Abstract
Therapeutic proteins and peptides have become notable in the drug delivery arena for their compatibility with the human body as well as their high potency. However, their biocompatibility and high potency does not negate the existence of challenges resulting from physicochemical properties of proteins and peptides, including large size, short half-life, capability to provoke immune responses and susceptibility to degradation. Various delivery routes and delivery systems have been utilized to improve bioavailability, patient acceptability and reduce biodegradation. The ocular route remains of great interest, particularly for responsive delivery of macromolecules due to the anatomy and physiology of the eye that makes it a sensitive and complex environment. Research in this field is slowly gaining attention as this could be the breakthrough in ocular drug delivery of macromolecules. This work reviews stimuli-responsive polymeric delivery systems, their use in the delivery of therapeutic proteins and peptides as well as examples of proteins and peptides used in the treatment of ocular disorders. Stimuli reviewed include pH, temperature, enzymes, light, ultrasound and magnetic field. In addition, it discusses the current progress in responsive ocular drug delivery. Furthermore, it explores future prospects in the use of stimuli-responsive polymers for ocular delivery of proteins and peptides. Stimuli-responsive polymers offer great potential in improving the delivery of ocular therapeutics, therefore there is a need to consider them in order to guarantee a local, sustained and ideal delivery of ocular proteins and peptides, evading tissue invasion and systemic side-effects.
Highlights
Therapeutic proteins and peptides are advantageous over small molecule drugs in that they mimic similar molecules found in the human body; they are biocompatible and highly potent.limitations do exist, caused by their high molecular weight, poor transfer across biological membranes, provocation of immune responses, short half-lives and instability of the molecules [1,2]
Much attention is drawn to the ocular route for the reason that this review focuses on the future prospects in responsive ocular delivery of macromolecules
The ocular route is potentially useful for systemic delivery of therapeutic proteins and peptides; it is often used for localized delivery of ophthalmic agents
Summary
Therapeutic proteins and peptides are advantageous over small molecule drugs in that they mimic similar molecules found in the human body; they are biocompatible and highly potent. The ocular route is potentially useful for systemic delivery of therapeutic proteins and peptides; it is often used for localized delivery of ophthalmic agents It is the most interesting and challenging route in drug delivery due to the sensitive and complex environment of the eye [5]. Biocompatibility, contaminant/pyrogen-free, non-toxic, low cost, high loading capacity and an excellent stability profile The use of these polymers provides a less invasive delivery approach via externally controlled stimuli and extended stability in the body owing to their stimuli specificity and site-specific release [14]. The rationale for these systems arises from a number of formulation shortcomings which will be discussed in detail below [16,17]
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