塞来昔布局部平台抗菌活性和伤口愈合的体外、离体和体内研究:比较评估。

IF 2.4 4区 医学 Q3 CHEMISTRY, MEDICINAL
Priyanka Mundankar, Pankaj Neje, Shubhada Mangrulkar, Pranav Shah, Madhur Kulkarni
{"title":"塞来昔布局部平台抗菌活性和伤口愈合的体外、离体和体内研究:比较评估。","authors":"Priyanka Mundankar, Pankaj Neje, Shubhada Mangrulkar, Pranav Shah, Madhur Kulkarni","doi":"10.1080/03639045.2025.2469805","DOIUrl":null,"url":null,"abstract":"<p><strong>Background & rationale: </strong>Celecoxib (CXB), with its anti-inflammatory and recently discovered antibacterial activity, especially against sensitive and methicillin-resistant <i>Staphylococcus aureus (MRSA),</i> could be promising in treating local pain, superficial skin infections, wounds and infected wounds. The study aims to develop and compare commercially scalable topical formulations of CXB to explore their antimicrobial and wound-healing potential.</p><p><strong>Methods: </strong>Carbopol gel, o/w cream, polyethylene glycol (PEG) ointment, and paraffin ointment were selected as the vehicles for the preparation of 3% CXB topical formulations. Appearance, pH, viscosity, spreadability, drug content, stability, <i>in vitro</i> release and permeation, and skin retention studies were performed. Further, antimicrobial assay, <i>in vivo</i> wound-healing and histopathology studies were carried out for each formulation.</p><p><strong>Results: </strong>The formulations had an acceptable appearance, viscosity, spreadability, and drug content. The drug release at 6h was the highest from gel (2428.8ug/cm<sup>2</sup>), followed by PEG ointment (2230.1ug/cm<sup>2</sup>), cream (1897.8ug/cm<sup>2</sup>), and lastly, the paraffin ointment (1217.2ug/cm<sup>2</sup>). PEG ointment and gel showed the highest skin permeation, whereas cream and gel were better able to retain the drug in the skin. All the formulations exhibited appreciable zones of inhibition against sensitive and the resistant strains of <i>Staphylococcus aureus</i>. PEG ointment exerted a significantly greater (<i>p</i> < 0.001) wound-healing effect. Accelerated stability studies confirmed good physicochemical stability of the formulations.</p><p><strong>Conclusion: </strong>PEG ointment, with its optimal drug release profile, skin permeation ability, and greater wound-healing action, can be considered as a promising topical delivery vehicle for CXB. CXB's antimicrobial potential could further aid in the prevention as well as treatment of wound infection.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"319-331"},"PeriodicalIF":2.4000,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"<i>In vitro</i>, <i>ex vivo</i>, and <i>in vivo</i> studies of celecoxib topical platforms for antimicrobial activity and wound healing: a comparative assessment.\",\"authors\":\"Priyanka Mundankar, Pankaj Neje, Shubhada Mangrulkar, Pranav Shah, Madhur Kulkarni\",\"doi\":\"10.1080/03639045.2025.2469805\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background & rationale: </strong>Celecoxib (CXB), with its anti-inflammatory and recently discovered antibacterial activity, especially against sensitive and methicillin-resistant <i>Staphylococcus aureus (MRSA),</i> could be promising in treating local pain, superficial skin infections, wounds and infected wounds. The study aims to develop and compare commercially scalable topical formulations of CXB to explore their antimicrobial and wound-healing potential.</p><p><strong>Methods: </strong>Carbopol gel, o/w cream, polyethylene glycol (PEG) ointment, and paraffin ointment were selected as the vehicles for the preparation of 3% CXB topical formulations. Appearance, pH, viscosity, spreadability, drug content, stability, <i>in vitro</i> release and permeation, and skin retention studies were performed. Further, antimicrobial assay, <i>in vivo</i> wound-healing and histopathology studies were carried out for each formulation.</p><p><strong>Results: </strong>The formulations had an acceptable appearance, viscosity, spreadability, and drug content. The drug release at 6h was the highest from gel (2428.8ug/cm<sup>2</sup>), followed by PEG ointment (2230.1ug/cm<sup>2</sup>), cream (1897.8ug/cm<sup>2</sup>), and lastly, the paraffin ointment (1217.2ug/cm<sup>2</sup>). PEG ointment and gel showed the highest skin permeation, whereas cream and gel were better able to retain the drug in the skin. All the formulations exhibited appreciable zones of inhibition against sensitive and the resistant strains of <i>Staphylococcus aureus</i>. PEG ointment exerted a significantly greater (<i>p</i> < 0.001) wound-healing effect. Accelerated stability studies confirmed good physicochemical stability of the formulations.</p><p><strong>Conclusion: </strong>PEG ointment, with its optimal drug release profile, skin permeation ability, and greater wound-healing action, can be considered as a promising topical delivery vehicle for CXB. CXB's antimicrobial potential could further aid in the prevention as well as treatment of wound infection.</p>\",\"PeriodicalId\":11263,\"journal\":{\"name\":\"Drug Development and Industrial Pharmacy\",\"volume\":\" \",\"pages\":\"319-331\"},\"PeriodicalIF\":2.4000,\"publicationDate\":\"2025-04-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Development and Industrial Pharmacy\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/03639045.2025.2469805\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/2/25 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Development and Industrial Pharmacy","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/03639045.2025.2469805","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/2/25 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

摘要

背景与理由:塞来昔布(CXB)具有抗炎和最近发现的抗菌活性,特别是对敏感和耐甲氧西林的金黄色葡萄球菌(MRSA),可能在治疗局部疼痛、浅表皮肤感染、伤口和感染伤口方面有希望。该研究旨在开发和比较商业上可扩展的CXB局部配方,以探索其抗菌和伤口愈合潜力。方法:以卡波波凝胶、o/w乳膏、聚乙二醇软膏、石蜡软膏为载体,制备3% CXB外用制剂。进行了外观、pH、粘度、涂抹性、药物含量、稳定性、体外释放和渗透以及皮肤保留研究。此外,对每种制剂进行了抗菌试验、体内伤口愈合和组织病理学研究。结果:制剂的外观、粘度、涂抹性和药物含量均符合要求。凝胶释放量最高(2428.8ug/cm2),其次为PEG软膏(2230.1ug/cm2)、乳膏(1897.8ug/cm2),最后为石蜡软膏(1217.2ug/cm2)。PEG软膏和凝胶表现出最高的皮肤渗透性,而乳膏和凝胶能够更好地将药物保留在皮肤中。所有制剂对金黄色葡萄球菌敏感株和耐药株均有明显的抑制作用。结论:聚乙二醇软膏具有较好的释药特性、皮肤渗透能力和较强的创面愈合作用,可被认为是一种有前景的外用给药载体。CXB的抗菌潜力可以进一步帮助预防和治疗伤口感染。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vitro, ex vivo, and in vivo studies of celecoxib topical platforms for antimicrobial activity and wound healing: a comparative assessment.

Background & rationale: Celecoxib (CXB), with its anti-inflammatory and recently discovered antibacterial activity, especially against sensitive and methicillin-resistant Staphylococcus aureus (MRSA), could be promising in treating local pain, superficial skin infections, wounds and infected wounds. The study aims to develop and compare commercially scalable topical formulations of CXB to explore their antimicrobial and wound-healing potential.

Methods: Carbopol gel, o/w cream, polyethylene glycol (PEG) ointment, and paraffin ointment were selected as the vehicles for the preparation of 3% CXB topical formulations. Appearance, pH, viscosity, spreadability, drug content, stability, in vitro release and permeation, and skin retention studies were performed. Further, antimicrobial assay, in vivo wound-healing and histopathology studies were carried out for each formulation.

Results: The formulations had an acceptable appearance, viscosity, spreadability, and drug content. The drug release at 6h was the highest from gel (2428.8ug/cm2), followed by PEG ointment (2230.1ug/cm2), cream (1897.8ug/cm2), and lastly, the paraffin ointment (1217.2ug/cm2). PEG ointment and gel showed the highest skin permeation, whereas cream and gel were better able to retain the drug in the skin. All the formulations exhibited appreciable zones of inhibition against sensitive and the resistant strains of Staphylococcus aureus. PEG ointment exerted a significantly greater (p < 0.001) wound-healing effect. Accelerated stability studies confirmed good physicochemical stability of the formulations.

Conclusion: PEG ointment, with its optimal drug release profile, skin permeation ability, and greater wound-healing action, can be considered as a promising topical delivery vehicle for CXB. CXB's antimicrobial potential could further aid in the prevention as well as treatment of wound infection.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
CiteScore
6.80
自引率
0.00%
发文量
82
审稿时长
4.5 months
期刊介绍: The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信