FIELD: nanotechnology; anticancer drugs.
SUBSTANCE: invention relates to a method for producing a lipid-conjugated platinum compound. The method includes the following: reacting a water-soluble lipid salt with a water-soluble platinum compound in a substantially aqueous solution to produce a lipid-conjugated platinum compound as a precipitate, wherein the water-soluble lipid salt contains a compound of formula II, where X is NH or N-CH2COO-, X1 is selected from the group consisting of -(CH2)nO-, -(CH2)nNHCOO-, -(CH2)nCONH(CH2)nO-, -(CH2)nO(CH2)nO-, -(CH2)nC(O)-, -(CH2)nNHCO(CH2)nO- and -(CH2)nCOO-, n is 0–2. Preparation of the water-soluble lipid salt of formula II consists of: a. covalent connection of the linker with the lipid of formula II; and b. reaction of a linker covalently attached to a lipid with a base, which is LiOH, NaOH, KOH, RbOH, CsOH, Mg(OH)2, Ca(OH)2, Sr(OH)2, Ba(OH)2, with an acid, such as trifluoroacetic acid (TFA), or any combination thereof. A method for producing nanoparticles and compositions for use in chemotherapy are also proposed.
EFFECT: proposed method provides >50% yield and >70% purity for the lipid-conjugated platinum compound.
44 cl, 30 dwg, 22 tbl, 13 ex
Lipid(Formula II)
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Authors
Dates
2023-05-02—Published
2016-05-18—Filed