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首页> 美国卫生研究院文献>Ophthalmology and Eye Diseases >The role of KPI-121 0.25 in the treatment of dry eye disease: penetrating the mucus barrier to treat periodic flares
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The role of KPI-121 0.25 in the treatment of dry eye disease: penetrating the mucus barrier to treat periodic flares

机译：KPI-121 0.25％在治疗干眼症的作用：穿透粘液屏障治疗周期性耀斑

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The tear film, which includes mucins that adhere to foreign particles, rapidly clears allergens and pathogens from the ocular surface, protecting the underlying tissues. However, the tear film’s ability to efficiently remove foreign particles during blinking can also pose challenges for topical drug delivery, as traditional eye drops (solutions and suspensions) are cleared from the ocular surface before the drug can penetrate into the conjunctival and corneal epithelium. In the past 15 years, there has been an increase in the development of nanoparticles with specialized coatings that have reduced affinity to mucins and are small enough in size to pass through the mucus barrier. These mucus-penetrating particles (MPPs) have been shown to efficiently penetrate the mucus barrier and reach the ocular surface tissues. Dry eye disease (DED) is a common inflammatory ocular surface disorder that often presents with periodic flares (exacerbations). However, currently approved immunomodulatory treatments for DED are intended for long-term use. Thus, there is a need for effective short-term treatments that can address intermittent flares of DED. Loteprednol etabonate, an ocular corticosteroid, was engineered to break down rapidly after administration to the ocular surface tissues and thereby reduce risks associated with other topical steroids. KPI-121 is an ophthalmic suspension that uses the MPP technology to deliver loteprednol etabonate more efficiently to the ocular tissues, achieving in animal models a 3.6-fold greater penetration of loteprednol etabonate to the cornea than traditional loteprednol etabonate ophthalmic suspensions. In clinical trials, short-term treatment with KPI-121 0.25% significantly reduced signs and symptoms of DED compared with its vehicle (placebo). Recently approved KPI-121 0.25%, with its novel drug delivery design and ease of use, has the potential to effectively treat periodic flares of DED experienced by many patients.
机译：包括粘附到异物颗粒的粘膜，迅速清除来自眼表面的过敏原和病原体，保护下面的组织。然而，撕裂膜在闪烁期间有效地除去外来颗粒的能力也可以对局部药物递送构成挑战，因为传统的眼药水（溶液和悬浮液）在药物渗透到结膜和角膜上皮中之前从眼表面清除。在过去的15年中，纳米颗粒的开发有增加，具有对粘蛋白的亲和力降低的专用涂层，并且尺寸足够小，以通过粘液屏障。已经显示出这些粘液穿透颗粒（MPPS），以有效地渗透粘液屏障并到达眼表面组织。干眼症（DED）是一种常见的炎症眼疾病，通常具有周期性耀斑（恶化）。然而，目前批准的德国免疫调节治疗旨在长期使用。因此，需要有效的短期处理，可以解决DED的间歇性耀斑。 Loteprednol eTabonate，一种眼皮质类固醇，在给予眼部组织后，在给予眼部组织后迅速分解，从而降低与其他局部类固醇相关的风险。 KPI-121是一种眼科悬浮液，使用MPP技术更有效地向眼部组织提供LotePrednol Etabonate，在动物模型中实现3.6倍，比传统的单萜烯酸酯眼科悬浮液对角膜更大的3.6倍更大的渗透。在临床试验中，KPI-121的短期治疗0.25％显着降低了与其车辆（安慰剂）相比的症状和症状。最近批准的KPI-121 0.25％，其新的药物递送设计和易用性，有可能有效地治疗许多患者经验丰富的定期耀斑。

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