奥利戈阿金宁的结构及其对细胞透的影响在眼部药物输送中
Stefana Duca1, Naa Dei Nikoi1, Madeline Berrow1
1School of Pharmacy, University of Nottingham, Nottingham, UK.
Heliyon
|August 22, 2024
概括
奥利高氨酸可以增强与年龄相关的黄斑变性 (AMD) 的眼部药物输送. 体长度在战略上准不同的眼睛细胞,改善治疗效果,没有毒性.
科学领域:
- 眼部药物输送是通过眼部药物输送的.
- 基于的治疗药物.
- 与年龄相关的黄斑变性 (AMD) 治疗
背景情况:
- 橄 arginine 细胞透 (CPP) 对于增强药物输送到细胞至关重要.
- 它们在用于AMD治疗的眼部局部配方中的应用具有显著的兴趣.
- 的长度和结构是影响药物递送效率的关键因素.
研究的目的:
- 为了研究橄 arginine 长度 (Rn) 对透机制的影响.
- 评估它们的药物递送能力和抗菌性质,用于潜在的AMD治疗.
- 提供关于优化CPP用于眼部交付的见解.
主要方法:
- 使用含有 carboxyfluorescein 的脂质体模型来评估孔形成能力.
- 评估了不同细菌类和CPP长度的抗菌疗效.
- 评估了与眼部输送相关的哺乳动物细胞的细胞毒性.
- 在*in vitro*眼细胞模型 (角膜和视网膜上皮质) 中研究了膜转移和货物输送.
主要成果:
- 奥利高氨酸表现出有限的孔隙形成,其中R9显示出显著的活性.
- 抗菌有效性随着长度的增加而增加,因细菌类而异.
- 奥利高氨酸对相关的哺乳动物眼细胞没有表现出任何毒性.
- 货物交付因细胞类型和长而异:较长的链有利于角膜细胞,较短的链有利于视网膜细胞.
- 膜转移是独立于货物的存在.
结论:
- 利氨酸CPP长度可以战略性地操纵,以在特定的眼部区域内向药物输送.
- 这为优化 AMD 和其他疾病的眼部局部配方提供了一种新的方法.
- 这些发现增强了对CPPs作为透增强剂的理解,以改善眼部治疗交付.
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