Varela-Fernández Rubén, Díaz-Tomé Victoria, Luaces-Rodríguez Andrea, Conde-Penedo Andrea, García-Otero Xurxo, Luzardo-Álvarez Asteria, Fernández-Ferreiro Anxo, Otero-Espinar Francisco J
Department of Pharmacology, Pharmacy and Pharmaceutical Technology, University of Santiago de Compostela (USC), Campus vida, 15782 Santiago de Compostela, Spain.
Clinical Neurosciences Group, University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), Travesía da Choupana s/n, 15706 Santiago de Compostela, Spain.
Pharmaceutics. 2020 Mar 16;12(3):269. doi: 10.3390/pharmaceutics12030269.
The treatment of the posterior-segment ocular diseases, such as age-related eye diseases (AMD) or diabetic retinopathy (DR), present a challenge for ophthalmologists due to the complex anatomy and physiology of the eye. This specialized organ is composed of various static and dynamic barriers that restrict drug delivery into the target site of action. Despite numerous efforts, effective intraocular drug delivery remains unresolved and, therefore, it is highly desirable to improve the current treatments of diseases affecting the posterior cavity. This review article gives an overview of pharmacokinetic and biopharmaceutics aspects for the most commonly-used ocular administration routes (intravitreal, topical, systemic, and periocular), including information of the absorption, distribution, and elimination, as well as the benefits and limitations of each one. This article also encompasses different conventional and novel drug delivery systems designed and developed to improve drug pharmacokinetics intended for the posterior ocular segment treatment.
由于眼睛复杂的解剖结构和生理机能，后段眼部疾病（如年龄相关性眼病（AMD）或糖尿病性视网膜病变（DR））的治疗对眼科医生而言是一项挑战。这个特殊的器官由各种静态和动态屏障组成，这些屏障限制了药物输送到作用靶点。尽管付出了诸多努力，但有效的眼内药物递送问题仍未解决，因此，非常需要改进目前对影响后房疾病的治疗方法。这篇综述文章概述了最常用的眼部给药途径（玻璃体内注射、局部给药、全身给药和眼周给药）的药代动力学和生物药剂学方面的内容，包括吸收、分布和消除的信息，以及每种给药途径的优缺点。本文还涵盖了为改善用于后段眼部治疗的药物药代动力学而设计和开发的不同传统和新型药物递送系统。
