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使用2-基-β-基基基菌片向眼部组织输送基酸盐

Butsabarat Klahan¹, Niall J O'Reilly¹, Hakon Hrafn Sigurdsson²

¹Ocular Therapeutics Research Group (OTRG), Pharmaceutical and Molecular Biotechnology Research Centre (PMBRC), South East Technological University (SETU), X91 K0EK Waterford, Ireland.

International journal of pharmaceutics

|March 1, 2025

概括

这项研究开发了多假罗塔xanes (PPRs) 来改善眼部药物输送的纤维酸 (FEB) 溶解度,显著增强眼部组织的药物透,用于潜在的治疗视力障碍疾病.

科学领域:

眼部药物输送眼部药物输送
纳米技术在医学中的应用
制药科学制药科学

背景情况:

与年龄相关的黄斑退化和糖尿病视网膜病变导致显著的视力损伤.
目前用于这些疾病的静脉内注射有副作用;局部输送是首选的,但受到眼壁的阻碍.
纤维酸 (FEB) 是一种水溶性较差的药物,需要增强的输送系统用于眼部应用.

研究的目的:

为了制备和表征使用2-基-β-环氧 (2-HPβCD),Pluronic® F127 (PF127) 和Soluplus®的多 (假) 基 (PPRs),我们使用Pluronic® F127 (PF127) 和 Soluplus®.
为了提高纤维酸 (FEB) 的溶解性和眼睛透性,用于潜在的眼睛疾病治疗.
为了研究药物封装,可溶性增强机制和透动力学.

主要方法:

使用动态光散射 (DLS),核磁共振 (NMR) 和X射线衍射 (XRD) 制备和描述FEB载荷的和PPR.
在准备的配方中对FEB可溶性增强的评估.
通过猪膜组织的ex vivo透研究和使用Fick定律的数学建模.

主要成果:

FEB成功地被封装成具有小颗粒大小 (7-67 nm) 的微粒和PPR.
通过添加2-HPβCD,FEB溶解度增加了910倍,证明了协同效应.
装有FEB的PPRs促进了FEB通过结膜组织的透,透水平从0.27到4.25μg/cm2不等.

结论:

聚假 (PPRs) 显示出作为一种有效的药物输送系统的显著潜力,用于眼部应用.
2-HPβCD的协同效应大大提高了水溶性较差的药物的可溶性,如FEB.
数学建模对于理解眼组织中药物透机制至关重要.

关键词:

2-HPβCDCD 是一种双HPβCD.菲诺纤维酸盐的使用方法微粒微粒 (Micelles) 是一种微粒.混合的米塞尔.第127章在PF127 多 (或伪) 罗塔克桑酸.

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