Background: Diabetic retinopathy (DR) is one of the major complications of diabetes,
and the consequences often lead to loss of vision. Currently, the treatments for DR are expensive,
not easily available and the use of synthetic drugs leads to various toxic effects. Bioactive compound
has been reported to be an alternative for the treatment of DR due to its ability to target multiple
pathophysiological signaling pathways. However, bioactive compound suffers from some inherent
physicochemical characteristics which restrict their use as therapeutic agents.
Objective: This review emphasizes an overview of the bioactive agents which are delivered as
nano-formulation for safe and effective ocular delivery for the treatment of DR. Additional focus
include site-specific ocular delivery with increased bioavailability to ensure highly efficacious treatment
Results: Utilization of various bioactive compounds such as polyphenols, flavonoids, tannins, etc.,
can counterbalance the damages that occur in the retinal tissues and thereby may ameliorate DR
progression. Encapsulation of these bioactive compounds in a nanotechnology-based delivery system
can improve bioavailability, reduce the toxic effect and achieve site-specific ocular delivery.
Conclusion: The pros and cons of bioactive compounds in treating DR and the use of nanotechnology
to deliver bioactive compounds are discussed.