Diabetic retinopathy (DR) is a significant complication of diabetes, leading to blindness worldwide. Current treatments, including anti-VEGF drugs, steroids, laser photocoagulation, and vitrectomy, have limitations and adverse effects. This review summarizes the current pathophysiology, therapeutic approaches, and drug-delivery methods for treating DR. Recent research highlights the efficacy of novel receptor inhibitors and agonists, such as aldose reductase inhibitors, angiotensin-converting enzyme inhibitors, and peroxisome proliferator-activated receptor alpha agonists. Nanotechnology has also developed new drug delivery systems that address the limitations of traditional treatments, such as low solubility and poor penetration. The review emphasizes the need for continuous exploration to enhance our understanding of DR pathogenesis and improve treatment options.Diabetic retinopathy (DR) is a significant complication of diabetes, leading to blindness worldwide. Current treatments, including anti-VEGF drugs, steroids, laser photocoagulation, and vitrectomy, have limitations and adverse effects. This review summarizes the current pathophysiology, therapeutic approaches, and drug-delivery methods for treating DR. Recent research highlights the efficacy of novel receptor inhibitors and agonists, such as aldose reductase inhibitors, angiotensin-converting enzyme inhibitors, and peroxisome proliferator-activated receptor alpha agonists. Nanotechnology has also developed new drug delivery systems that address the limitations of traditional treatments, such as low solubility and poor penetration. The review emphasizes the need for continuous exploration to enhance our understanding of DR pathogenesis and improve treatment options.