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Lipoplatin is a liposomal formulation of the conventional chemotherapeutic agent cisplatin, designed to reduce systemic toxicity and enhance tumor-specific delivery. Developed by Regulon Inc., it consists of cisplatin encapsulated within long-lasting liposomes (approximately 110 nm in diameter) composed of lipids such as dipalmitoyl phosphatidylcholine (DPPC) and soy phosphatidylcholine. The mechanism of action involves the extravasation of liposomes through the leaky vasculature of tumors (the enhanced permeability and retention or EPR effect), followed by the release of cisplatin into the tumor microenvironment and uptake by cancer cells. Once inside, cisplatin forms DNA adducts, primarily intrastrand cross-links, which inhibit DNA replication and transcription, ultimately leading to apoptosis. Lipoplatin has demonstrated reduced nephrotoxicity, neurotoxicity, and ototoxicity compared to conventional cisplatin in clinical trials, particularly in non-small cell lung cancer (NSCLC).
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