眼科用比马托普罗斯特载荷的尼奥索姆在位凝:准备,优化和体内药学动力学研究
Mohammed F Aldawsari1, Ehssan H Moglad1,2, Hadil Faris Alotaibi3
1Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
Polymers
|November 14, 2023
概括
这项研究开发了一种新型的niosomal in situ凝,用于眼部输送Bimatoprost,一种抗白血病剂. 新配方显著降低了子的眼内压力,没有观察到刺激,为玻璃眼癌治疗提供了一个有希望的替代方案.
科学领域:
- 制药科学 制药科学
- 眼科医生 眼科 眼科
- 药物输送系统 药物输送系统
背景情况:
- 玻璃眼是全球不可逆转的失明的主要原因.
- 由于眼睛的复杂解剖学和生理障碍,有效的眼部药物输送仍然是一个挑战.
- 比马托普罗斯特是一种有效的抗葡萄糖瘤药物,但需要经常服用.
研究的目的:
- 为了配制和表征比马托普罗斯特载体在位凝 (BMT-ISG) 增强眼部输送.
- 评估BMT-ISG配方的体外和体内性能.
- 评估尼奥索姆在位凝的潜力,作为一种可行的输送系统,用于抗瘤药物.
主要方法:
- 用胆固醇和Span 60进行薄膜水化方法制备封装Bimatoprost的尼奥索姆.
- 优化后的体被纳入基于Pluronic F127/F68的现场凝系统.
- 配方的特点是捕获效率,颗粒大小和sol-gel过渡温度.
- 在子中评估了体外药物释放和体内疗效 (眼内压力降低).
主要成果:
- 优化的BMT-ISG配方显示了高捕获效率 (81.2%) 和小颗粒大小 (167.3 nm).
- 在BMT-ISG展现了持续的体外药物释放24小时.
- 与Bimatoprost溶液 (5.8mmHg) 相比,BMT-ISG的局部眼部施用导致眼内压力显著降低 (9.7mmHg),比Bimatoprost溶液 (5.8mmHg) 大得多.
- 在BMT-ISG配方中没有观察到眼部刺激.
结论:
- 尼奥索姆 in situ 凝是一种可行的和有效的载体,用于局部眼部输送像比马托普罗斯特这样的抗白内障药物.
- 这种配方提供持续释放和提高降低眼内压力的有效性.
- 开发的BMT-ISG配方显示了改善患者遵守和治疗结果的潜力.
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