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德菲拉西洛克斯纳米悬浮装载溶解微针用于眼部药物输送
Hafsa Shahid Faizi1, Muhammad Iqbal Nasiri2, Yu Wu3
1School of Pharmacy, Medical Biology Centre, Queen's University Belfast, 97 Lisburn Road, Belfast BT9 7BL, Northern Ireland, United Kingdom; College of Pharmacy, University of Sargodha, University Road, Sargodha, Punjab 40100, Pakistan.
International journal of pharmaceutics
|August 21, 2024
概括
装入微针的deferasirox (DFS) 纳米悬浮为治疗视网膜疾病提供了一种不那么侵入性的方法. 这种新方法改善了药物的溶解性和向眼睛的输送,增强了神经保护.
科学领域:
- 眼科医生 眼科 眼科
- 纳米技术 纳米技术
- 药物输送系统 药物输送系统
背景情况:
- 德费拉西洛克斯 (DFS) 是一种口服铁化剂,具有神经保护性,有利于治疗视网膜疾病,如与年龄相关的黄斑变性 (AMD).
- 传统的口服DFS面临挑战,包括频繁的剂量和第一通代谢.
- 微针 (MNs) 提供了一个微侵袭的替代方案,用于内药物输送,可能克服口服和内途径的局限性.
研究的目的:
- 开发和评估装入纳米悬浮 (NS) 的deferasirox (DFS),并将其纳入聚合物溶解微针 (MN) 中,用于眼部药物输送.
- 评估DFS-NS装载微针 (DFS-NS-OcMNs) 的溶解性,稳定性,机械性能和眼组织透率.
- 评估DFS-NS-OcMNs的安全性和有效性,用于将DFS输送到眼睛的后部.
主要方法:
- 通过使用聚乙醇 (PVA) 作为稳定剂的湿媒磨,DFS被制成纳米悬浮 (NS).
- DFS-NS被装入聚合物溶解微针 (OcMNs) 中.
- 评估了溶解性,稳定性 (通过TGA进行短期和热),机械强度,膜透 (OCT成像),药物沉积 (膜沉积研究) 和细胞活力 (ARPE细胞).
主要成果:
- 与纯粹的DFS相比,DFS-NS显示溶解度增加了4倍.
- DFS-NS-OcMNs显示出足够的机械强度来穿透膜,其中81.23 ± 7.35%的MN高度被插入猪膜.
- 膜沉积研究显示,DFS-NS-OcMNs在5分钟内沉积了64%的药物,几乎是纯DFS-OcMNs的5倍.
- 无论是DFS还是DFS-NS-OcMN,都在人类视网膜色素 (ARPE) 细胞上表现出良好的细胞活力.
结论:
- 将DFS制成纳米悬浮剂显著提高了其溶解性和稳定性.
- 装有DFS-NS的聚合物溶解微针提供了一种有效和最少的侵入性方法,用于将DFS输送到眼睛后部.
- DFS-NS-OcMNs显示出作为用于治疗视网膜疾病的传统DFS输送方法的安全和有效替代品的潜力.
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