Clearside Biomedical Inc., 900 North Point Parkway, Suite 200, Alpharetta, GA 30005, United States of America.
Clearside Biomedical Inc., 900 North Point Parkway, Suite 200, Alpharetta, GA 30005, United States of America.
J Control Release. 2022 Sep;349:1045-1051. doi: 10.1016/j.jconrel.2022.05.061. Epub 2022 Sep 8.
Drug delivery to the suprachoroidal space (SCS®) has become a clinical reality after the 2021 FDA approval of CLS-TA, a triamcinolone acetonide injectable suspension for suprachoroidal use (XIPERE®), administered via a microneedle-based device, the SCS Microinjector®. Suprachoroidal (SC) delivery facilitates targeting, compartmentalization, and durability of small molecule suspensions, thereby potentially addressing some of the efficacy, safety, and treatment burden limitations of current retinal therapies. Herein, the design features of the SCS Microinjector are reviewed, along with the biomechanics of SC drug delivery. Also presented are preclinical evaluations of SC small molecule suspensions from 4 different therapeutic classes (plasma kallikrein inhibitor, receptor tyrosine kinase inhibitor, corticosteroid, complement factor D inhibitor), highlighting their potential for durability, targeted compartmentalization, and acceptable safety profiles following microinjector-based SC delivery. The clinical evaluations of the safety, tolerability and efficacy of SC delivered triamcinolone further supports potential of SC small molecule suspensions as a clinically viable strategy for the treatment of chorioretinal diseases. Also highlighted are current limitations, key pharmacological considerations, and future opportunities to optimize the SC microinjector platform for safe, effective, and potentially long-acting drug delivery for the treatment of chorioretinal disorders.
在 2021 年 FDA 批准 CLS-TA(一种用于脉络膜上腔的曲安奈德注射混悬剂,商品名:XIPERE®)后,药物递送至脉络膜上腔(SCS®)成为了临床现实,CLS-TA 通过基于微针的装置 SCS Microinjector®给药。脉络膜上腔(SC)给药有利于小分子混悬剂的靶向、分区和持久性,从而有可能解决当前视网膜治疗方法的一些疗效、安全性和治疗负担限制。本文回顾了 SCS Microinjector 的设计特点,以及 SC 药物递送的生物力学。还介绍了来自 4 个不同治疗类别的 SC 小分子混悬剂的临床前评估(血浆激肽释放酶抑制剂、受体酪氨酸激酶抑制剂、皮质类固醇、补体因子 D 抑制剂),突出了它们在基于微注射器的 SC 给药后具有持久性、靶向分区和可接受安全性的潜力。基于 SC 递送来的曲安奈德的安全性、耐受性和疗效的临床评估进一步支持了 SC 小分子混悬剂作为治疗脉络膜视网膜疾病的一种有临床应用前景的策略。还强调了当前的局限性、关键的药理学考虑因素,以及未来通过优化 SC 微注射器平台以实现安全、有效和潜在长效药物传递的机会,用于治疗脉络膜视网膜疾病。