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A Gastric Cancer Peptide GX1-Modified Nano-Lipid Carriers Encapsulating Paclitaxel: Design and Evaluation of Anti-Tumor Activity.
Drug Design, Development and Therapy ( IF 4.7 ) Pub Date : 2020-06-12 , DOI: 10.2147/dddt.s233023 Yufan Jian 1, 2 , Meina Zhao 1, 2 , Jinyi Cao 1 , Tingting Fan 1 , Wei Bu 1 , Yang Yang 3 , Weiwei Li 1 , Wei Zhang 1 , Yi Qiao 1 , Jingwen Wang 1 , Aidong Wen 1, 2
Drug Design, Development and Therapy ( IF 4.7 ) Pub Date : 2020-06-12 , DOI: 10.2147/dddt.s233023 Yufan Jian 1, 2 , Meina Zhao 1, 2 , Jinyi Cao 1 , Tingting Fan 1 , Wei Bu 1 , Yang Yang 3 , Weiwei Li 1 , Wei Zhang 1 , Yi Qiao 1 , Jingwen Wang 1 , Aidong Wen 1, 2
Affiliation
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 1H 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.
Keywords: gastric cancer, paclitaxel, nano-lipid carriers, gastric cancer peptide, anti-tumor activity
中文翻译：
封装紫杉醇的胃癌肽 GX1 修饰的纳米脂质载体：抗肿瘤活性的设计和评估。
目的：本研究的目的是开发一种 GX1 修饰的纳米结构脂质载体 (NLC)，并评估其改善紫杉醇 (PTX) 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修饰的NLCs并负载PTX（GX1-PTX-NLCs）。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： GX1 修饰的 NLC 成功合成并由1H NMR和MALDI-TOF-MS。负载 PTX 的 NLC 产生的颗粒平均粒径分布小于或等于 222 nm，具有良好的载药和包埋效率。体外研究表明，GX1-PTX-NLCs对Co-HUVEC细胞的抑制作用比PTX和未修饰的PTX-NLCs更明显。细胞摄取结果还显示GX1-PTX-NLCs主要集中在Co-HUVEC细胞中，GX1-PTX-NLCs在Co-HUVEC中的摄取率高于游离药物和PTX-NLC。体内研究表明，GX1-PTX-NLCs 具有很强的抗肿瘤作用，在裸鼠中表现出更高的肿瘤生长抑制和更低的毒性。
意义：这些结果表明GX1修饰的NLCs增强了PTX的抗肿瘤活性并有效降低了其毒性。GX1-PTX-NLCs 可被认为是治疗胃癌的有效药物递送系统。
关键词：胃癌 紫杉醇 纳米脂质载体 胃癌肽 抗肿瘤活性
更新日期：2020-06-12
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 1H 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.
Keywords: gastric cancer, paclitaxel, nano-lipid carriers, gastric cancer peptide, anti-tumor activity
中文翻译：
封装紫杉醇的胃癌肽 GX1 修饰的纳米脂质载体：抗肿瘤活性的设计和评估。
目的：本研究的目的是开发一种 GX1 修饰的纳米结构脂质载体 (NLC)，并评估其改善紫杉醇 (PTX) 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修饰的NLCs并负载PTX（GX1-PTX-NLCs）。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： GX1 修饰的 NLC 成功合成并由1H NMR和MALDI-TOF-MS。负载 PTX 的 NLC 产生的颗粒平均粒径分布小于或等于 222 nm，具有良好的载药和包埋效率。体外研究表明，GX1-PTX-NLCs对Co-HUVEC细胞的抑制作用比PTX和未修饰的PTX-NLCs更明显。细胞摄取结果还显示GX1-PTX-NLCs主要集中在Co-HUVEC细胞中，GX1-PTX-NLCs在Co-HUVEC中的摄取率高于游离药物和PTX-NLC。体内研究表明，GX1-PTX-NLCs 具有很强的抗肿瘤作用，在裸鼠中表现出更高的肿瘤生长抑制和更低的毒性。
意义：这些结果表明GX1修饰的NLCs增强了PTX的抗肿瘤活性并有效降低了其毒性。GX1-PTX-NLCs 可被认为是治疗胃癌的有效药物递送系统。
关键词：胃癌 紫杉醇 纳米脂质载体 胃癌肽 抗肿瘤活性
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