聚的超分子输送系统:一种绿色方法,通过体外设置来预测体内透性
Maddalena Sguizzato1, Federica Agosta1, Antonella Ciancetta1
1Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, Via Luigi Borsari, 46, 44121 Ferrara, Italy.
International journal of pharmaceutics
|January 5, 2025
概括
这项研究探讨了使用β-cyclodextrins (CDs) 来改善口服药物输送的不溶性化合物,如 rutin, hesperidin 和黄素. 研究证实,CDs有效形成复合体,增强药物的透性和生物可用性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 绿色化学 绿色化学
背景情况:
- 开发用于预测体内药物透性的体外模型对于口服药物配方至关重要,特别是对于难以溶解和透的药物 (BCS Class II和IV).
- 绿色制药方法越来越多地利用自然分子作为治疗剂,需要提高其生物可用性的策略.
- 鲁丁,赫斯佩里丁和黄素被选为模型脂性药物,原因是它们的溶解度低,阻碍了它们的口服和治疗应用.
研究的目的:
- 为了研究β-cyclodextrins (CDs),特别是基-β-CD (HPBCD) 和甲基-β-CD (MBCD) 的潜力,以提高鲁丁,hesperidin和curcumin的可溶性,透性和生物利用性.
- 用各种分析技术来描述这些药物和CD之间形成的包容复合体.
- 用一种新的无细胞测定方法评估这些药物-CD复合物的体外透性.
主要方法:
- 阶段溶解性研究和对接计算被用来确认药物和CDs之间1:1的固体测量纳入复合物的形成.
- 使用UV-Vis局部光谱来评估CD药物复合物的扩散和稳定性.
- 通过PermeaPad®板,一个体外无细胞测定,被用来评估药物穿透度通过生物模拟膜.
- 动态光散射 (DLS) 被用来检测纳米超分子系统.
主要成果:
- 在与HPBCD和MBCD一起的鲁丁,赫斯佩里丁和黄素之间形成了稳定的1:1纳入复合体,增加了它们的水友性.
- 扩散实验证实了这些复合物的高稳定性,特别是黄素,表明它们是主要的扩散物种.
- 通过PermeaPad®测试,证明β-环氧的类型显著影响药物透性,反映了未水层 (UWL) 的影响.
- 光谱数学分析和DLS建议对黄素形成纳米超分子系统,验证了该模型的精度.
结论:
- β-环氧,特别是HPBCD和MBCD,有效地形成稳定的含有复合物,与低溶性药物如 rutin,hesperidin 和curcumin.
- 这些复合物增强药物的透性和生物可用性,为改善口服药物递送系统提供了一个有前途的战略.
- 无细胞PermeaPad®测定为评估药物透性提供了一个有价值的工具,受UWL等因素的影响,有助于合理设计药物配方.
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