Yasukawa Tsutomu, Tabata Yasuhiko, Kimura Hideya, Ogura Yuichiro
Department of Ophthalmology and Visual Science, Nagoya City University Graduate School of Medical Sciences, Nagoya, Japan.
Recent Pat Drug Deliv Formul. 2011 Jan;5(1):1-10. doi: 10.2174/187221111794109529.
Vitreoretinal diseases are refractory to both topical and systemic pharmacological approaches because of specific environment of the eye. That is, the cornea, the sclera, nasolacrimal drainage of tears, frontward stream of aqueous humor, blood-aqueous barrier, and blood-retinal barrier strictly limit penetration and diffusion of drug into the retina. However, recent advances in intraocular drug delivery systems (DDS) have enabled drug to be delivered effectively into the eye. Clinically successful or promising cases involve non-biodegradable implants and inserts, biodegradable inserts and microparticles, intravitreal or sub-Tenon's injection of triamcinolone acetonide, and a photodynamic therapy (PDT) with verteporfin, a photosensitizer. More recently, a variety of pharmacological challenges to treat exudative age-related macular degeneration and macular edema are proceeding into clinical trials, as soon as anti-vascular endothelial growth factor (anti-VEGF) therapies have been proved to be effective by repeated intravitreal injections. In the near future, DDS must be required not only to develop a new treatment modality but also to improve efficacy and/or reduce injection numbers of currently available drugs. Here we introduce controlled release of drug and discussion of recent patents with biodegradable or non-biodegradable implants and drug targeting by modification of systemically administered drug.
由于眼睛的特殊环境,玻璃体视网膜疾病对局部和全身药物治疗均难以奏效。也就是说,角膜、巩膜、鼻泪管的泪液引流、房水的向前流动、血-房水屏障以及血-视网膜屏障严格限制了药物向视网膜的渗透和扩散。然而,眼内给药系统(DDS)的最新进展已使药物能够有效地递送至眼内。临床上成功或有前景的案例包括不可生物降解的植入物和插入物、可生物降解的插入物和微粒、玻璃体内或Tenon囊下注射曲安奈德,以及使用光敏剂维替泊芬的光动力疗法(PDT)。最近,随着反复玻璃体内注射抗血管内皮生长因子(anti-VEGF)疗法被证明有效,多种治疗渗出性年龄相关性黄斑变性和黄斑水肿的药物挑战正在进入临床试验阶段。在不久的将来,DDS不仅必须开发新的治疗方式,还必须提高现有药物的疗效和/或减少注射次数。在此我们介绍药物的控释以及对近期关于可生物降解或不可生物降解植入物的专利的讨论,还有通过修饰全身给药药物实现的药物靶向。