Veterinary Hygiene and Management Department, Faculty of Vet. Medicine, Cairo University, Giza, 12211, Egypt.
Department of Pharmaceutics, Egyptian Drug Authority Formerly Known As National Organization for Drug Control and Research (NODCAR), Giza, Egypt.
AAPS PharmSciTech. 2022 Aug 26;23(7):243. doi: 10.1208/s12249-022-02387-6.
Hypericum perforatum (HP) is characterized by potent medicinal activity. However, the poor water solubility of many HP constituents limits their therapeutic effectiveness. Self-nanoemulsifying self-nanosuspension loaded with HP (HP.SNESNS) was formulated to improve the bioefficacy of HP. It was prepared using 10% triacetin, 57% Tween 20, and 33% PEG 400 and then incorporated with HP extract (100 mg/mL). HP.SNESNS demonstrated a bimodal size distribution (258.65 ± 29.35 and 9.08 ± 0.01 nm) corresponding to nanosuspension and nanoemulsion, respectively, a zeta potential of -8.03 mV, and an enhanced dissolution profile. Compared to the unformulated HP (100 mg/kg), HP.SNESNS significantly improved cardiac functions by decreasing the serum myocardial enzymes, nitric oxide (NO), and tumor necrosis factor- α (TNF-α) as well as restoring the heart tissue's normal architecture. Furthermore, it ameliorates anxiety, depressive-like behavior, and cognitive dysfunction by decreasing brain TNF-α, elevating neurotransmitters (norepinephrine and serotonin), and brain-derived neurotrophic factor (BDNF). In addition, HP.SNESNS augmented the immunohistochemical expression of cortical and hippocampal glial fibrillary acidic protein (GFAP) levels while downregulating the cortical Bcl-2-associated X protein (Bax) expression levels. Surprisingly, these protective activities were comparable to the HP (300 mg/kg). In conclusion, HP.SNESNS (100 mg/kg) exerted antidepressant and cardioprotective activities in the post-MI depression rat model.
贯叶金丝桃（HP）具有很强的药用活性。然而，许多 HP 成分的水溶性差限制了其治疗效果。载有 HP 的自微乳自纳米混悬剂（HP.SNESNS）的配方旨在提高 HP 的生物功效。它是使用 10%三醋酸甘油酯、57%吐温 20 和 33%PEG400 制备的，然后与 HP 提取物（100mg/mL）混合。HP.SNESNS 表现出双峰粒径分布（分别为 258.65±29.35nm 和 9.08±0.01nm），对应于纳米混悬液和纳米乳液，zeta 电位为-8.03mV，溶解特性得到增强。与未成型的 HP（100mg/kg）相比，HP.SNESNS 通过降低血清心肌酶、一氧化氮（NO）和肿瘤坏死因子-α（TNF-α）以及恢复心脏组织的正常结构，显著改善了心脏功能。此外，它通过降低大脑 TNF-α、提高神经递质（去甲肾上腺素和血清素）和脑源性神经营养因子（BDNF）来改善焦虑、抑郁样行为和认知功能障碍。此外，HP.SNESNS 增加了皮质和海马神经胶质纤维酸性蛋白（GFAP）水平的免疫组织化学表达，同时下调了皮质 Bcl-2 相关 X 蛋白（Bax）的表达水平。令人惊讶的是，这些保护作用与 HP（300mg/kg）相当。总之，HP.SNESNS（100mg/kg）在 MI 后抑郁大鼠模型中发挥了抗抑郁和心脏保护作用。
