Diabetic foot ulcers are the most common lower extremity complications of diabetes. Peripheral neuropathy and peripheral vascular disease are the underlying risk factors for diabetic foot ulcers, subsequently leading to infections and requiring antimicrobial therapy for the management of the disease. Each risk factor is a target for clinical intervention, with the intent to delay or prevent disease progression to amputation. The effective therapy includes interdisciplinary care, which involves optimized pharmacological interventions in concert with other treatments such as debridement strategies and specialized wound dressings. The pharmacological therapy alone cannot lead to successful therapy, and therefore, these supplementary techniques/modalities should not be overlooked. It is therefore the aim of this report to review various pharmacological interventions, specific to the diabetic foot and wound healing, along with incorporation of advanced therapies required to achieve a multifaceted treatment of diabetic foot ulcers and provide basis for superior drugs as well as drug delivery systems.