Zovko Marijana, Barbarić Monika, Zorc Branka, Hafner Anita, Filipović-Grcić Jelena
Faculty of Pharmacy and Biochemistry, University of Zagreb, Zagreb, Croatia.
Acta Pharm. 2005 Jun;55(2):169-76.
Two types of polymer-drug conjugates were synthesized starting from styrene-maleic acid anhydride copolymer (SMA). Fenoprofen and gemfibrozil were chosen as model drugs because of their short plasma half lives. Both drugs were first converted to their 2-aminoethylamides, which possess free amino groups capable of reacting with SMA anhydride rings. By modifying the degree and type of substitution, lipophilic and hydrophilic conjugates were obtained. Drug loading in the conjugates was between 17 and 47%.
从苯乙烯-马来酸酐共聚物（SMA）出发合成了两种类型的聚合物-药物偶联物。由于非诺洛芬和吉非贝齐的血浆半衰期较短，因此选择它们作为模型药物。两种药物首先都被转化为它们的2-氨基乙酰胺，这些2-氨基乙酰胺具有能够与SMA酸酐环反应的游离氨基。通过改变取代度和取代类型，获得了亲脂性和亲水性偶联物。偶联物中的药物负载量在17%至47%之间。
