眼部输送由比马托普罗斯特加载的固体脂质纳米颗粒,以有效管理玻璃眼瘤
Sandeep Divate Satyanarayana1, Amr Selim Abu Lila2,3, Afrasim Moin3
1Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Mangalore 575018, India.
Pharmaceuticals (Basel, Switzerland)
|July 29, 2023
概括
这项研究开发了含比马托普罗斯特的固体脂质纳米粒子 (SLN),以改善青光眼治疗. 优化的SLN增强了药物输送,并没有显示眼部刺激,为治疗青光眼提供了一种有前途的方法.
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:
- 玻璃眼瘤是一种渐进的视神经病变,由于眼内压力升高 (IOP) 导致视神经受损.
- 比马托普罗斯特是一种前列腺素模拟剂,有效降低了IOP,但在当前配方中眼部生物可用性较低.
- 开发先进的药物输送系统对于提高Bimatoprost在眼治疗中的有效性至关重要.
研究的目的:
- 为了制造和优化Bimatoprost装载的固体脂质纳米粒子 (SLNs) 以提高眼部输送.
- 评估开发的SLNs的物理化学性质,药物释放和眼睛耐受性.
- 评估SLNs作为改善Bimatoprost角膜透率和生物可用性的可行载体的潜力.
主要方法:
- 装有比马托普罗斯特的SLN使用溶剂蒸发/超声波技术与糖单酸盐 (GMS) 和407.7波洛克萨默 (poloxamer) 制备.
- 为了优化SLN,采用了中央复合设计.
- 特性包括粒子大小,泽塔潜力,捕获效率,TEM,药物释放研究,无菌性,同位素性,HET-CAM和组织病理学测试.
主要成果:
- 优化SLN的粒子大小为183.3 ± 13.3 nm,泽塔电位为-9.96 ± 1.2 mV,封装效率为71.8 ± 1.1%.
- 在HET-CAM和基因病理学研究中,SLN显示Bimatoprost持续释放长达12小时,并且没有显示眼部刺激.
- TEM揭示了几乎光滑表面的纳米大小的粒子.
结论:
- 固体脂质纳米颗粒 (SLN) 是Bimatoprost在青光眼治疗中的一个有前途的药物输送系统.
- 开发的SLN增强了比马托普罗斯特的眼部生物可用性和角膜透.
- 该配方安全用于眼部,没有显著的刺激或组织损伤.
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