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首页> 外文期刊>Drug Design, Development and Therapy >A Gastric Cancer Peptide GX1-Modified Nano-Lipid Carriers Encapsulating Paclitaxel: Design and Evaluation of Anti-Tumor Activity
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A Gastric Cancer Peptide GX1-Modified Nano-Lipid Carriers Encapsulating Paclitaxel: Design and Evaluation of Anti-Tumor Activity

机译：一种胃癌肽GX1-改性纳米脂质载体包封紫杉醇：抗肿瘤活性的设计和评估

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Aim: The aim of this study was to develop a GX1-modified nanostructured lipid carrier (NLCs) and to evaluate its ability to improve the anti-gastric cancer tumor effects of paclitaxel (PTX). Main Methods: The GX1-modified NLCs were synthesized and loaded with PTX (GX1-PTX-NLCs) by emulsion solvent evaporation technique. The anti-tumor activity and pharmacodynamics were then evaluated by in vitro cell studies and animal experiments. Key Findings: The GX1-modified NLCs were successfully synthesized and confirmed by sup1/supH NMR and MALDI-TOF-MS. PTX-loaded NLCs produced particles with average size distribution less than or equal to 222 nm and good drug loading and entrapment efficiency. In vitro studies demonstrated that GX1-PTX-NLCs had a more obvious inhibitory effect on Co-HUVEC cells than PTX and unmodified PTX-NLCs. The cellular uptake results also showed that GX1-PTX-NLCs were largely concentrated in Co-HUVEC cells, and the uptake rates of GX1-PTX-NLCs in Co-HUVEC were higher than those of the free drug and the PTX-NLC. In vivo studies demonstrated that GX1-PTX-NLCs possess strong anti-tumor effect and showed higher tumor growth inhibition and lower toxicity in nude mice. Significance: These results suggest that GX1-modified NLCs enhanced the anti-tumor activity of PTX and reduced its toxicity effectively. GX1-PTX-NLCs may be considered as a potent drug delivery system for therapy of gastric cancer.
机译：目的：本研究的目的是开发GX1改性的纳米结构脂质载体（NLC），并评估其改善紫杉醇（PTX）的抗胃癌肿瘤作用的能力。主要方法：通过乳液溶剂蒸发技术合成GX1改性的NLC并用PTX（GX1-PTX-NLCs）加载。然后通过体外细胞研究和动物实验评估抗肿瘤活性和药效学。主要发现：通过 1 H NMR和MALDI-TOF-MS来成功合成和证实GX1改性的NLC。 PTX加载的NLCS产生平均尺寸分​​布小于或等于222nm和良好药物负载和夹紧效率的颗粒。体外研究表明，GX1-PTX-NLCs对CO-HUVEC细胞具有比PTX和未修饰的PTX-NLC更明显的抑制作用。细胞摄取结果还表明，GX1-PTX-NLC在很大程度上浓缩在CO-HUVEC细胞中，并且CO-HUVEC中的GX1-PTX-NLC的摄取率高于游离药物和PTX-NLC。体内研究表明，GX1-PTX-NLCs具有强烈的抗肿瘤作用，并显示出裸鼠肿瘤的肿瘤生长抑制和较低的毒性。意义：这些结果表明，GX1改性的NLC增强了PTX的抗肿瘤活性，有效地降低了毒性。 GX1-PTX-NLC可以被认为是用于治疗胃癌的有效药物递送系统。

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