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Introduction: Rasashastra and Bhaishajya Kalpana (RSBK), integral branches of Ayurveda, emphasize the use of herbo-mineral formulations through precise pharmaceutical techniques like shodhana (purification) and marana (calcination). Their safety, efficacy, and unique pharmaceutics align remarkably with modern pharmaceutical sciences. Despite concerns about heavy metals, evidence suggests that traditional methods render formulations safe and effective. Methods: A comprehensive literature review was conducted through PubMed, Scopus, Web of Science, AYUSH Research Portal, and classical Ayurvedic texts. Articles from 2000–2023, including clinical, experimental, and review studies, were included, focusing on safety, efficacy, nanomedicine parallels, and integrative applications of RSBK. Exclusion criteria involved anecdotal reports and poorly documented studies. Results: RSBK formulations demonstrated therapeutic benefits across chronic diseases, metabolic syndromes, and immune disorders. Bhasmas were shown to possess nanoparticle dimensions, explaining their bioavailability and pharmacological effects. Comparative studies revealed synergy between herbo-mineral combinations and modern drugs. However, gaps remain in standardization, toxicological profiling, and global regulatory acceptance. Discussion: RSBK principles share parallels with modern pharmaceutics, particularly in detoxification, stability, and drug delivery. Evidence supports their potential role in integrative medicine by complementing allopathic treatments. Regulatory concerns, lack of pharmacovigilance, and insufficient clinical trials limit global acceptance. Conclusion: With robust validation, GMP adherence, and interdisciplinary collaboration, RSBK can significantly contribute to integrative medicine and modern pharmaceutics, offering safe, effective, and holistic therapeutic options.

KEYWORDS: Ayurveda, Bhaishajya Kalpana, Integrative medicine, Modern pharmaceutics, Rasashastra