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脂质体吡罗昔康制剂对脂多糖刺激的 RAW 264.7 巨噬细胞的细胞保护和增强抗炎活性。

Cytoprotective and enhanced anti-inflammatory activities of liposomal piroxicam formulation in lipopolysaccharide-stimulated RAW 264.7 macrophages.

机构信息

Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia.

出版信息

Int J Nanomedicine. 2013;8:1245-55. doi: 10.2147/IJN.S42801. Epub 2013 Mar 22.

DOI:10.2147/IJN.S42801
PMID:23569374
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3615925/
Abstract

BACKGROUND

Liposomal drug delivery systems, a promising lipid-based nanoparticle technology, have been known to play significant roles in improving the safety and efficacy of an encapsulated drug.

METHODS

Liposomes, prepared using an optimized proliposome method, were used in the present work to encapsulate piroxicam, a widely prescribed nonsteroidal anti-inflammatory drug. The cytotoxic effects as well as the in vitro efficacy in regulation of inflammatory responses by free-form piroxicam and liposome-encapsulated piroxicam were evaluated using a lipopolysaccharide-sensitive macrophage cell line, RAW 264.7.

RESULTS

Cells treated with liposome-encapsulated piroxicam demonstrated higher cell viabilities than those treated with free-form piroxicam. In addition, the liposomal piroxicam formulation resulted in statistically stronger inhibition of pro-inflammatory mediators (ie, nitric oxide, tumor necrosis factor-α, interleukin-1β, and prostaglandin E2) than piroxicam at an equivalent dose. The liposome-encapsulated piroxicam also caused statistically significant production of interleukin-10, an anti-inflammatory cytokine.

CONCLUSION

This study affirms the potential of a liposomal piroxicam formulation in reducing cytotoxicity and enhancing anti-inflammatory responses in vitro.

摘要

背景

脂质体药物递送系统是一种有前途的基于脂质的纳米颗粒技术,已被证明在提高包裹药物的安全性和疗效方面发挥着重要作用。

方法

本研究采用优化的前体脂质体方法制备脂质体,用于包裹吡罗昔康,这是一种广泛应用的非甾体抗炎药。使用脂多糖敏感的巨噬细胞系 RAW 264.7 评估游离吡罗昔康和脂质体包封的吡罗昔康的细胞毒性作用以及体外调节炎症反应的疗效。

结果

用脂质体包封的吡罗昔康处理的细胞比用游离吡罗昔康处理的细胞具有更高的细胞活力。此外,与等剂量的吡罗昔康相比,脂质体吡罗昔康制剂对促炎介质(即一氧化氮、肿瘤坏死因子-α、白细胞介素-1β和前列腺素 E2)的抑制作用更强。脂质体包封的吡罗昔康还可引起抗炎细胞因子白细胞介素-10 的显著产生。

结论

本研究证实了脂质体吡罗昔康制剂在减少细胞毒性和增强体外抗炎反应方面的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/b151189a517d/ijn-8-1245f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/1b1015ff2377/ijn-8-1245f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/3296f537fc12/ijn-8-1245f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/82bc90b6b1c6/ijn-8-1245f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/1061c0be0885/ijn-8-1245f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/8a9c1d423f9f/ijn-8-1245f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/b151189a517d/ijn-8-1245f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/1b1015ff2377/ijn-8-1245f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/3296f537fc12/ijn-8-1245f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/82bc90b6b1c6/ijn-8-1245f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/1061c0be0885/ijn-8-1245f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/8a9c1d423f9f/ijn-8-1245f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1527/3615925/b151189a517d/ijn-8-1245f6.jpg

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