开发和优化vildagliptin固体脂质纳米颗粒载荷的ocuserts控制眼部输送:一个有希望的方法来治疗糖尿病视网膜病变
Abd El Hakim Ramadan1, Mahmoud M A Elsayed2, Amani Elsayed3
1Department of Pharmaceutics, Faculty of Pharmacy, Port Said University, Port Said 42515, Egypt.
International journal of pharmaceutics: X
|February 15, 2024
概括
新的眼睛插入器使用固体脂质纳米粒子 (SLNPs) 输送维达格利普丁 (VLD),以有效治疗糖尿病视网膜病变 (DRP). 这种方法增强了药物输送,减少了副作用,并为管理DRP提供了一个有希望的替代方案.
科学领域:
- 眼科和制药科学 眼科和制药科学
- 药物输送系统 药物输送系统
- 纳米技术在医学中的应用
背景情况:
- 糖尿病视网膜病变 (DRP) 是糖尿病 (DM) 的一个主要的微血管并发症.
- 维尔达利普丁 (VLD) 通过减少眼部炎症和改善视网膜血液流动,显示出对DRP治疗的潜力,但口服导致不良影响.
- 目前的VLD输送方法面临挑战,原因是眼睛吸收不良,剂量频繁,以及全身副作用.
研究的目的:
- 为了开发和优化vildagliptin固体脂质纳米颗粒 occuserts (VLD-SLNPs-OCUs) 进行有效的DRP治疗.
- 克服口服VLD的局限性,例如耐受性差和全身副作用.
- 为了增强眼部药物输送,延长保留时间,并实现延长药物释放以获得持续的治疗效果.
主要方法:
- 固体脂质纳米粒子 (SLNPs) 使用双乳液/溶分散技术进行制备.
- 最佳的SLNP公式被纳入了奥克苏斯特 (OCU).
- 使用盒式设计 (BBD) 来优化和开发VLD-SLNPs-OCU,随后进行了*in vitro*和*in vivo*药物释放研究以及眼部刺激测试.
主要成果:
- 优化的VLD-SLNPs-OCU实现了高药载荷效率95.28 ± 2.87%.
- 差分扫描热量计 (DSC) 证实了VLD的无形状态及其在ocusert矩阵中的均分布.
- *在体外*和体内*的药物释放研究显示,VLD在24小时内持续释放 (36.89 ± 3.11%和35.12 ± 2.47%,分别),配方没有显示眼部刺激.
结论:
- VLD-SLNPs-OCU提供了一种先进的药物输送系统,用于持续的VLD释放,最大限度地减少与口服相关的全身不良影响.
- 这种新的配方为糖尿病视网膜病变治疗提供了一个有前途的替代方案,有可能改善超出血糖控制的视网膜微血管血流.
- 开发的体证明了安全性和有效性,为改善DRP的管理铺平了道路.
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