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首页> 外文期刊>Molecular and Cellular Pharmacology >Curcumin-encapsulating Nanogels as an Effective Anticancer Formulation for Intracellular Uptake
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Curcumin-encapsulating Nanogels as an Effective Anticancer Formulation for Intracellular Uptake

机译:姜黄素包裹纳米凝胶作为细胞内摄取的有效抗癌制剂。

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Nanoscale drug delivery systems represent an attractive strategy to improve both the efficacy and safety of anticancer drugs. In this work, we describe nanoformulation of curcumin, a most potent natural anticancer compound capable of killing cancer cells while sparing the normal tissues. Since curcumin is a natural hydrophobic polyphenol, it has a low aqueous solubility and bioavailability, which are challenging to its therapeutic efficacy. We developed and evaluated a novel colloidal nanogel carrier for encapsulation of curcumin to increase its solubility and cytotoxicity. Amphiphilic Poloxamer-cationic network in the nanogel NG127 was designed to efficiently encapsulate curcumin. Homogenous drug complexes were obtained with 20-25% content of curcumin and the particle size of ca. 150 nm. Using ImageStream multispectral imaging flow cytometry, we demonstrated that the curcumin-nanogel formulation (C-NG) was readily internalized into MDA-231 breast cancer cells. A real-time cell growth electronic sensing assay was used to measure proliferation responses of various breast cancer cells to C-NG treatments. Our results indicated that the C-NG formulation was 70-85% more effective in inhibiting growth, at concentrations lower than IC 50 of free curcumin. This was also confirmed morphologically by modified acridine orange/ethidium bromide staining and fluorescent microscopy. Importantly, nanocarrier NG127 alone displayed practically no cytotoxicity. We conclude that nanogel carriers offer an innovative way to encapsulate curcumin and to obtain more effective anticancer therapeutics than curcumin alone with a potential to specific tumor targeting, such as using antibodies against surface receptors specific to breast cancer cells. Normal 0 false false false EN-US X-NONE X-NONE /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin-top:0in; mso-para-margin-right:0in; mso-para-margin-bottom:10.0pt; mso-para-margin-left:0in; line-height:150%; mso-pagination:widow-orphan; font-size:12.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin;}
机译:纳米级药物递送系统代表了一种有吸引力的策略,可以同时提高抗癌药物的功效和安全性。在这项工作中,我们描述了姜黄素的纳米配方,姜黄素是一种最有效的天然抗癌化合物,能够杀死癌细胞,同时保留正常组织。由于姜黄素是天然的疏水性多酚,因此其水溶性和生物利用度低,这对其治疗功效提出了挑战。我们开发和评估了一种新型的胶体纳米凝胶载体,用于包裹姜黄素以增加其溶解度和细胞毒性。纳米凝胶NG127中的两亲泊洛沙姆阳离子网络旨在有效地封装姜黄素。得到的均质药物复合物的姜黄素含量为20%至25%,粒径约为。 150纳米使用ImageStream多光谱成像流式细胞仪,我们证明了姜黄素-纳米凝胶制剂(C-NG)易于内化到MDA-231乳腺癌细胞中。实时细胞生长电子传感测定法用于测量各种乳腺癌细胞对C-NG治疗的增殖反应。我们的结果表明,C-NG制剂在抑制生长方面的功效提高了70-85%,其浓度低于游离姜黄素的IC 50浓度。修饰的a啶橙/溴化乙锭染色和荧光显微镜在形态上也证实了这一点。重要的是,仅纳米载体NG127几乎没有表现出细胞毒性。我们得出的结论是,与单独的姜黄素相比,纳米凝胶载体提供了一种封装姜黄素并获得更有效的抗癌治疗药物的创新方法,具有针对特定肿瘤靶向的潜力,例如使用针对乳腺癌细胞特异性表面受体的抗体。正常0否否否EN-US X-NONE X-NONE / *样式定义* / table.MsoNormalTable {mso-style-name:“ Table Normal”; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:是; mso-style-priority:99; mso-style-parent:“”; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin-top:0in; mso-para-margin-right:0in; mso-para-margin-bottom:10.0pt; mso-para-margin-left:0in;行高:150%; mso分页:寡妇孤儿;字体大小:12.0pt;字体家族:“ Calibri”,“ sans-serif”; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin;}

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