Development of a parenterally administrable hydrosol preparation of the "third generation platinum complex" [(+/-)-1,2-bis(4-fluorophenyl)ethylenediamine]dichloroplatinum(II). Part 1. Preparation and studies on the stability and antitumor activity.
The development of a galenical formulation for poorly water soluble dichloroplatinum(II) complexes suitable for the parenteral administration in cancer chemotherapy is described. The procedure, which we elaborated for [(+/-)-1,2-bis(4-fluorophenyl)ethylenediamine]dichloroplatinum(II) (rac-4F-PtCl2), is based on the reaction of a soluble diaquaplatinum(II) salt with sodium chloride in water in the presence of pluronic F 68 as stabilizer and results in a sufficiently stable colloidal solution (i.e. hydrosol). In contrast to the poorly water soluble synthetic rac-4F-PtCl2, which was ineffective towards the hormone sensitive MXT-M-3.2 breast cancer of the mouse, its hydrosol formulation proved to be highly active and was very well tolerated.
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000302:isolation & purification* / Q000494:pharmacology; D004355:Drug Stability; D005260:Female; D006801:Humans; D007263:Infusions, Parenteral; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy; D051379:Mice; D009944:Organoplatinum Compounds / Q000008:administration & dosage / Q000302:isolation & purification* / Q000494:pharmacology; D012995:Solubility; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C064244:(1,2-bis(4-fluorophenyl)ethylenediamine)dichloroplatinum(II)