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含松节油精、樟脑和薄荷醇的水杨酸甲酯凝胶对肌肉和关节疼痛进行症状性局部治疗的渗透能力及局部抗炎作用

[Penetration capacity and local anti-inflammatory effect of a methyl salicylate gel with turpentine essence, camphor, and menthol for the symptomatic local treatment of muscular and joint pains].

作者信息

Vidal Montserrat, Roldán Taïs

机构信息

Directora del área científica de Crossdata España.

Responsable técnico y directora de asuntos regulatorios, médicos y de seguridad de Reckitt Benckiser Healthcare, España España.

出版信息

Farm Comunitarios. 2024 Apr 17;16(3):5-11. doi: 10.33620/FC.2173-9218.(2024).15. eCollection 2024 Jul 15.

Abstract

INTRODUCTION

Oral non-steroidal anti-inflammatory drugs (NSAIDs) are effective in managing musculoskeletal pain, but often are associated with side effects. Therefore, topical anti-inflammatory drugs are considered a suitable alternative for certain patients.

OBJECTIVE

To determine the skin penetration capacity and anti-inflammatory efficacy of a methyl salicylate gel (MS) with turpentine essence, camphor and menthol (GelSMETAM).

METHODS

Human skin explants were used (three biological replicates with 3 technical replicates each were performed). To assess penetration capacity, methyl salicylate (MS) levels were quantified at different intervals using liquid chromatography with tandem mass spectrometry (LC-MS/MS). For the anti-inflammatory effect, the gene expression of major pro-inflammatory factors was quantified 30 minutes, 8 hours, and 12 hours after an impact; comparing GelSMETAM application with untreated controls.

RESULTS

The results showed that approximately 0.8% of the total applied methyl salicylate penetrated the skin with a time-dependent concentration increase. The anti-inflammatory effect demonstrated a significant reduction in the gene expression of TNFα, IL1α, IL6, IL8, and NFKβ at 30 minutes (between -39% and -53.6% compared to control), which was maintained at 8 hours except for TNFα (between -59% and -92.6%) and persisted even at 12 hours (-69.4%) for IL1α.

CONCLUSION

The results support the hypothesis that GelSMETAM provides an effective and prolonged anti-inflammatory response, positioning it as a suitable option for the management of musculoskeletal pain.

摘要

引言

口服非甾体抗炎药(NSAIDs)在管理肌肉骨骼疼痛方面有效,但常伴有副作用。因此,局部抗炎药被认为是某些患者的合适替代药物。

目的

确定含有松节油精、樟脑和薄荷醇的水杨酸甲酯凝胶(GelSMETAM)的皮肤渗透能力和抗炎功效。

方法

使用人体皮肤外植体(进行了三次生物学重复,每次重复有3次技术重复)。为评估渗透能力,使用液相色谱-串联质谱法(LC-MS/MS)在不同时间间隔对水杨酸甲酯(MS)水平进行定量。对于抗炎作用,在冲击后30分钟、8小时和12小时对主要促炎因子的基因表达进行定量;将GelSMETAM的应用与未处理的对照进行比较。

结果

结果表明,所应用的水杨酸甲酯总量中约0.8%穿透皮肤,且浓度随时间增加。抗炎作用显示,在30分钟时TNFα、IL1α、IL6、IL8和NFKβ的基因表达显著降低(与对照相比,降低幅度在-39%至-53.6%之间),除TNFα外,在8小时时仍保持降低(降低幅度在-59%至-92.6%之间),IL1α在12小时时甚至仍保持降低(-69.4%)。

结论

结果支持以下假设,即GelSMETAM能提供有效且持久的抗炎反应,使其成为管理肌肉骨骼疼痛的合适选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49b7/11346264/b148826a24d4/FC16-03-02_gf01.jpg

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