统的报道,我们进一步评估了 SWCNT-Cur 的性能和特性。SWCNT-Cur 可使小鼠血液中的姜黄素浓度显著增加,最高可达 18 倍。在 S180 荷瘤小鼠模型中,SWCNT-Cur 对肿瘤生长的抑制效果明显更高,而对主要器官无明显毒性。此外,SWCNT 在近红外辐射下的光热治疗也进一步促进了 SWCNT-Cur 抑制肿瘤生长。此外,SWCNT-Cur 制剂中溶剂残留可忽略不计,GC 色谱和 IR 光谱表明载体空穴与姜黄素之间形成了氢键。此外,共聚焦显微镜和荧光分光光度计实验表明,SWCNT-Cur 使姜黄素在人前列腺癌 PC-3 细胞中的摄取量增加了 6 倍,而天然姜黄素的摄取量则较低。综上所述,用功能化 SWCNT 递运姜黄素是一种很有前途的策略,可通过提高细胞摄取率和血液浓度、改变姜黄素的理化性质以及将光疗与化疗相结合来增强抗癌活性。