Abstract
Ocular disorders originating in the retina can result in a partial or total loss of vision, making drug delivery to the retina of vital importance. However, effectively delivering drugs to the retina remains a challenge for ophthalmologists due to various anatomical and physicochemical barriers in the eye. This review introduces diverse administration routes and the accordant pharmacokinetic profiles of ocular drugs to aid in the development of safe and efficient drug delivery systems to the retina with a focus on peptidomimetics as a growing class of retinal drugs, which have great therapeutic potential and a high degree of specificity. We also discuss the pharmacokinetic profiles of small molecule drugs due to their structural similarity to small peptidomimetics. Lastly, various formulation strategies are suggested to overcome pharmacokinetic hurdles such as solubility, retention time, enzymatic degradation, tissue targeting, and membrane permeability. This knowledge can be used to help design ocular delivery platforms for peptidomimetics, not only for the treatment of various retinal diseases, but also for the selection of potential peptidomimetic drug targets.
Highlights
This review aims to discuss the potential of small molecule peptidomimetics as promising retinal drugs with their pharmacokinetic consideration
Alkoxyalkyl chains can be cleaved via cellular enzymes, resulting in release of the parent drugs. This technique has been used for the long-lasting efficacy of both retinal drugs cidofovir and 9-(S)-(3-Hydroxyl-2-Phosphonomehoxypropyl)adenine, which are hydrophilic small nucleoside antiviral drugs used to treat retinal inflammation caused by cytomegalovirus (CMV) [106,108]
This study provided a promising strategy in Cell penetrating peptides (CPPs) sequence modification for retinal drug delivery, the overall in vivo pharmacokinetic profiles of modified CPP after drug incorporation needs confirmation
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Peptidomimetics have gained traction as potential therapeutics, and the number of peptide-based drugs is expected to rise [4,5] They often exhibit superior selectivity (i.e., low off-target effects) relative to small molecules and are relatively straightforward to synthesize compared to other classes of biopharmaceutics. Peptidomimetics consist of a large class of molecules that mimic the natural protein interactions of peptides [6] They can possess a high degree of peptide character, where side chain and/or backbone modifications are used to enhance the physicochemical properties while maintaining the general peptide motif. They can be more small molecule-like, where a non-peptide based chemical scaffold projects substituents in an appropriate orientation to imitate the natural protein–peptide interactions. We discuss various ocular drug formulation strategies to overcome delivery hurdles of peptidomimetic drugs and enhance their bioavailability in the retina
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