<br>5-氨基水杨酸-血红蛋白生物粘附纳米颗粒的口服制剂可提高溃疡性结肠炎小鼠的治疗效率：临床前评估,Journal of Pharmaceutical Sciences

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5-氨基水杨酸-血红蛋白生物粘附纳米颗粒的口服制剂可提高溃疡性结肠炎小鼠的治疗效率：临床前评估
Journal of Pharmaceutical Sciences ( IF 3.7 ) Pub Date : 2024-04-04 , DOI: 10.1016/j.xphs.2024.03.028
Zahra Vaezi ₁ , Shaghayegh Baradaran Ghavami ₂ , Maryam Farmani ₂ , Reza Mahdavian ₃ , Hamid Asadzadeh Aghdaei ₂ , Hossein Naderi-Manesh ₄

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结肠特异性给药的口服制剂设计在溃疡性结肠炎的治疗中带来了一些治疗益处。我们最近报道了将血红蛋白纳米颗粒结合 5-氨基水杨酸 (5-ASA-HbNP) 特异性递送至发炎部位。在当前的研究中，5-ASA-HbNPs制剂的治疗效果在体内得到了证实。与游离 5-ASA 相比，对 5-ASA-HbNP 的评估不仅显示出由于粘合特性而具有更长的结肠保留时间，而且还为其提供了充分的支持。它被认为是一种合适的生物粘附纳米颗粒，具有粘膜粘附特性，可以穿过粘液层并积聚到粘膜中。在 UC 模型小鼠中，5-ASA-HbNP 治疗组的疾病活动指数和结肠重量/长度比显着降低两倍。该组接受了标准剂量 1% 的 5-ASA (50 μg/kg)，同时，对于大量游离 5-ASA (5 mg/kg) 也观察到了类似的结果。此外，提取的结肠的组织学切片的显微图像表明，5-ASA-HbNP 和 5-ASA 组显示结肠内炎症损伤的情况。然而，与结肠炎组相比，这种损害的程度相对中等，表明 5-ASA-HbNPs 以较低的剂型提高了治疗效果。

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Oral Formulation of 5-Aminosalicylic Acid-Hemoglobin Bio-Adhesive Nanoparticles Enhance Therapeutic Efficiency in Ulcerative Colitis Mice: A Preclinical Evaluation

The oral formulation design for colon-specific drug delivery brings some therapeutic benefits in the ulcerative colitis treatment. We recently reported the specific delivery of hemoglobin nanoparticles-conjugating 5-aminosalicylic acid (5-ASA-HbNPs) to the inflamed site. In the current study, the therapeutic effect of the 5-ASA-HbNPs formulation was confirmed in vivo. This evaluation of 5-ASA-HbNPs not only shows longer colonic retention time due to adhesive properties, also provides full support for it as compared with free 5-ASA. It was considered as a suitable bio-adhesive nanoparticle with mucoadhesive property to pass through the mucus layer and accumulate into the mucosa. In UC model mice, a two-fold decrease in the disease activity indexes and colon weight/length ratios was significantly observed in the group treated with 5-ASA-HbNPs. This group received one percent of the standard dosage of 5-ASA (50 μg/kg), while, a similar result was observed for a significant amount of free 5-ASA (5 mg/kg). Furthermore, microscopic images of histological sections of the extracted colons demonstrated that the 5-ASA-HbNPs and 5-ASA groups displayed instances of inflammatory damage within the colon. However, in comparison to the colitis group, the extent of this damage was relatively moderate, suggesting 5-ASA-HbNPs improved therapeutic efficacy with the lower dosage form.

更新日期：2024-04-04

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