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载盐酸吉西他滨 PLGA/大豆卵磷脂纳米粒的制备及其对非小细胞肺癌的治疗作用。

Development of Gemcitabine Loaded PLGA/Lecithin Nanoparticles for Non-Small Cell Lung Cancer Therapy.

机构信息

Department of Pharmaceutical Technology, Gulhane Faculty of Pharmacy, University of Health Sciences, Ankara, Turkey.

Stem Cell Research Center, Gulhane Institute of Health Sciences, University of Health Sciences, Ankara, Turkey.

出版信息

Curr Drug Deliv. 2020;17(7):622-628. doi: 10.2174/1567201817666200512094145.

Abstract

BACKGROUND

Compared to polymeric nanoparticles prepared using non-lipid surfactants, lecithin addition forms larger nanoparticles and exhibits higher drug loading and the stability of nanoparticles can be conferred by adding Vitamin E Polyethylene Glycol Succinate (TPGS) into the formulation.

AIM

The aim of this study is to prepare Gemcitabine (Gem) loaded lecithin/PLGA nanoparticles. Moreover, the effect of TPGS and sodium cholate (SK) on the preparation of lecithin/PLGA nanoparticles was compared.

METHODS

It was found that while PC addition into PLGATPGS nanoparticles formed larger particles (251.3± 6.0 nm for Gem-PLGATPGS NPs and 516,9 ± 3.9 nm for Gem-PLGA-PCTPGS NPs), the particle size of PLGASK nanoparticles was not affected by lecithin addition (p>0.05;).

RESULTS

In cytotoxicity studies, it was found that the SK-MES-1 cell inhibition rates of Gem-PLGATPGS NPs, Gem-PLGA-PCTPGS NPs, Gem-PLGASK NPs, Gem-PLGA-PCSK NPs were similar with free Gem (p>0.05;). In cytotoxicity studies, it was found that the encapsulation into nanoparticles did not change the cytotoxicity of the drug. However, higher cellular uptake has been observed when the lecithin was used in the preparation of PLGA nanoparticles.

CONCLUSION

Compared with free Gem, the Gem-loaded nanoparticles enhanced the uptake of the drug by SK-MES-1 cells which can increase the effect of gemcitabine for non-small cell lung cancer therapy.

摘要

背景

与使用非脂质表面活性剂制备的聚合物纳米颗粒相比,添加卵磷脂可形成更大的纳米颗粒,并具有更高的载药量,通过在配方中添加维生素 E 聚乙二醇琥珀酸酯(TPGS)可以赋予纳米颗粒的稳定性。

目的

本研究旨在制备吉西他滨(Gem)负载的卵磷脂/PLGA 纳米颗粒。此外,比较了 TPGS 和胆酸钠(SK)对卵磷脂/PLGA 纳米颗粒制备的影响。

方法

结果发现,PC 添加到 PLGATPGS 纳米颗粒中会形成较大的颗粒(Gem-PLGATPGS NPs 为 251.3±6.0nm,Gem-PLGA-PCTPGS NPs 为 516.9±3.9nm),而卵磷脂的添加不会影响 PLGASK 纳米颗粒的粒径(p>0.05)。

结果

在细胞毒性研究中,发现 Gem-PLGATPGS NPs、Gem-PLGA-PCTPGS NPs、Gem-PLGASK NPs 和 Gem-PLGA-PCSK NPs 的 SK-MES-1 细胞抑制率与游离 Gem 相似(p>0.05)。在细胞毒性研究中,发现药物包封成纳米颗粒不会改变药物的细胞毒性。然而,当卵磷脂用于 PLGA 纳米颗粒的制备时,观察到更高的细胞摄取。

结论

与游离 Gem 相比,载药纳米颗粒增强了 SK-MES-1 细胞对药物的摄取,从而可以提高吉西他滨治疗非小细胞肺癌的效果。

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