Polymeric micelle containing cisplatin enclosed therein and use thereof
AssigneeToudai TLO, Ltd.
InventorsKazunori Kataoka, Nobuhiro Nishiyama, Masayuki Yokoyama, Teruo Okano
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Abstract
A complex comprising cisplatin and a poly(ethylene glycol)/poly(glutamic acid) block copolymer, wherein the cisplatin is enclosed in the copolymer through ligand displacement in which a carboxyl anion of the copolymer is replaced with a chlorine ion of the cisplatin. This complex can give a medicine reduced in toxicity and usable by a new method of administration.
Claims12
A complex which originates in a block copolymer represented by Formula I or II:
- 5
- (in Formula I and II described above, R1 represents independently a hydrogen atom or an alkyl group which may be substituted with a functional group;
- A represents independently NH, CO or R5(CH2)pR6, in which R5 is O, OCO, OCONH, NHCO, NHCOO, NHCONH, CONH or COO;
- R6 is NH or CO;
- and p is an integer of 1 to 6;
- R2 represents independently a hydrogen atom or an alkyl group or an aralkyl group;
- R3 represents independently a hydrogen atom or a hydrophobic residue;
- m is independently an integer of 50 to 5000;
- and n is independently an integer of 5 to 500) and cisplatin and in which an equivalent ratio (Pt/COO−) of Pt in cisplatin to a carboxyl anion of the above copolymer is 0.3 or more.
A medicinal preparation comprising a medicinally effective amount of a complex which originates in a block copolymer represented by Formula I or II:
- 7
- (in Formula I and II described above, R1 represents independently a hydrogen atom or an alkyl group which may be substituted with a functional group;
- A represents independently NH, CO or R5(CH2)pR6, in which R5 is O, OCO, OCONH, NHCO, NHCOO, NHCONH, CONH or COO;
- R6 is NH or CO;
- and p is an integer of 1 to 6;
- R2 represents independently a hydrogen atom or an alkyl group or an aralkyl group;
- R3 represents independently a hydrogen atom or a hydrophobic residue;
- m is independently an integer of 50 to 5000;
- and n is independently an integer of 5 to 500) and cisplatin and in which an equivalent ratio (Pt/COO−) of Pt in cisplatin to a carboxyl anion of the above copolymer is 0.3 or more, a filler or a diluent.
Dependencies are inferred from the claim text.