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超高分子量透明质酸作为治疗性滴眼液的增强载体:在一种新型青光眼用拉坦前列素制剂中的应用。

Very High Molecular Weight Hyaluronic Acid as an Enhanced Vehicle in Therapeutic Eye Drops: Application in a Novel Latanoprost Formulation for Glaucoma.

作者信息

Pujol-Martí Jesús, Müller-Lierheim Wolfgang G K

机构信息

i.com Medical GmbH, 81241 Munich, Germany.

出版信息

Bioengineering (Basel). 2025 Aug 24;12(9):907. doi: 10.3390/bioengineering12090907.

Abstract

The efficacy of topical drug delivery via eye drops is often achieved at the expense of tolerability, and consequently, efforts are being made to design strategies that minimize the adverse effects associated with the passage of active pharmaceutical ingredients (APIs) across the ocular surface. Many of these approaches are too complex, costly and challenging to implement on an industrial scale, yet there is increasing evidence that hylan A, a very high molecular weight hyaluronic acid (≥3.0 MDa), may be a promising vehicle for topical drug delivery of ocular therapies. In this review, we explore how the mucoadhesive and viscoelastic properties of eye drop formulations based on hylan A help extend the residence time of APIs at the ocular surface, while maintaining patient comfort. Moreover, we examine how hylan A facilitates the dissolution and stabilization of APIs, as well as their transport across the ocular epithelial barrier, without the need to use toxic penetration enhancers, thereby preserving ocular surface health. Finally, we present evidence indicating that the intrinsic biological properties of hylan A, including its anti-inflammatory effects, help mitigate side effects commonly associated with certain APIs. To illustrate these advantages, we examine the pioneering use of a hylan A-based aqueous eye drop formulation as a vehicle to deliver latanoprost, a prostaglandin analogue widely used in the treatment of glaucoma. This case study demonstrates the potential of hylan A-based eye drops to offer safer and more effective topical drug delivery, especially for long-term ocular therapies where tolerability and biocompatibility are critical.

摘要

通过滴眼液进行局部给药的疗效通常是以耐受性为代价实现的,因此,人们正在努力设计各种策略,以尽量减少与活性药物成分(API)透过眼表相关的不良反应。其中许多方法过于复杂、成本高昂且在工业规模上实施具有挑战性,但越来越多的证据表明,高分子量透明质酸(≥3.0 MDa)的海兰A可能是眼部治疗局部给药的一种有前景的载体。在本综述中,我们探讨了基于海兰A的滴眼液制剂的粘膜粘附和粘弹性特性如何有助于延长API在眼表的停留时间,同时保持患者的舒适度。此外,我们研究了海兰A如何促进API的溶解和稳定,以及它们穿过眼上皮屏障的运输,而无需使用有毒的渗透促进剂,从而保护眼表健康。最后,我们提供的证据表明,海兰A的内在生物学特性,包括其抗炎作用,有助于减轻通常与某些API相关的副作用。为了说明这些优势,我们研究了一种基于海兰A的水性滴眼液制剂作为载体递送拉坦前列素的开创性应用,拉坦前列素是一种广泛用于治疗青光眼的前列腺素类似物。该案例研究证明了基于海兰A的滴眼液在提供更安全、更有效的局部给药方面的潜力,特别是对于耐受性和生物相容性至关重要的长期眼部治疗。

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