Development of cisplatin as an anti-cancer drug

Pangarkar, Kasturi (2025) Development of cisplatin as an anti-cancer drug. GSC Advanced Research and Reviews, 23 (1). 005-011. ISSN 2582-4597

Cisplatin, a platinum-based chemotherapeutic agent, has been a cornerstone in the treatment of various cancers since its FDA approval in 1978. It is particularly effective against cancers such as ovarian, colorectal, prostate, bladder, and non-small cell lung cancer (NSCLC). Cisplatin exerts its anticancer effects by forming platinum-DNA adducts that inhibit DNA replication and transcription, leading to cell cycle arrest and apoptosis. However, its clinical application is limited by severe side effects, including renal toxicity, nausea, vomiting, and the development of drug resistance. To mitigate these challenges, there has been increasing interest in encapsulating cisplatin in nanocarriers, particularly liposomes. Liposomal formulations, such as Lipoplatin™, enhance cisplatin’s accumulation in tumors through the enhanced permeability and retention (EPR) effect while reducing toxicity to healthy tissues. Further innovations, including cisplatin encapsulated in PLGA-coated liposomes and co-encapsulation with other therapeutic agents, have shown promise in improving drug release profiles and therapeutic efficacy. This review examines the molecular mechanisms of cisplatin action, its therapeutic challenges, and advancements in its nanostructured formulations. Emphasis is placed on liposomal delivery systems, which offer significant potential to improve cisplatin’s effectiveness, reduce systemic toxicity, and overcome resistance, paving the way for more efficient and targeted cancer treatments.