含有Ivermectin的半孔和聚合物纳米囊:对药物负载的影响,体内溶解能力的提高和释放性能
Maiara Callegaro Velho1,2, Nadine Lysyk Funk1,2, Monique Deon2,3
1Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 90610-000, RS, Brazil.
Pharmaceutics
|March 28, 2024
概括
与晶体IVM相比,对ivermectin (IVM) 在无机颗粒 (IVM-MCM) 和有机纳米 (IVM-NC) 的纳米封装显著提高了其水溶性和受控释放.
科学领域:
- 纳米技术纳米技术
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
背景情况:
- 甲 (IVM) 具有较差的水溶性和生物可用性,阻碍了其治疗应用.
- IVM的高脂性 (log P) 呈现出配方方面的挑战.
- 纳米封装提供了一种潜在的策略,可以改善IVM的溶解性和输送.
研究的目的:
- 为了研究IVM在无机半孔颗粒 (IVM-MCM) 和有机聚ε-烯酸) 纳米囊 (IVM-NC) 中的纳米封装.
- 为了比较IVM-MCM和IVM-NC的药物载荷,物理化学性质和体外释放概况.
- 评估这些纳米配方在增强IVM输送方面的潜力.
主要方法:
- 合成和表征IVM-MCM (无机) 和IVM-NC (有机) 的纳米粒子.
- 药物加载效率和物理化学稳定性的确定.
- 在 72 小时内使用透析袋方法进行体外药物释放研究.
主要成果:
- 与晶体形式相比,IVM-MCM和IVM-NC都显示了IVM的水溶性增强.
- IVM-MCM表现出高药物负载 (10% w/w),具有六角半孔结构.
- 与IVM-MCM (72%) 和晶体IVM (40%) 相比,IVM-NC显示出高封装效率 (100%),良好的稳定性和持续释放 (78%超过72小时).
结论:
- 在无机和有机纳米颗粒中的IVM纳米封装改善了其水溶性和药物释放.
- IVM-NC提供了更持久的释放特征,表明了改善治疗疗效的潜力.
- 对于优化的IVM纳米配方,需要进一步研究注射途径,安全性和临床转化.
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