聚合物纳米颗粒的配方加载巴里西提尼布作为眼部应用的局部方法
Negar Beirampour1, Paola Bustos-Salgado1,2, Núria Garrós1
1Departament de Farmàcia i Tecnologia Farmacèutica, i Fisicoquímica, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, Spain.
Pharmaceutics
|August 29, 2024
概括
这项研究开发了优化的PLGA和PCL纳米颗粒,用于增强巴里西提尼布 (BTB) 的眼部药物输送. 这些安全有效的纳米颗粒可以改善药物透和保持在眼睛中的情况.
科学领域:
- 眼科医生 眼科 眼科
- 纳米技术纳米技术
- 药品制造 药品制造 药品制造
背景情况:
- 局部眼部药物输送是具有挑战性的,因为生理障碍和快速的眼周转率.
- 由于药物透性和生物可用性差,传统的眼滴的有效性有限.
- 纳米粒子为眼部药物输送提供了潜在的优势,包括提高溶解度,控制释放和向输送.
研究的目的:
- 设计和优化用于眼部输送巴里西提尼布 (BTB) 的聚乳-同-甘油酸 (PLGA) 和聚烯酸 (PCL) 纳米颗粒.
- 评估开发的纳米粒子配方的物理化学性质,微生物安全性,ex vivo透性和体外眼睛耐受性.
主要方法:
- 用因数设计 (2^3+星设计) 来进行纳米粒子优化.
- 纳米颗粒的特征包括尺寸,多分散度指数,表面电荷和捕获效率.
- 使用挑战测试来评估微生物安全性.
- 通过猪角膜进行了ex vivo透研究.
- 在实验室内对眼睛的耐受性进行了评估,包括HET-CAM测试.
主要成果:
- 优化的PLGA和PCL纳米粒子显示出小尺寸,低多分散性,负表面电荷和高捕获效率.
- 这些纳米粒子配方通过了挑战测试,表明了微生物安全性.
- 与普通溶液相比,ex vivo研究显示巴里替尼的透系数增加了15倍以上.
- 纳米颗粒证明了药物保留和角膜组织中的储存效应.
- 在体外眼睛耐受性研究和HET-CAM测试证实没有显著的刺激性.
结论:
- PLGA和PCL纳米颗粒是有效的载体,用于眼部巴里西提尼布的输送.
- 开发的纳米粒子增强药物透和保持在眼睛组织内.
- 这些配方显示出安全和改善局部眼部药物输送的有希望的潜力,最大限度地减少全身暴露.
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