a Department of Research and Development , Atos Pharma , Cairo , Egypt.
b Department of Pharmacognosy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
Drug Deliv. 2018 Nov;25(1):417-425. doi: 10.1080/10717544.2018.1431977.
The active compounds present in Hypericum perforatum L. (Hypericaceae) include hyperforin, hypericins and flavonoids, which are assumed to be responsible for the activity of the extract in the treatment of wounds and scars. The present study aimed to incorporate H. perforatum extract standardized to a known content of phloroglucinols, naphthodianthrones and polyphenolic compounds into an effective transdermal drug delivery system capable of entrapping both lipophilic and hydrophilic constituents in the form of niosomal gels for wound treatment. An 80% ethanol extract (HE) was prepared on a pilot scale using DIG-MAZ. An HPLC-DAD holistic profile was established for HE and was standardized to contain 3.4 ± 4 rutin, 1.1 ± 3 chlorogenic acid, 0.5 ± 2 quercitrin, 2.8 ± 2 hyperforin, and 0.51 ± 3% w/w total hypericins. Niosomes were prepared using the modified reverse phase evaporation technique (REV). The wound healing effect of the gel was tested on 16 adult mongrel dogs. A significant decrease in the inflammatory cell count (18.4 ± 5.3) was recorded in the niosomal gel 1.5% NaCMC-treated group at the 7th day post wounding. It induced a marked regression in the inflammatory phase and enhanced the early beginning of the proliferative phase of wound healing. After 21 days, it showed complete re-epithelization, formation of new matrix fibers and significant reduction in the wound size, compared to the control and the Panthenol® 2% cream treated groups. This is the first study of H. perforatum in a niosomal topical drug delivery system.
贯叶金丝桃（藤黄科）中的活性化合物包括贯叶金丝桃素、金丝桃素和类黄酮，这些化合物被认为是提取物在治疗伤口和疤痕中具有活性的原因。本研究旨在将贯叶金丝桃提取物标准化为已知的苯丙素醇、萘二蒽酮和多酚化合物含量，并将其纳入一种有效的经皮药物传递系统，该系统能够以类脂囊泡凝胶的形式捕获亲脂性和亲水性成分，用于伤口治疗。使用 DIG-MAZ 在中试规模上制备 80%乙醇提取物（HE）。建立了 HE 的 HPLC-DAD 整体图谱，并将其标准化为含有 3.4±4 芦丁、1.1±3 绿原酸、0.5±2 槲皮苷、2.8±2 贯叶金丝桃素和 0.51±3%w/w 总金丝桃素。使用改良的反向相蒸发技术（REV）制备类脂囊泡。在 16 只成年杂种犬上测试了凝胶的伤口愈合效果。在第 7 天，在 1.5%NaCMC 处理的类脂囊泡凝胶组中，炎症细胞计数显著减少（18.4±5.3）。它在炎症期明显消退，并促进了伤口愈合的早期增生期开始。21 天后，与对照组和泛醇®2%乳膏治疗组相比，它显示出完全的再上皮化、新基质纤维的形成和伤口大小的显著减少。这是贯叶金丝桃在类脂囊泡局部药物传递系统中的首次研究。
