Diabetic retinopathy (DR) is a serious complication of diabetes that affects nearly 103.12 million people worldwide. It is a leading cause of irreversible blindness in people over 50 years old. DR is characterized by neurodegeneration, inflammation, and oxidative stress. Current treatments, including anti-VEGF drugs, steroids, laser photocoagulation, and vitrectomy, have limitations and adverse effects, necessitating the exploration of novel treatment strategies. This review summarizes the current pathophysiology, therapeutic approaches, and drug-delivery methods for treating DR, and discusses their development potential. Recent research indicates the efficacy of novel receptor inhibitors and agonists, such as aldose reductase inhibitors, angiotensin-converting enzyme inhibitors, and peroxisome proliferator-activated receptor alpha agonists, in delaying DR. Advances in nanotechnology have led to new drug delivery systems that can address limitations of clinical drug therapy, such as low solubility and poor penetration. This review serves as a theoretical foundation for future research on DR treatment. While highlighting promising therapeutic targets, it underscores the need for continuous exploration to enhance understanding of DR pathogenesis. The limitations of current treatments and the potential for future advancements emphasize the importance of ongoing research in this field. Laser photocoagulation is widely used to prevent the progression from severe NPDR to PDR. However, it has side effects such as retinal scars and macular edema. Newer laser treatments, such as pattern-scanning lasers, are less destructive and reduce treatment time and patient discomfort. Surgical treatments, such as vitrectomy, are used for advanced DR with intravitreal hemorrhage and retinal detachment. These procedures aim to clear vitreous body, remove fibrovascular membranes, and inhibit vitreoretinal proliferation. Anti-VEGF drugs, such as bevacizumab, ranibizumab, and aflibercept, are effective in reducing retinal neovascularization and vitreous hemorrhage. Steroid drugs, such as triamcinolone acetonide, are used to reduce inflammation and VEGF expression. Senolytic drugs eliminate senescent cells, which may help in treating DR. Retinal ganglion cell injury and regeneration-related drugs, such as epigallocatechin-3-gallate and curcumin, have neuroprotective effects. Other drugs, such as fenofibrate and SGLT2 inhibitors, may help in preventing and treating DR. Gene therapy and nanotechnology are promising new approaches for DR treatment. Despite these advancements, challenges remain in the development of safe and effective treatments for DR.Diabetic retinopathy (DR) is a serious complication of diabetes that affects nearly 103.12 million people worldwide. It is a leading cause of irreversible blindness in people over 50 years old. DR is characterized by neurodegeneration, inflammation, and oxidative stress. Current treatments, including anti-VEGF drugs, steroids, laser photocoagulation, and vitrectomy, have limitations and adverse effects, necessitating the exploration of novel treatment strategies. This review summarizes the current pathophysiology, therapeutic approaches, and drug-delivery methods for treating DR, and discusses their development potential. Recent research indicates the efficacy of novel receptor inhibitors and agonists, such as aldose reductase inhibitors, angiotensin-converting enzyme inhibitors, and peroxisome proliferator-activated receptor alpha agonists, in delaying DR. Advances in nanotechnology have led to new drug delivery systems that can address limitations of clinical drug therapy, such as low solubility and poor penetration. This review serves as a theoretical foundation for future research on DR treatment. While highlighting promising therapeutic targets, it underscores the need for continuous exploration to enhance understanding of DR pathogenesis. The limitations of current treatments and the potential for future advancements emphasize the importance of ongoing research in this field. Laser photocoagulation is widely used to prevent the progression from severe NPDR to PDR. However, it has side effects such as retinal scars and macular edema. Newer laser treatments, such as pattern-scanning lasers, are less destructive and reduce treatment time and patient discomfort. Surgical treatments, such as vitrectomy, are used for advanced DR with intravitreal hemorrhage and retinal detachment. These procedures aim to clear vitreous body, remove fibrovascular membranes, and inhibit vitreoretinal proliferation. Anti-VEGF drugs, such as bevacizumab, ranibizumab, and aflibercept, are effective in reducing retinal neovascularization and vitreous hemorrhage. Steroid drugs, such as triamcinolone acetonide, are used to reduce inflammation and VEGF expression. Senolytic drugs eliminate senescent cells, which may help in treating DR. Retinal ganglion cell injury and regeneration-related drugs, such as epigallocatechin-3-gallate and curcumin, have neuroprotective effects. Other drugs, such as fenofibrate and SGLT2 inhibitors, may help in preventing and treating DR. Gene therapy and nanotechnology are promising new approaches for DR treatment. Despite these advancements, challenges remain in the development of safe and effective treatments for DR.