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聚氧乙烯蓖麻油 188 通过物理吸附载大蒜素明胶纳米粒增强细胞毒性。

Augmented cytotoxicity using the physical adsorption of Poloxamer 188 on allicin-loaded gelatin nanoparticles.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, The British University in Egypt (BUE), Cairo, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

出版信息

J Pharm Pharmacol. 2021 Mar 27;73(5):664-672. doi: 10.1093/jpp/rgab006.

Abstract

OBJECTIVES

The aim of this work was to study the effect of the physically adsorbed Poloxamer 188 coating polymer on the cytotoxic activity of allicin-loaded gelatin nanoparticles.

METHODS

The double desolvation method was utilised to prepare the nanoparticles which were characterised for particle size (PS), polydispersity index (PDI) and zeta potential and visualised using transmission electron microscopy. The coating density of the used polymer was determined using 1H-nuclear magnetic resonance (1H-NMR); 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was used to evaluate the cytotoxicity on HepG-2 cell lines.

KEY FINDINGS

The particles were spherical possessing a PS of 714 ± 25.21 nm and a PDI of 0.663 ± 0.143. These results together with the 1H-NMR results analysis confirmed the efficient coating of Poloxamer 188. The coating of particles rendered them more cytotoxic, scoring an IC50 of 6.736 µm (2-folds lower than the uncoated counter parts and 4-folds lesser than the allicin solution), and apt for cancer-targeting. Moreover, the prepared nanoparticles were stable to gamma-sterilisation and to a storage of 12 months.

CONCLUSIONS

Augmented cytotoxicity on HepG-2 cell lines was obtained using the physical adsorption of an abundant and relatively cheap material, Poloxamer 188, on allicin-loaded gelatin nanoparticles.

摘要

目的

本研究旨在研究物理吸附的聚氧乙烯-聚氧丙烯嵌段共聚物(Poloxamer 188)对大蒜素载明胶纳米粒细胞毒性的影响。

方法

采用双重去溶剂化法制备纳米粒,通过透射电子显微镜对其粒径(PS)、多分散指数(PDI)和zeta 电位进行了表征。采用 1H 核磁共振(1H-NMR)测定所使用聚合物的包封密度;采用 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐(MTT)比色法评价其对 HepG-2 细胞系的细胞毒性。

关键发现

所制备的纳米粒呈球形,PS 为 714 ± 25.21nm,PDI 为 0.663 ± 0.143。这些结果结合 1H-NMR 结果分析证实了 Poloxamer 188 的有效包封。纳米粒的包封使其具有更高的细胞毒性,IC50 为 6.736µm(未包被的对照物的 2 倍,大蒜素溶液的 4 倍),适合用于癌症靶向治疗。此外,所制备的纳米粒经γ射线灭菌和 12 个月的储存后仍保持稳定。

结论

通过将丰富且相对廉价的材料——Poloxamer 188 物理吸附到大蒜素载明胶纳米粒上,获得了对 HepG-2 细胞系更高的细胞毒性。

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