中药促渗剂对甲氧胺酸皮肤透性的影响。

IF 1.8 Q3 PHARMACOLOGY & PHARMACY Turkish Journal of Pharmaceutical Sciences Pub Date : 2023-05-09 DOI:10.4274/tjps.galenos.2022.60669
Anayatollah Salimi, Sahba Sheykholeslami
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引用次数: 1

摘要

目的:甲氧胺酸(MA)是一种强效的非甾体抗炎药,但由于其有限的口服生物利用度和全身服用的副作用,最好是局部使用。本研究的主要目的是观察某些渗透增强剂如何影响MA的体外皮肤渗透性。在制造的Franz扩散池中,用玉米油、橄榄油、丁香油、桉树油和薄荷醇等几种渗透性增强剂预处理大鼠皮肤进行了MA渗透性测试,并与水合大鼠皮肤作为对照进行了比较。材料和方法:研究了稳态通量(Jss)、渗透系数(Kp)和扩散系数。采用傅里叶红外光谱(FTIR)比较了不对称和对称C- h拉伸、C=O拉伸、C=O拉伸(酰胺I)和C- n拉伸角蛋白(酰胺II)吸光度的峰位和强度变化,并采用差示扫描量热法(DSC)比较了平均转变温度和它们的焓。结果:丁香油、橄榄油和桉树油是最有效的增强剂,与湿润皮肤相比,其通量分别增加7.91倍、3.32倍和2.6倍,扩散系数分别增加3.25倍、1.34倍和1.25倍。FTIR和DSC数据显示,渗透增强剂导致皮肤SC层的脂质流化、提取、脂质结构破坏,以及皮肤该区域的蛋白质长期脱水。结论:药物渗透增强剂可提高药物在大鼠皮肤中的渗透性。更大的ERflux, ERD和ERP比率的最合理的机制是脂质流化,脂质结构的破坏,以及桉树油,薄荷醇,玉米油,橄榄油和丁香油在SC中的细胞内角蛋白不可逆变性。
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The Effect of Herbal Penetration Enhancers on the Skin Permeability of Mefenamic Acid Through Rat Skin.

Objectives: Mefenamic acid (MA) is a strong non-steroidal anti-inflammatory drug, but because of its limited oral bioavailability and the side effects that come with taking it systemically, it is better to apply it topically. The major goal of this study was to see how certain permeation enhancers affected MA is in vitro skin permeability. In manufactured Franz diffusion cells, MA permeability tests using rat skin pretreatment with several permeation enhancers such as corn oil, olive oil, clove oil, eucalyptus oil, and menthol were conducted and compared to hydrate rat skin as a control.

Materials and methods: The steady-state flux (Jss), permeability coefficient (Kp), and diffusion coefficient are among the permeability metrics studied. The permeability enhancement mechanisms of the penetration enhancer were investigated using fourier transform infrared spectroscopy (FTIR) to compare changes in peak position and intensities of asymmetric and symmetric C-H stretching, C=O stretching, C=O stretching (amide I), and C-N stretching of keratin (amide II) absorbance, as well as differential scanning calorimetry (DSC) to compare mean transition temperature and their enthalpies.

Results: Clove oil, olive oil, and eucalyptus oil were the most effective enhancers, increasing flux by 7.91, 3.32, and 2.6 times, as well as diffusion coefficient by 3.25, 1.34, and 1.25, respectively, when compared to moist skin. FTIR and DSC data show that permeation enhancers caused lipid fluidization, extraction, disruption of lipid structures in the SC layer of skin, and long-term dehydration of proteins in this area of the skin.

Conclusion: According to the findings, the permeation enhancers used improved drug permeability through excised rat skin. The most plausible mechanisms for greater ERflux, ERD, and ERP ratios were lipid fluidization, disruption of the lipid structure, and intracellular keratin irreversible denaturation in the SC by eucalyptus oil, menthol, corn oil, olive oil, and clove oil.

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CiteScore
3.60
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5.90%
发文量
79
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