Modulated approaches for strategic transportation of proteins and peptides via ocular route

The influence of macromolecules in major eye disorders including retinal neovascularization, retinopathy, age-related macular degeneration, choroidal neovascularization, etc. offers substantial advantages in the development of formulations, designing of new delivery approaches, and setting of new effective therapies. The transportation of proteins and peptides like recombinant proteins, aptamers, monoclonal antibodies face major challenges due to their high molecular weight (MW > 100 kDa), rapid degradation, low solubility and instability for long-term and alleviated condition.

To overcome such limitations, the ocular route offers major advantages like prevention of first-pass metabolism, high retention time, less degradation, ease of access for injectables as well as accurate dosing of dosage form. This review article focuses on newer and advanced approaches like dendrimers, nanoparticles/spheres, microparticles/spheres, minimally-invasive microneedles, stimuli-responsive polymeric systems, in-situ gel formulations, delivery using cell-penetrating peptide, use of penetration enhancers and prodrug approach, chemical chaperones, use of anti-VEGF agents, TNF-α agents, use of living cells, etc. for effective and strategic transportation of macromolecules across the eye for controlled and sustained delivery systems without significant adverse events.

For advancement in diagnostic and treatment, ophthalmic route is integrated with 3D printing, electronic chip-embedded drug delivery, artificial intelligence, teleophthalmology and quantum dots. These approaches propose efficient delivery of actives with lower toxicity and higher stability for serving the purpose of modernised delivery systems in near future.

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Article information: Maitri Bhatt, Pravin Shende, Modulated approaches for strategic transportation of proteins and peptides via ocular route, Journal of Drug Delivery Science and Technology, Volume 66, 2021. https://doi.org/10.1016/j.jddst.2021.102835.