泪液性质对转移体理化、黏附及眼内渗透特性的影响。

IF 4.4 2区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-11 DOI:10.1016/j.ejpb.2025.114745

Santosh Bhujbal , Priyanka Agarwal , Soma Sengupta , Cornelia M. Keck , Ilva D. Rupenthal

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引用次数: 0

摘要

由于干眼症（DED）患者泪液特性的改变，滴眼液的性能可能会改变。本研究探讨了泪液性质对转移体（TFS）滴眼液的理化、黏附及眼内渗透特性的影响。具体而言，研究了泪液pH值和渗透压对未加载以及加载姜黄素和托那伯塞的TFS的囊泡大小、多分散性指数（PDI）和ζ电位（ZP）的影响。最后，利用离体猪角膜-巩膜椎间盘研究了泪液性质改变对姜黄素TFS角膜渗透的影响。与水相比，姜黄素和托纳伯沙TFS悬浮在健康和DED泪液中，其囊泡大小和PDI显著增加。此外，在健康泪液和DED泪液中，水中测量的ZP向中性偏移，表明囊泡的静电稳定性降低。与健康泪液中悬浮的TFS相比，悬浮在水中的姜黄素TFS的组织渗透性更深，而与DED泪液混合的TFS渗透性明显更低。本研究证实泪液性质显著影响TFS特性，从而影响其穿透能力，强调了在反映疾病状态的生理条件下评估眼部药物传递系统的重要性。

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Influence of tear fluid properties on physicochemical, mucoadhesion and ocular penetration characteristics of transfersomes

Due to changes in the tear fluid properties in dry eye disease (DED), eye drop performance may be altered. This study investigated the impact of tear fluid properties on the physicochemical, mucoadhesion and ocular penetration characteristics of transfersome (TFS) eye drops. Specifically, the effect of tear fluid pH and osmolarity on vesicle size, polydispersibility index (PDI) and zeta potential (ZP) of unloaded as well as curcumin- and tonabersat-loaded TFS were studied. Finally, the effect of altered tear fluid properties on corneal penetration of curcumin TFS was investigated using ex vivo porcine corneo-scleral discs. A significant increase in vesicle size and PDI was observed for curcumin and tonabersat TFS suspended in healthy and DED tears compared to water. Moreover, the ZP measured in water shifted towards neutral in the case of healthy and DED tears, suggesting reduced electrostatic stability of the vesicles. Deeper tissue penetration was observed for curcumin TFS suspended in water compared to TFS suspended in healthy tears, with significantly less penetration for TFS mixed with DED tears. This study confirmed that tear fluid properties significantly influence TFS characteristics and thus their penetration ability, highlighting the importance of evaluating ocular drug delivery systems under physiological conditions that reflect the disease state.

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来源期刊

European Journal of Pharmaceutics and Biopharmaceutics 医学-药学

CiteScore

8.80

自引率

4.10%

发文量

211

审稿时长

36 days

期刊介绍： The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.