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Ketamine, originally developed as an anesthetic, has shown significant potential for treating depression, chronic pain, and other conditions. However, its conventional formulations often result in side effects such as hallucinations and dizziness due to rapid spikes in blood concentration. This article explores recent patents that optimize ketamine delivery and efficacy: subcutaneous injectable compositions, ketamine conjugates with various molecules, and dual-release formulations combining ketamine with aspirin. These innovations promise to improve ketamine-based treatments’ pharmacokinetic profiles, therapeutic outcomes, and safety.