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通过单壁碳纳米管递药系统增强姜黄素的抗肿瘤疗效和进一步光热消融肿瘤生长

Enhancement of curcumin antitumor efficacy and further photothermal ablation of tumor growth by single-walled carbon nanotubes delivery system .

机构信息

School of Pharmaceutical Sciences, Zhengzhou University , Zhengzhou , PR China.

出版信息

Drug Deliv. 2019 Dec;26(1):1017-1026. doi: 10.1080/10717544.2019.1672829.

DOI:10.1080/10717544.2019.1672829
PMID:31578087
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6781245/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39f2/6781245/68d950440f56/IDRD_A_1672829_F0007_C.jpg
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