Pharmaceutics Department, Faculty of Pharmacy, October 6 University, 6th of October City, Central Axis, Part 1/1, Behind Sixth October City Authority, Giza, 12585, Egypt.
Biochemistry Department, Faculty of Pharmacy, October 6 University, 6th of October City, Central Axis, Part 1/1, Behind Sixth October City Authority, Giza, 12585, Egypt.
AAPS PharmSciTech. 2021 Jun 15;22(5):180. doi: 10.1208/s12249-021-02042-6.
Oleogel consists of hydrophobic solvent and an oleogelator. In this study, attempts were made to study the influence of Celecoxib solubility, concentration and dispersability on its release, absorption, and biological performance. Oleogels were prepared to study the formulation variables on its stability and release. Castor oil was selected as the oil and the oleogelator concentration was 4.5% w/w. F3 revealed the highest release and stability compared to other formulae. The percent permeated across the rat intestine showed a 7.5-fold increase over free Celecoxib, and its lifetime was found to be greater than 18 months. The efficacy of free Celecoxib and oleogel formulae to treat rats with ulcerative colitis was done via the induction of ulcerative colitis (UC) through administration of 5% dextran sodium sulphate (DSS). Celecoxib besides its formulae significantly reduced the release of Leucine rich 2 glycoprotein (LRG), Myeloperoxidase (MPO), Tumor necrosis factor-α (TNF-α), proinflammatory cytokine expression, High mobility group box 1 (HMGB1), Nuclear factor kappa B (NF-ΚB), Trefoil Factor 3 (TFF3), Metalloproteinase-3 (MMP3), and miRNA31. Moreover, F3 significantly increased the colonic cAMP in DSS treated rats and reduced the intestinal inflammation beside healing of mucosa and restitution of the epithelium of the gastrointestinal tract.
油凝胶由疏水性溶剂和油凝胶剂组成。在这项研究中，尝试研究塞来昔布溶解度、浓度和分散性对其释放、吸收和生物学性能的影响。制备油凝胶以研究其稳定性和释放的配方变量。选择蓖麻油作为油，油凝胶剂浓度为 4.5%w/w。与其他配方相比，F3 显示出最高的释放和稳定性。与游离塞来昔布相比，大鼠肠内渗透的百分比增加了 7.5 倍，其半衰期大于 18 个月。通过给予 5%葡聚糖硫酸钠（DSS）诱导溃疡性结肠炎（UC），研究游离塞来昔布和油凝胶配方治疗溃疡性结肠炎大鼠的疗效。除了其配方外，塞来昔布还显著降低了富含亮氨酸 2 糖蛋白（LRG）、髓过氧化物酶（MPO）、肿瘤坏死因子-α（TNF-α）、促炎细胞因子表达、高迁移率族蛋白 B1（HMGB1）、核因子κB（NF-ΚB）、三叶因子 3（TFF3）、金属蛋白酶-3（MMP3）和 miRNA31 的释放。此外，F3 显著增加了 DSS 处理大鼠结肠中的 cAMP，并在修复粘膜和恢复胃肠道上皮的同时减轻了肠道炎症。
