塞来昔布眼部疾病治疗的递药系统：色素和糖尿病的影响。
Delivery of celecoxib for treating diseases of the eye: influence of pigment and diabetes.
机构信息
Quinitles, Inc., Clinical Pharmacology, Overland Park, KS 66211, USA.
出版信息
Expert Opin Drug Deliv. 2010 May;7(5):631-45. doi: 10.1517/17425241003663236.
IMPORTANCE OF THE FIELD
Age-related macular degeneration (AMD) and diabetic retinopathy (DR) are two major causes of blindness. In these disorders, growth factors such as vascular endothelial growth factor (VEGF) are upregulated, leading to either enhanced vascular permeability or proliferation of endothelium. While corticosteroid therapies available at present suffer from side effects including cataracts and elevated intraocular pressure, anti-VEGF antibody therapies require frequent intravitreal injections, a procedure that can potentially lead to retinal detachment or endophthalmitis. Thus, there is a need to develop safe, sustained release therapeutic approaches for treating AMD and DR.
AREAS COVERED IN THIS REVIEW
This review discusses the pharmacological basis for using celecoxib, an anti-inflammatory drug capable of selectively inhibiting cycloxygenase 2, in treating AMD and DR. In addition, this article discusses the safety, delivery advantage and efficacy of celecoxib by transscleral retinal delivery, a periocular delivery approach that is less invasive to the globe compared with intravitreal injections.
WHAT THE READER WILL GAIN
The reader will gain insights into the development of a pharmacological agent and a sustained release delivery system for treating DR and AMD. Further, the reader will gain insights into the influence of eye physiology including pigmentation and disease states such as DR on retinal drug delivery.
TAKE HOME MESSAGE
Transscleral sustained delivery of anti-inflammatory agents is a viable option for treating retinal disorders.
重要性领域
年龄相关性黄斑变性（AMD）和糖尿病性视网膜病变（DR）是导致失明的两个主要原因。在这些疾病中，血管内皮生长因子（VEGF）等生长因子上调，导致血管通透性增强或内皮细胞增殖。虽然目前可用的皮质类固醇疗法存在包括白内障和眼内压升高在内的副作用，但抗 VEGF 抗体疗法需要频繁的玻璃体内注射，这一过程可能导致视网膜脱离或眼内炎。因此，有必要开发安全、持续释放的治疗方法来治疗 AMD 和 DR。
本综述讨论了使用塞来昔布（一种能够选择性抑制环氧化酶 2 的抗炎药物）治疗 AMD 和 DR 的药理学基础。此外，本文还讨论了经巩膜视网膜递送（一种与玻璃体内注射相比对眼球侵袭性较小的眼周递送方法）的塞来昔布的安全性、递送优势和疗效。
读者将获得的收益
读者将深入了解治疗 DR 和 AMD 的药理学药物和持续释放递送系统的开发。此外，读者将深入了解眼生理学（包括色素沉着）和疾病状态（如 DR）对视网膜药物递送的影响。
带回家的信息
经巩膜持续递送抗炎药物是治疗视网膜疾病的可行选择。
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