用于改善阿西克洛维尔口服通透性的基于聚莉素乳的菌丝的配方和评估
Jyoti Verma1, Fanny Frejborg2, Marta Mantegna3
1Pharmaceutical Sciences Laboratory, Department of Natural and Health Sciences, Faculty of Science and Engineering, Åbo Akademi University, 20520 Turku, Finland.
概括
这项研究开发了新的阳离子聚合物微粒来增强阿西克洛维尔 (ACV) 的生物可用性. 这些微粒改善了ACV的溶解性和透性,为更好的抗病毒疗法提供了有前途的方法.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 抗病毒研究 抗病毒研究
背景情况:
- 乙克洛维尔 (ACV) 是一种BCSIII类抗病毒药物,由于透性差,其口服生物可用性较低.
- 为了保持治疗水平,需要经常剂量ACV,这会导致潜在的副作用和患者不良服药.
- 提高ACV的透性对于改善其治疗疗效和患者的治疗结果至关重要.
研究的目的:
- 开发和评估基于酸功能化聚酸 (莉花乳) 的阳离子聚合物微粒,以提高阿西克洛维尔 (ACV) 的溶解性和透性.
- 评估充满ACV的小胞体对简单疹病毒1型病毒的抗病毒功效.
- 在模拟的生理条件下,研究这些细胞对ACV透性的影响.
主要方法:
- 使用酸功能化聚 ((莉花乳)) 合成了阳离子聚合物微粒 (~100 nm).
- 确定了阿西克洛维尔 (ACV) 的负载能力和水溶性.
- 使用简单疹病毒1型抑制试验评估了抗病毒活性.
- 透性研究使用基于脂囊泡的透性试验 (PVPA),有或没有粘液层进行.
- 使用GastroPlus® (GPX) 软件进行了in silico模拟,以模拟ACV行为.
主要成果:
- 聚合物微粒显著增加了ACV的水溶性,从1.81 mg/mL增加到4.32 mg/mL.
- 载有ACV的小胞体在预防和治疗环境中表现出与释放ACV相似的抗病毒功效.
- 在PVPA研究中,即使存在粘液,也显示了与菌体的增强ACV透性.
- 在 silico 模拟证实了 in vitro 透性增强.
结论:
- 负电荷的多乳微粒有效地提高了阿西克洛维尔 (ACV) 的溶解性和口服透性.
- 这种先进的药物输送系统具有显著的潜力,可以改善ACV的治疗结果.
- 开发出来的片为克服ACV生物可用性限制提供了一个有希望的策略,有可能改善患者的服药性并减少副作用.
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