Laboratory of General Biochemistry and Physical Pharmacy, Faculty of Pharmaceutical Sciences, Ghent University, 9000 Ghent, Belgium.
Department of Ophthalmology, Ghent University Hospital, Corneel Heymanslaan 10, 9000 Ghent, Belgium.
J Control Release. 2021 May 10;333:560-578. doi: 10.1016/j.jconrel.2021.04.008. Epub 2021 Apr 16.
Biologics, like peptides, proteins and nucleic acids, have proven to be promising drugs for the treatment of numerous diseases. However, besides the off label use of the monoclonal antibody bevacizumab for the treatment of corneal neovascularization, to date no other biologics for corneal diseases have reached the market. Indeed, delivering biologics in the eye remains a challenge, especially at the level of the cornea. While it appears to be a rather accessible tissue for the administration of drugs, the cornea in fact presents several anatomical barriers to delivery. In addition, also intracellular delivery barriers need to be overcome to achieve a promising therapeutic outcome with biologics. This review outlines efforts that have been reported to successfully deliver biologics into the cornea. Biochemical and physical methods for achieving delivery of biologics in the cornea are discussed, with a critical view on their efficacy in overcoming corneal barriers.
生物制剂,如肽、蛋白质和核酸,已被证明是治疗许多疾病的有前途的药物。然而,除了单克隆抗体贝伐单抗被超适应证用于治疗角膜新生血管化之外,迄今为止,尚无其他用于治疗眼部疾病的生物制剂进入市场。事实上,将生物制剂递送至眼部仍然是一个挑战,尤其是在角膜水平。尽管看起来药物给药似乎是一种相对容易的组织,但角膜实际上存在多种解剖屏障来阻止药物的传递。此外,还需要克服细胞内递药的障碍,才能使生物制剂获得有前景的治疗效果。本文综述了成功将生物制剂递送至角膜的研究进展。讨论了用于实现生物制剂在角膜中递药的生化和物理方法,并对其克服角膜屏障的效果进行了批判性评价。
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