具有增强抗真菌活性的伊特拉科纳荷载生物修复菌:制造,评估和分子模拟
Faisal Usman1, Mudassir Farooq2, Tanveer A Wani3
1Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan 66000, Pakistan.
Antibiotics (Basel, Switzerland)
|October 27, 2023
概括
这项研究开发了新型的伊特罗康纳 (ITZ) 载的表面素A (SA) 菌粒,增强了抗真菌活性6倍. 这些稳定的小胞提供了一个有前途的药物输送平台,用于溶性较差的伊特拉科纳.
科学领域:
- 制药科学 制药科学
- 生物技术是生物技术.
- 菌类学 菌类学是指菌类学.
背景情况:
- 伊特拉科纳 (ITZ) 是一种广泛的抗真菌剂,用于各种真菌感染.
- 由于ITZ的溶解性较差,其治疗效果受到限制.
- 表面素A (SA) 是一种脂,表现出强大的抗真菌特性.
研究的目的:
- 通过与表面素A (SA) 配制来增强伊特拉科纳 (ITZ) 的抗真菌活性.
- 开发和表征伊特拉可纳装载的表面蛋白A微粒作为药物输送系统.
- 评估开发的配方的体外释放,稳定性和抗真菌协同作用.
主要方法:
- 表面素A (SA) 的提取和净化.
- 使用单冲洗方法制备充满伊特拉科纳 (ITZ) 的SA.
- 微粒的特征 (粒子大小,泽塔电位,FTIR光谱).
- 在pH 1.2的体外溶解研究和血液溶解试验.
- ITZ-SA复杂相互作用的分子模拟.
主要成果:
- 稳定,非球形的伊特拉可纳装载表面活性蛋白A小粒 (平均大小~179 nm) 已成功制备.
- FTIR分析证实ITZ和SA之间没有化学相互作用.
- 与纯ITZ相比,配方表现出减少的血液溶解.
- 药物释放遵循Korsmeyer-Peppas模型,表明扩散控制的释放.
- 在酸性缓冲中,药物释放率在2小时内从73-89%不等.
- 分子模拟显示了ITZ-SA复合体的有利结合和稳定性.
结论:
- 含有伊特拉科纳的表面蛋白A小粒因协同作用而表现出高达6倍的抗真菌活性.
- 开发的状配方是一种稳定且有前途的药物输送平台,用于稀释性较差的伊特拉科纳.
- ITZ和SA之间的π-基接触有助于复合物的稳定性和有效性.
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