Department of Obstetrics and Gynecology, Faculty of Medicine, Mu'tah University, Mu'tah, Jordan.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Pharm Dev Technol. 2020 Oct;25(8):930-935. doi: 10.1080/10837450.2020.1764032. Epub 2020 May 13.
Phloretin is a promising polyphenolic compound known for its anti-inflammatory properties, but its poor solubility and low bioavailability hinder its clinical applicability. Till current date, its potential in the treatment of vaginitis has not been explored, and only very few papers reported its formulation as nanoparticles to overcome its pharmaceutical challenges. Therefore, in the current study, phloretin was formulated in microemulsion of 11 nm size, and its anti-inflammatory properties were explored using histamine and IL-6 release inhibition assays, protease inhibition assay, and membrane stabilization potential. The anti-inflammatory properties of phloretin microemulsion were compared to the drug phloretin, and the reference standard non-steroidal anti-inflammatory drugs (NSAIDs). Results proved that both phloretin and phloretin microemulsion significantly inhibited the release of the inflammatory mediators histamine and IL-6, inhibited protease action, and exhibited membrane stabilization potential. Phloretin microemulsion exhibited comparable anti-inflammatory properties to the NSAIDs diclofenac and indomethacin, and, hence, it can be delineated as a promising therapeutic tool in topical treatment of vaginal inflammation.
根皮素是一种有前景的多酚化合物,以其抗炎特性而闻名,但其溶解度差和生物利用度低阻碍了其临床应用。迄今为止,其在阴道炎治疗中的潜力尚未得到探索,只有极少数论文报道了将其制成纳米粒来克服药物挑战。因此,在本研究中,根皮素被制成了 11nm 大小的微乳剂,并通过组胺和 IL-6 释放抑制试验、蛋白酶抑制试验和膜稳定潜力来探索其抗炎特性。将根皮素微乳剂的抗炎特性与药物根皮素和参考标准非甾体抗炎药(NSAIDs)进行了比较。结果表明,根皮素和根皮素微乳剂均能显著抑制炎症介质组胺和 IL-6 的释放,抑制蛋白酶的作用,并具有膜稳定潜力。根皮素微乳剂表现出与 NSAIDs 双氯芬酸和吲哚美辛相当的抗炎特性,因此可将其描绘为治疗阴道炎症的局部治疗有前途的治疗工具。