Santos Valdeene Vieira, da Hora Borges Matheus Antônio, Jatobá da Silva Karoline Cristina, Dos Santos Costa Rafael, Santo Renan Fernandes do Espírito, Velozo Eudes da Silva, Villarreal Cristiane Flora, Azeredo Francine Johansson
Pharmacy Graduate Program, College of Pharmacy, Federal University of Bahia, Salvador 40170-115, Brazil.
College of Pharmacy, Federal University of Bahia, Salvador 40170-115, Brazil.
Pharmaceutics. 2024 May 26;16(6):714. doi: 10.3390/pharmaceutics16060714.
The compound 6-methoxyseselin, derived from , demonstrates various therapeutic properties, including vasorelaxation, antinociceptive, anti-inflammatory, and immunomodulatory effects, along with recently discovered antiasthmatic properties. This study aimed to evaluate its preclinical pharmacokinetics and pulmonary delivery in Balb/c mice. The method involved administering the compound via inhalation and intravenous routes, followed by blood sample collection for analysis using high-performance liquid chromatography with diode array detection (HPLC-DAD). The results indicated good linearity, precision, accuracy, and stability of the compound in the biological samples. Pharmacokinetic parameters such as the rate of elimination, half-life, clearance, volume of distribution, area under the curve, and mean residence time were determined for both administration routes, showing similar profiles. The lung concentrations were notably higher than the plasma concentrations, indicating significant lung penetration. These findings suggest 6-methoxyseselin as a promising candidate for new anti-asthmatic drugs, supported by its favorable pharmacokinetic profiles and high lung penetration factors. This study represents the first exploration of the pharmacokinetics and pulmonary delivery of 6-methoxyseselin in mice, highlighting its potential for further drug development.
从……中提取的化合物6-甲氧基邪蒿素具有多种治疗特性,包括血管舒张、抗伤害感受、抗炎和免疫调节作用,以及最近发现的抗哮喘特性。本研究旨在评估其在Balb/c小鼠中的临床前药代动力学和肺部给药情况。该方法包括通过吸入和静脉途径给药,随后采集血样,使用带二极管阵列检测的高效液相色谱法(HPLC-DAD)进行分析。结果表明该化合物在生物样品中具有良好的线性、精密度、准确度和稳定性。确定了两种给药途径的药代动力学参数,如消除速率、半衰期、清除率、分布容积、曲线下面积和平均驻留时间,显示出相似的特征。肺部浓度明显高于血浆浓度,表明有显著的肺部渗透。这些发现表明,6-甲氧基邪蒿素因其良好的药代动力学特征和高肺部渗透因子,有望成为新型抗哮喘药物的候选物。本研究首次探索了6-甲氧基邪蒿素在小鼠中的药代动力学和肺部给药情况,突出了其在进一步药物开发中的潜力。