A Novel biodegradable system based on poly (lactic‐co‐glycolic acid) nanoparticles for delivery of a novel anticancer peptide delivery of a novel anticancer peptide

A. Faheem, A. Elkordy, Mohamed El-Tanani, Samuel Girgis
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Abstract

The main objective of this work was to formulate novel amphiphilic PLGA nanoparticles with improved physicochemical properties for the delivery of the novel peptide (CK-10) to be used for targeting of the cancerous/tumour tissue. This was achieved by blending of various amphiphilic polymers with PLGA, especially by using a novel microfluidic technique which can overcome several problems of the conventional techniques like the double emulsion technique e.g. low peptide loading efficiencies, large sizes, and high PDI. Loading efficiency was measured by modified Lowry assay; size and zeta potential were characterized by dynamic light scattering and tuneable pore resistive sensing techniques; images were scanned by scanning and transmission electron microscopes; stability and interaction were confirmed by HPLC-MS, FTIR, DSC and CZE. PLGA/Poloxamer nanoparticles exhibited higher peptide loading than the other types of PLGA nanoparticles [56.13 %m/m for the novel microfluidic technique]. PLGA/Poloxamer prepared by the microfluidics technique had the smallest size with the lowest PDI (208.90 nm, 0.11) which is a vital parameter for targeting. The successful development of better physicochemical properties for the CK-10 loaded PLGA nanoparticles can improve the RAN blocking by CK-10.
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一种新型的基于聚乳酸- co -乙醇酸纳米颗粒的可生物降解体系,用于递送一种新型抗癌肽
这项工作的主要目的是制备具有改进的物理化学性质的新型两亲性PLGA纳米颗粒,用于递送用于靶向癌/肿瘤组织的新型肽(CK-10)。这是通过将各种两亲性聚合物与PLGA共混而实现的,特别是通过使用一种新的微流控技术,该技术可以克服双乳液技术等传统技术的几个问题,例如肽装载效率低,尺寸大,PDI高。采用改良Lowry法测定负载效率;采用动态光散射和可调孔电阻传感技术表征了尺寸和zeta电位;用扫描电镜和透射电镜对图像进行扫描;通过HPLC-MS、FTIR、DSC和CZE等方法证实了其稳定性和相互作用。PLGA/Poloxamer纳米颗粒比其他类型的PLGA纳米颗粒具有更高的肽负载[56.13% m/m的新型微流控技术]。微流控技术制备的PLGA/Poloxamer具有最小的尺寸和最低的PDI (208.90 nm, 0.11),这是靶向的重要参数。成功开发出了具有较好理化性质的负载CK-10的PLGA纳米颗粒,可以改善CK-10对RAN的阻断作用。
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