将水溶性差的物质无创导入眼球的新平台

O. Strauss
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摘要

时至今日,使用油性眼药水和非侵入性视网膜给药仍是一项重大挑战。油性眼药水通常会对眼部造成刺激,影响眼睛的正常功能,而眼部注射视网膜给药会造成严重的不良反应,给医疗系统带来沉重负担。在此,作者报告了一种新型局部非侵入性眼部给药平台(NIODP),通过眶周皮肤在非人灵长类动物模型(NHP)中实现高效的眼部前后给药。通过 NIODP 输送单剂量约 7 毫克 JV-MD2(欧米茄 3 DHA),到达视网膜的 Cmax 为 111 微克/克,到达角膜的 Cmax 为 66 微克/克。NIODP 还能像眼药水一样有效地将正在开发的干眼病抗炎药 JV-DE1 输送到 NHP 的前段。局部 NIODP 似乎可以通过角膜途径将候选药物输送到眼球前段,并通过结膜/巩膜途径输送到眼球后段。新型 NIODP 方法有可能重塑眼部给药的格局。对于油性眼药水和视网膜给药来说尤其如此,因为治疗的成功与否取决于药物在目标组织中的眼部耐受性和生物利用度。
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Eine neue Plattform zum nicht invasiven Einbringen schlecht wasserlöslicher Substanzen ins Auge
To this day, the use of oily eye drops and non-invasive retinal delivery remain a major challenge. Oily eye drops usually cause ocular irritation and interfere with the normal functioning of the eye, while ocular injections for retinal drug delivery cause significant adverse effects and a high burden on the healthcare system. Here, the authors report a novel topical non-invasive ocular delivery platform (NIODP) through the periorbital skin for high-efficiency anterior and posterior ocular delivery in a non-human primate model (NHP). A single dose of about 7 mg JV-MD2 (omega 3 DHA) was delivered via the NIODP and reached the retina at a Cmax of 111 μg/g and the cornea at a Cmax of 66 μg/g. The NIODP also delivered JV-DE1, an anti-inflammatory agent in development for dry eye diseases, as efficiently as eye drops did to the anterior segments of the NHP. The topical NIODP seems to transport drug candidates through the corneal pathway to the anterior and via the conjunctiva/sclera pathway to the posterior segments of the eye. The novel NIODP method has the potential to reshape the landscape of ocular drug delivery. This is especially the case for oily eye drops and retinal delivery, where the success of the treatment lies in the ocular tolerability and bioavailability of drugs in the target tissue.
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