Joseph Mary, Trinh Hoang M, Cholkar Kishore, Pal Dhananjay, Mitra Ashim K
a Division of Pharmaceutical Sciences, School of Pharmacy , University of Missouri-Kansas City , Kansas City , MO , USA.
b Formulations R&D , RiconPharma LLC , Denville , NJ , USA.
Expert Opin Drug Deliv. 2017 May;14(5):631-645. doi: 10.1080/17425247.2016.1227783. Epub 2016 Sep 6.
Biologics are generally macromolecules, large in size with poor stability in biological environments. Delivery of biologics to tissues at the back of the eye remains a challenge. To overcome these challenges and treat posterior ocular diseases, several novel approaches have been developed. Nanotechnology-based delivery systems, like drug encapsulation technology, macromolecule implants and gene delivery are under investigation. We provide an overview of emerging technologies for biologics delivery to back of the eye tissues. Moreover, new biologic drugs currently in clinical trials for ocular neovascular diseases have been discussed. Areas covered: Anatomy of the eye, posterior segment disease and diagnosis, barriers to biologic delivery, ocular pharmacokinetic, novel biologic delivery system Expert opinion: Anti-VEGF therapy represents a significant advance in developing biologics for the treatment of ocular neovascular diseases. Various strategies for biologic delivery to posterior ocular tissues are under development with some in early or late stages of clinical trials. Despite significant progress in the delivery of biologics, there is unmet need to develop sustained delivery of biologics with nearly zero-order release kinetics to the back of the eye tissues. In addition, elevated intraocular pressure associated with frequent intravitreal injections of macromolecules is another concern that needs to be addressed.
生物制剂通常是大分子,尺寸较大,在生物环境中稳定性较差。将生物制剂递送至眼后部组织仍然是一项挑战。为了克服这些挑战并治疗后部眼部疾病,已开发出几种新方法。基于纳米技术的递送系统,如药物包封技术、大分子植入物和基因递送等正在研究中。我们概述了用于将生物制剂递送至眼后部组织的新兴技术。此外,还讨论了目前正在进行眼部新生血管疾病临床试验的新型生物药物。涵盖领域:眼睛解剖结构、眼后段疾病与诊断、生物制剂递送的障碍、眼部药代动力学、新型生物制剂递送系统 专家观点:抗血管内皮生长因子(VEGF)疗法在开发用于治疗眼部新生血管疾病的生物制剂方面取得了重大进展。目前正在开发多种将生物制剂递送至眼后部组织的策略,其中一些处于临床试验的早期或晚期阶段。尽管在生物制剂递送方面取得了重大进展,但仍有未满足的需求,即开发具有接近零级释放动力学的生物制剂向眼后部组织的持续递送。此外,与频繁玻璃体内注射大分子相关的眼内压升高是另一个需要解决的问题。