Elgewelly Mahmoud A, Elmasry Soha M, Sayed Nesrine S El, Abbas Haidy
Pharmaceutics Department, Faculty of Pharmacy, Damanhour University, Egypt.
Pharmacology and Toxicology Department, Faculty of Pharmacy, Cairo University, Egypt.
J Pharm Sci. 2022 Feb;111(2):417-431. doi: 10.1016/j.xphs.2021.08.023. Epub 2021 Aug 28.
This work aimed to develop a new efficient approach for safe treatment of psoriasis. To achieve that, resveratrol-loaded spanlastics(F1-F12) were prepared and evaluated by complete in vitro characterization. The two optimal formulations (F10 and F11) had their particle size in the nano range with high entrapment efficiency and sustainable drug release. These two formulae were incorporated in carbopol 934 gel formulations (G1-G8) with different concentrations of drug and carbopol 934 polymer. G1 and G5 (1% w/w Carbopol 934 gel and 0.1% resveratrol) showed 40.13% ± 2.017% and 73.76% ± 2.46%,8 hours drug release, respectively. Their pH was accepted and non-irritant. At a shear stress of 500 s, G1 and G5 showed a reasonable viscosity of 1048.5 ± 2.12 cps and 954 ± 2.15 cps, respectively. In the in vivo psoriasis study, mice treated by G5 gel showed significant improvement of erythema and scaling compared to positive control group and they maintained healthy skin as shown in histopathological observations. Moreover, this group showed the least changes in mRNA expression of inflammatory cytokines. Concisely, our results suggest that selected carbopol gel of resveratrol-loaded spanlastics could maximize resveratrol topical anti-psoriatic effect.
这项工作旨在开发一种安全治疗银屑病的新的有效方法。为此,制备了载有白藜芦醇的弹性脂质体(F1 - F12),并通过完整的体外表征进行评估。两种最佳制剂(F10和F11)的粒径在纳米范围内,具有高包封率和可持续的药物释放。将这两种配方掺入含有不同浓度药物和卡波姆934聚合物的卡波姆934凝胶制剂(G1 - G8)中。G1和G5(1% w/w卡波姆934凝胶和0.1%白藜芦醇)分别显示出40.13% ± 2.017%和73.76% ± 2.46%的8小时药物释放率。它们的pH值符合要求且无刺激性。在500 s的剪切应力下,G1和G5的粘度分别为1048.5 ± 2.12 cps和954 ± 2.15 cps,较为合理。在体内银屑病研究中,与阳性对照组相比,用G5凝胶治疗的小鼠的红斑和鳞屑有显著改善,并且如组织病理学观察所示,它们保持了健康的皮肤。此外,该组炎症细胞因子的mRNA表达变化最小。简而言之,我们的结果表明,所选的载有白藜芦醇的弹性脂质体卡波姆凝胶可使白藜芦醇的局部抗银屑病效果最大化。