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(+)-柠檬烯 1,2-环氧化物负载的 SLNs:在 HaCaT 细胞系中评估药物释放、抗氧化活性和细胞毒性。

(+)-Limonene 1,2-Epoxide-Loaded SLNs: Evaluation of Drug Release, Antioxidant Activity, and Cytotoxicity in an HaCaT Cell Line.

机构信息

Faculty of Pharmacy (FFUC), Department of Pharmaceutical Technology, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.

CEB-Centre of Biological Engineering, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal.

出版信息

Int J Mol Sci. 2020 Feb 20;21(4):1449. doi: 10.3390/ijms21041449.

Abstract

In this work, we developed a solid lipid nanoparticle (SLN) formulation with (+)-limonene 1,2-epoxide and glycerol monostearate (-SLNs), stabilized with Poloxamer 188 in aqueous dispersion to modify the release profile of the loaded monoterpene derivative. We also evaluated the role of SLNs in lipid peroxidation and cytotoxicity in a spontaneously transformed aneuploid immortal keratinocyte cell line from adult human skin (the HaCaT cell line). For the cell viability assay, the colorimetric 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used. -SLNs with a loading capacity and encapsulation efficiency of 0.39% and 63%, respectively, were produced by high pressure homogenization. A mean particle size of 194 ± 3.4 nm and polydispersity index of 0.244 were recorded for the loaded -SLNs, as compared to 203 ± 1.5 nm (PI 0.213) for the non-loaded (blank) SLNs. The loading of the monoterpene derivative into glycerol monostearate SLNs fitted into the zero-order kinetics, and ameliorated both lipid peroxidation and cytotoxicity in a keratinocyte cell line. A promising formulation for antioxidant and anti-tumoral activities is here proposed.

摘要

在这项工作中,我们开发了一种固体脂质纳米粒(SLN)制剂,其中含有(+)-柠檬烯 1,2-环氧化物和甘油单硬脂酸酯(-SLNs),并在水性分散体中用泊洛沙姆 188 稳定,以改变负载单萜衍生物的释放特性。我们还评估了 SLNs 在自发性转化的人成纤维细胞永生化细胞系(HaCaT 细胞系)中脂质过氧化和细胞毒性中的作用。对于细胞活力测定,使用比色法 3-(4,5-二甲基-2-噻唑基)-2,5-二苯基-2H-四唑溴盐(MTT)测定法。通过高压匀浆生产了载药量和包封效率分别为 0.39%和 63%的 -SLNs。负载 -SLNs 的平均粒径为 194 ± 3.4nm,多分散指数为 0.244,而非负载(空白)SLNs 的粒径为 203 ± 1.5nm(PI 0.213)。单萜衍生物在甘油单硬脂酸酯 SLNs 中的负载符合零级动力学,改善了角质形成细胞系中的脂质过氧化和细胞毒性。本文提出了一种具有抗氧化和抗肿瘤活性的有前途的制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6fec/7073088/7df752e6f4b8/ijms-21-01449-g001.jpg

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