Cisplatin liposome formulation

Preparations of liposomes via SCF processing are designated as critical fluid liposomes (CFLs). CFLs have successfully encapsulated hydrophobic drugs such as taxoids, camptothecins, doxorubicin, vincristine, and cisplatin. In addition, stable paclitaxel liposomes with a size of 150-250 nm were obtained. Aphios Co. s patent (US Patent 5,776,486) on Super-Fluids CFL describes a method that is useful for the nanoencapsulation of paclitaxel and campothecin in aqueous liposomal formulations called Taxosomes and Camposomes , respectively. 

Nedaplatin has been registered in Japan, whereas other derivatives, like satraplatin (JM216, which is the only orally available platinum derivative), ZD0473, BBR3464, and SPI-77 (a liposomal formulation of cisplatin), are still under investigation (10-13). 

Zamboni, W. C., Gervais, A. C., Egorin, M. J., Schellens, J. H., Zuhowski, E. G., Pluim, D., et al. (2004), Systemic and tumor disposition of platinum after administration of cisplatin or STEALTH liposomal-cisplatin formulations (SPI-077 and SPI-077 B103) in a preclinical tumor model of melanoma, Cancer Chemother. Pharmacol., 53, 329-336. 

Lipoplatin (Regulon Inc. Mountain View, CA, USA) is another pegylated liposomal cisplatin formulation composed of showed plasma half-life is 60-117 h in clinical study, depeuding on the dose (Boulikas et al. 2005 Stathopoulos et al. 2005). The study also found that Lipoplatin has no nephrotoxicity up to a dose of 125 mg/m every 14 days without the serious side effects of cisplatin. Clinical evaluation of pegylated liposomal... 

These are also die major frictors involved in acquired resistance to cisplatin (7,8). Hie genoal phaimacokinetic principle is diat free unbound drug is the active principle, allowing distribution to tissue. Thus an important parameter in general is tissue availability - stability in plasma and protein binding may be manipulated by qiprtqiriate formuladon and liposomes and other mediods of formulation have n used (3). 

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