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载 6-姜酚的 PEG 化纳米囊泡的制备、表征、创伤愈合和细胞毒性测定。

Preparation, Characterization, Wound Healing, and Cytotoxicity Assay of PEGylated Nanophytosomes Loaded with 6-Gingerol.

机构信息

Pharmacological and Diagnostic Research Centre, Department Pharmacological, Faculty of Pharmacy, Al-Ahliyya Amman University, Amman 19328, Jordan.

Cell Therapy Center, The University of Jordan, Amman 11942, Jordan.

出版信息

Nutrients. 2022 Dec 5;14(23):5170. doi: 10.3390/nu14235170.

DOI:10.3390/nu14235170
PMID:36501201
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9741217/
Abstract

BACKGROUND

Nutrients are widely used for treating illnesses in traditional medicine. Ginger has long been used in folk medicine to treat motion sickness and other minor health disorders. Chronic non-healing wounds might elicit an inflammation response and cancerous mutation. Few clinical studies have investigated 6-gingerol's wound-healing activity due to its poor pharmacokinetic properties. However, nanotechnology can deliver 6-gingerol while possibly enhancing these properties. Our study aimed to develop a nanophytosome system loaded with 6-gingerol molecules to investigate the delivery system's influence on wound healing and anti-cancer activities.

METHODS

We adopted the thin-film hydration method to synthesize nanophytosomes. We used lipids in a ratio of 70:25:5 for DOPC(dioleoyl-sn-glycero-3-phosphocholine): cholesterol: DSPE/PEG2000, respectively. We loaded the 6-gingerol molecules in a concentration of 1.67 mg/mL and achieved size reduction via the extrusion technique. We determined cytotoxicity using lung, breast, and pancreatic cancer cell lines. We performed gene expression of inflammation markers and cytokines according to international protocols.

RESULTS

The synthesized nanophytosome particle sizes were 150.16 ± 1.65, the total charge was -13.36 ± 1.266, and the polydispersity index was 0.060 ± 0.050. Transmission electron microscopy determined the synthesized particles' spherical shape and uniform size. The encapsulation efficiency was 34.54% ± 0.035. Our biological tests showed that 6-gingerol nanophytosomes displayed selective antiproliferative activity, considerable downregulation of inflammatory markers and cytokines, and an enhanced wound-healing process.

CONCLUSIONS

Our results confirm the anti-cancer activity of PEGylated nanophytosome 6-gingerol, with superior activity exhibited in accelerating wound healing.

摘要

背景

营养素在传统医学中被广泛用于治疗疾病。生姜在民间医学中一直被用于治疗晕动病和其他轻微健康障碍。慢性不愈合的伤口可能会引发炎症反应和癌变突变。由于其较差的药代动力学特性,很少有临床研究调查 6-姜酚的伤口愈合活性。然而,纳米技术可以输送 6-姜酚,同时可能增强这些特性。我们的研究旨在开发一种负载 6-姜酚分子的纳米植物囊泡系统,以研究该递药系统对伤口愈合和抗癌活性的影响。

方法

我们采用薄膜水化法合成纳米植物囊泡。我们使用脂质的比例为 70:25:5,分别为 DOPC(二油酰基-sn-甘油-3-磷酸胆碱):胆固醇:DSPE/PEG2000。我们以 1.67mg/ml 的浓度加载 6-姜酚分子,并通过挤压技术实现了尺寸减小。我们使用肺癌、乳腺癌和胰腺癌细胞系来测定细胞毒性。我们根据国际协议进行了炎症标志物和细胞因子的基因表达。

结果

合成的纳米植物囊泡粒径为 150.16±1.65nm,总电荷量为-13.36±1.266mV,多分散指数为 0.060±0.050。透射电子显微镜确定了合成粒子的球形形状和均匀的尺寸。包封效率为 34.54%±0.035。我们的生物学测试表明,6-姜酚纳米植物囊泡显示出选择性的抗增殖活性,对炎症标志物和细胞因子的显著下调,以及增强的伤口愈合过程。

结论

我们的结果证实了 PEG 化纳米植物囊泡 6-姜酚的抗癌活性,其在加速伤口愈合方面表现出更好的活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/d8c52dbdd6e0/nutrients-14-05170-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/7b018b2ff114/nutrients-14-05170-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/685bfac2733c/nutrients-14-05170-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/03dc1850a563/nutrients-14-05170-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/1999c87bea0e/nutrients-14-05170-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/f86758e7f99d/nutrients-14-05170-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/d8c52dbdd6e0/nutrients-14-05170-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/7b018b2ff114/nutrients-14-05170-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/685bfac2733c/nutrients-14-05170-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/03dc1850a563/nutrients-14-05170-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/1999c87bea0e/nutrients-14-05170-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/f86758e7f99d/nutrients-14-05170-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fdcd/9741217/d8c52dbdd6e0/nutrients-14-05170-g006.jpg

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