Swami Pooja Ganpat, Singhavi Dilesh Jagdish, Ganjiwale Rajendra Onkarappa
Institute of Pharmaceutical Education and Research, Wardha, India.
Turk J Pharm Sci. 2025 May 14;22(2):119-130. doi: 10.4274/tjps.galenos.2025.02772.
Ayurvedic texts mention the use of fruit in colitis and other gastrointestinal ailments. The polyphenolic contents of the fruit, however, have poor bioavailability, limiting their therapeutic use. The study aimed to develop and optimise the fruit extract-phospholipid (AMEP) complex to improve the oral bioavailability of the extract (AME), and compare the effect of AME and AMEP in dextran sulfate sodium (DSS)-induced ulcerative colitis in rats.
The research work is the first of its kind to use a hydroalcoholic extract of fruit in the preparation of phospholipid complexes for ameliorating UC. The complexes were prepared using the solvent evaporation method and optimised by Box-Behnken design. The work compares the activity of plain AME, its phospholipid complexes, and the standard drug (mesalamine) in the alleviation of chemical-induced colitis in rats. AMEP was optimised using response surface methodology by Box-Behnken design. AMEP was characterised using scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, zeta analysis, and particle size analysis. A DSS-induced rat model was used studies to mimic ulcerative colitis. The pathogenesis of the disease was assessed by evaluating the levels of oxidative stress markers [nitric oxide (NO), malondialdehyde (MDA), and superoxide dismutase (SOD) activity], cytokines [tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6)], disease activity index, colon length, and histopathology.
The characterization confirmed the formation of AMEP, having a particle size of 673.6±4.30 nm, polydispersity index of 0.224±0.010, and zeta potential of -42.6 mV±0.51. The NO, MDA, TNF-α, and IL-6 levels were significantly reduced (<0.0001, <0.005, <0.0001, <0.01), and the SOD level was significantly increased (<0.05) in AMEP-treated groups compared to the AME-treated groups.
These findings suggessts that AMEP has a powerful potential to reduce the levels of oxidative markers and inflammatory cytokines, making it a promising treatment for ulcerative colitis.
阿育吠陀文献提及该果实可用于治疗结肠炎和其他胃肠道疾病。然而，该果实中的多酚类成分生物利用度较差，限制了其治疗用途。本研究旨在开发并优化该果实提取物-磷脂（AMEP）复合物，以提高提取物（AME）的口服生物利用度，并比较AME和AMEP对葡聚糖硫酸钠（DSS）诱导的大鼠溃疡性结肠炎的作用。
本研究首次使用该果实的水醇提取物制备用于改善溃疡性结肠炎的磷脂复合物。采用溶剂蒸发法制备复合物，并通过Box-Behnken设计进行优化。本研究比较了普通AME、其磷脂复合物和标准药物（美沙拉嗪）在减轻大鼠化学性结肠炎方面的活性。通过Box-Behnken设计采用响应面法对AMEP进行优化。使用扫描电子显微镜、傅里叶变换红外光谱、差示扫描量热法、zeta分析和粒度分析对AMEP进行表征。采用DSS诱导的大鼠模型模拟溃疡性结肠炎进行研究。通过评估氧化应激标志物[一氧化氮（NO）、丙二醛（MDA）和超氧化物歧化酶（SOD）活性]、细胞因子[肿瘤坏死因子-α（TNF-α）和白细胞介素-6（IL-6）]、疾病活动指数、结肠长度和组织病理学来评估疾病的发病机制。
表征证实形成了AMEP，其粒径为673.6±4.30 nm，多分散指数为0.224±0.010，zeta电位为-42.6 mV±0.51。与AME治疗组相比，AMEP治疗组的NO、MDA、TNF-α和IL-6水平显著降低（<0.0001、<0.005、<0.0001、<0.01），SOD水平显著升高（<0.05）。
这些发现表明AMEP具有强大的降低氧化标志物和炎性细胞因子水平的潜力，使其成为溃疡性结肠炎的一种有前景的治疗方法。
