Functionalized liposomes for intranasal levodopa delivery to the brain.

IF 2.4 4区医学 Q3 CHEMISTRY, MEDICINAL

Drug Development and Industrial Pharmacy Pub Date : 2025-05-27 DOI:10.1080/03639045.2025.2509273

Daria S Gordeeva, Achraf Sym Tameloucht, Irina I Semina, Rouslan I Moustafine

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引用次数: 0

Abstract

Objective: The study evaluated functionalized liposomes as potential carriers for intranasal delivery of levodopa.

Methods: Lipid film hydration method was used to obtain conventional and functionalized liposomes with polyethylene glycol or maleimide-PEG. The liposome structure was analyzed by dynamic light scattering and ¹H-NMR spectroscopy. Isolated sheep nasal mucosa was used for mucoadhesion and mucous penetration studies. Levodopa release was assessed using a Franz diffusion cell. In vivo experiments were conducted using a method based on the inhibition of dopaminergic transmission.

Results: The average liposome diameter was 81-91 ± 1 nm. The Pdi was less than 0.300. The zeta potential was negative. An increase in the molar weight of polyethylene glycol in the liposome structure improved mucosa penetration to 0.4 mm. The presence of maleimide did not affect the mucoadhesive properties. The levodopa release profile corresponded to Fickian diffusion. Intranasal administration of levodopa in vivo caused dopaminergic transmission inhibition in rats after 1 h.

Conclusion: According to the received results, functionalized liposomes are promising for further evaluation as intranasal drug carriers.

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左旋多巴经鼻入脑的功能化脂质体。

目的：研究功能化脂质体作为左旋多巴鼻内给药的潜在载体。方法：采用脂膜水合法分别用聚乙二醇或马来酰亚胺-聚乙二醇制备常规脂质体和功能化脂质体。采用动态光散射和1H-NMR分析了脂质体的结构。采用离体羊鼻黏膜进行粘膜粘连和粘膜渗透研究。用Franz扩散池测定左旋多巴释放量。体内实验采用基于抑制多巴胺能传递的方法进行。结果：脂质体平均直径为81 ~ 91±1 nm。Pdi小于0.300。电位是负的。脂质体结构中聚乙二醇摩尔质量的增加使粘膜穿透提高到0.4 mm。马来酰亚胺的存在对粘接性能没有影响。左旋多巴释放曲线符合菲克氏扩散。左旋多巴在大鼠体内经鼻给药1小时后可抑制多巴胺能传递。结论：功能化脂质体作为鼻内药物载体具有广阔的应用前景。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Drug Development and Industrial Pharmacy 医学-药学

CiteScore

6.80

自引率

0.00%

发文量

审稿时长

4.5 months

期刊介绍： The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.