Nanoparticle formulations of platinum compounds

Drug – bio-affecting and body treating compositions – Inorganic active ingredient containing – Heavy metal or compound thereof

Reexamination Certificate

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C556S137000, C514S492000, C977S717000, C977S911000

Reexamination Certificate

active

07611733

ABSTRACT:
Solid Lipid Nanoparticles of platinum compounds, particularly of antitumor platinum complexes are disclosed. The Nanoparticles of the invention are obtained by a process comprising: a) preparing a first microemulsion by mixing a molten lipid, a surfactant, and optionally a co-surfactant and the platinum compound acqueous solution; b) preparing a solution by mixing a surfactant and optionally a co-surfactant in water, heating to complete solution, preferably at the same melting temperature of the lipid used in a) and adding a co-surfactant; c) dispersing the microemulsion obtained in a) into the solution obtained in b) obtaining a multiple microemulsion c); d) dispersing the microemulsion obtained in c) in aqueous medium at a temperature ranging from 0.5° C. to 4° C. obtaining a dispersion of solid lipid microspheres; e) washing with aqueous medium through ultrafiltration the obtained lipid microspheres obtained in d) and lyophilizing, optionally in the presence of a bulking agent and of a cryoprotecting agent.

REFERENCES:
patent: 5250236 (1993-10-01), Gasco
patent: 6011166 (2000-01-01), Valsecchi et al.
patent: 6287593 (2001-09-01), Cherian
patent: 6596889 (2003-07-01), Menta et al.
patent: WO-94/20072 (1994-09-01), None
patent: WO-93/05768 (1996-04-01), None
Egea et al., “Penetration kinetics of cis-diamminedichloroplatinum(II) loaded nanoparticles in lipid monolayers as a membrane model of the reticuloendothelial system”, Thin Solid Films, vol. 210/211, pp. 364-367, 1992.

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