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Hiroshi Maeda

Khaled Greish

The present invention provides a polymeric agent which can incorporate a large amount of a drug, accumulate selectively in a tumor site, and has a molecular size of more than that for renal excretion. A metalloporphyrin derivative (such as zinc protoporphyrin) is associated with a styrene-maleic acid copolymer via non-covalent bond to give a SMA micelle complex, allowing provision of a polymeric pharmaceutical agent for treatment of cancer with a large amount of the drug incorporated. The SMA micelle complex can be produced by a method, wherein the metalloporphyrin derivative reacts with the styrene-maleic acid copolymer in the absence of a condensation agent under an alkaline condition, solubilized, adjusted to have a pH of 6-8, and subjected to a procedure for separating a polymer component to recover the micelle complex component for the polymeric pharmaceutical agent.

Polymeric pharmaceutical agent for treatment of cancer and method for production of the same

The present invention relates to polymeric antitumor agent which is formed in polymeric micelle complex by intermolecular bonding or mutual interaction between styrene maleic acid copolymer (SMA) and low molecule antitumor agent which is anthracyclins drug such as pirarubicin, doxorubicm, epirbicin, daunorbicin, acralbicin, or alkaloid antitumor agent such as cis-platinum, and taxol These polymeric antitumor agents may improve specificity to cancer cells so that it improves antitumor effect, while it may not be concentrated at normal organ or tissue, so that adverse effect may be diminished. These polymeric antitumor agents may be prepared by dissolving SMA and low molecule antitumor agent in aqueous solution, then in the presence of aqueous soluble carbodiimide, amino acids, or polyamine, adjusting pH to form micelle complex and recovering polymer fraction.

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Kumamoto, Japan

Khaled Greish