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负载吉非替尼的聚乳酸-羟基乙酸共聚物（PLGA）和壳聚糖包被的PLGA纳米颗粒对A549肺癌细胞系具有增强的细胞毒性。

Gefitinib loaded PLGA and chitosan coated PLGA nanoparticles with magnified cytotoxicity against A549 lung cancer cell lines.

作者信息

Alshetaili Abdullah S

机构信息

Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.

出版信息

Saudi J Biol Sci. 2021 Sep;28(9):5065-5073. doi: 10.1016/j.sjbs.2021.05.025. Epub 2021 May 20.

DOI:10.1016/j.sjbs.2021.05.025
PMID:34466084
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8381081/
Abstract

In the current study, gefitinib loaded PLGA nanoparticles (GFT-PLGA-NPs) and chitosan coated PLGA nanoparticles (GFT-CS-PLGA-NPs) were synthesized to investigate the role of surface charge of NPs for developing drug delivery system for non-small-cell lung cancer (NSCLC). The developed NPs were evaluated for their size, PDI, zeta potential (ZP), drug entrapment, drug loading, DSC, FTIR, XRD, release profile, and morphology. The anti-cancer activity of GFT loaded PLGA NPs and GFT loaded CS-PLGA-NPs were examined in human A549 lung cancer cell lines. In vitro release studies of GFT-CS-PLGA-NPs showed more sustained release in comparison to GFT-PLGA-NPs due surface charge attraction of chitosan. In addition, viability of A549 cells decreases significantly with the increasing concentration of GFT-PLGA NPs and GFT-CS-PLGA-NPs when compared to that of pure GFT and blank PLGA NPs. In addition, the microscopic analysis and counting of viable cells also validate the cytotoxicity of the developed NPs. This investigation proved that the developed NPs would be efficient carriers to deliver GFT with improved efficacy against NSCLC.

摘要

在当前研究中，合成了载有吉非替尼的聚乳酸-羟基乙酸共聚物纳米粒（GFT-PLGA-NPs）和壳聚糖包被的聚乳酸-羟基乙酸共聚物纳米粒（GFT-CS-PLGA-NPs），以研究纳米粒表面电荷在开发非小细胞肺癌（NSCLC）药物递送系统中的作用。对所制备的纳米粒进行了粒径、多分散指数（PDI）、zeta电位（ZP）、药物包封率、载药量、差示扫描量热法（DSC）、傅里叶变换红外光谱法（FTIR）、X射线衍射法（XRD）、释放曲线和形态学等方面的评估。在人A549肺癌细胞系中检测了载有GFT的PLGA纳米粒和载有GFT的CS-PLGA纳米粒的抗癌活性。GFT-CS-PLGA-NPs的体外释放研究表明，由于壳聚糖的表面电荷吸引作用，与GFT-PLGA-NPs相比，其释放更具持续性。此外，与纯GFT和空白PLGA纳米粒相比，随着GFT-PLGA纳米粒和GFT-CS-PLGA纳米粒浓度的增加，A549细胞的活力显著降低。此外，活细胞的显微镜分析和计数也证实了所制备纳米粒的细胞毒性。该研究证明所制备的纳米粒将是递送GFT的有效载体，对NSCLC具有更高的疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/d60612f1a9d2/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/3653c3afe971/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/0fea7242a368/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/240cf4bb274c/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/2072f2569966/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/d798c0f7fa43/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/c2f42105aa91/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/143e56cba7a3/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/d60612f1a9d2/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/3653c3afe971/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/0fea7242a368/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/240cf4bb274c/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/2072f2569966/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/d798c0f7fa43/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/c2f42105aa91/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/143e56cba7a3/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/995e/8381081/d60612f1a9d2/gr8.jpg

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