Delivery and activation through liposome incorporation of diaminocyclohexane platinum (II) complexes
AssigneeBoard of Regents, The University of Texas System
InventorsRoman Perez-Soler, Abdul R. Khokhar
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Abstract
Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having the formula ##STR1## where R.sub.1 is diaminocycloalkyl, and R.sub.2 and R.sub.3 each have the formula ##STR2## where R.sub.4, R.sub.5, and R.sub.6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, into a complex having the formula R.sub.1 --Pt--X.sub.2 where X is halogen.
Claims9
A method of delivering a biologically active chemical moiety internally to a mammal, comprising:
- providing an aqueous formulation of a first compound having the formula ##STR5## where R.sub.1 is diaminocycloalkyl and R.sub.2 and R.sub.3 independently have the formula ##STR6## where R.sub.4, R.sub.5, and R.sub.6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, the first compound being entrapped in a liposome, the first compound further being capable of forming a second compound which is biologically active upon exposure to a solution having an acidic pH;
- reducing the pH of the aqueous formulation to an acidic level, thereby converting the first compound to a second compound having the formula
- R.sub.1 --Pt--X.sub.2
- where R.sub.1 is as defined above and X is halogen;
- and
- administering the aqueous formulation to a mammal.
A method of delivering a biologically active chemical moiety internally to a mammal, comprising:
- providing an aqueous formulation of a first compound having the formula ##STR7## where R.sub.1 is 1,2-diaminocycloalkyl and R.sub.2 and R.sub.3 independently have the formula ##STR8## where R.sub.4, R.sub.5, and R.sub.6 are each independently alkyl having from 1 to about 3 carbon atoms, the first compound being entrapped in a liposome, the first compound further being capable of forming a second compound which is biologically active upon exposure to a solution having an acidic pH;
- reducing the pH of the aqueous formulation to an acidic level, thereby converting the first compound to a second compound having the formula
- R.sub.1 --Pt--X.sub.2
- where R.sub.1 is as defined above and X is halogen;
- and
- administering the aqueous formulation to a mammal.
Dependencies are inferred from the claim text.