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依托考昔和孟鲁司特铜氧化物纳米制剂的合成及其通过镇痛、抗炎、解热和急性毒性活性的评价。

Synthesis of Copper Oxide-Based Nanoformulations of Etoricoxib and Montelukast and Their Evaluation through Analgesic, Anti-Inflammatory, Anti-Pyretic, and Acute Toxicity Activities.

机构信息

Department of Chemistry, Islamia College University, Peshawar 25120, Khyber Pakhtunkhwa, Pakistan.

Nanosciences and Technology Department, National Centre for Physics, Quaid-i-Azam University Campus, Islamabad 44000, Punjab, Pakistan.

出版信息

Molecules. 2022 Feb 21;27(4):1433. doi: 10.3390/molecules27041433.

DOI:10.3390/molecules27041433
PMID:35209221
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8875186/
Abstract

Copper oxide nanoparticles (CuO NPs) were synthesized through the coprecipitation method and used as nanocarriers for etoricoxib (selective COX-2 inhibitor drug) and montelukast (leukotriene product inhibitor drug) in combination therapy. The CuO NPs, free drugs, and nanoformulations were investigated through UV/Vis spectroscopy, FTIR spectroscopy, XRD, SEM, and DLS. SEM imaging showed agglomerated nanorods of CuO NPs of about 87 nm size. The CE1, CE2, and CE6 nanoformulations were investigated through DLS, and their particle sizes were 271, 258, and 254 nm, respectively. The nanoformulations were evaluated through in vitro anti-inflammatory activity, in vivo anti-inflammatory activity, in vivo analgesic activity, in vivo anti-pyretic activity, and in vivo acute toxicity activity. In vivo activities were performed on albino mice. BSA denaturation was highly inhibited by CE1, CE2, and CE6 as compared to other nanoformulations in the in vitro anti-inflammatory activity. The in vivo bioactivities showed that low doses (5 mg/kg) of nanoformulations were more potent than high doses (10 and 20 mg/kg) of free drugs in the inhibition of pain, fever, and inflammation. Lastly, CE2 was more potent than that of other nanoformulations.

摘要

氧化铜纳米粒子(CuO NPs)通过共沉淀法合成,并用作依托考昔(选择性 COX-2 抑制剂药物)和孟鲁司特(白三烯产物抑制剂药物)联合治疗的纳米载体。通过紫外/可见分光光度法、傅里叶变换红外光谱法、XRD、SEM 和 DLS 研究了 CuO NPs、游离药物和纳米制剂。SEM 成像显示 CuO NPs 的纳米棒约为 87nm 大小。通过 DLS 研究了 CE1、CE2 和 CE6 纳米制剂,其粒径分别为 271nm、258nm 和 254nm。通过体外抗炎活性、体内抗炎活性、体内镇痛活性、体内解热活性和体内急性毒性活性评价了纳米制剂。体内活性在白化小鼠上进行。与其他纳米制剂相比,BSA 变性在体外抗炎活性中被 CE1、CE2 和 CE6 高度抑制。体内生物活性表明,纳米制剂的低剂量(5mg/kg)比游离药物的高剂量(10 和 20mg/kg)更能有效地抑制疼痛、发热和炎症。最后,CE2 比其他纳米制剂更有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/f9a39e6ed0ba/molecules-27-01433-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/bfb134eb3f26/molecules-27-01433-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/12c4d8384dde/molecules-27-01433-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/a12d060af1f1/molecules-27-01433-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/a74a7fc2ff5f/molecules-27-01433-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/45da47b0eb48/molecules-27-01433-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/60e20e9fdead/molecules-27-01433-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/27ca262af6d4/molecules-27-01433-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/f9a39e6ed0ba/molecules-27-01433-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/bfb134eb3f26/molecules-27-01433-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/12c4d8384dde/molecules-27-01433-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/a12d060af1f1/molecules-27-01433-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/a74a7fc2ff5f/molecules-27-01433-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/45da47b0eb48/molecules-27-01433-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/60e20e9fdead/molecules-27-01433-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/27ca262af6d4/molecules-27-01433-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/063e/8875186/f9a39e6ed0ba/molecules-27-01433-g008.jpg

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