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1、J.POLYMERSCI.:SymposiumNo.51,135-153(1975)STRUCTUREANDPROPERTIESOFPHARMACOLOGICALLYACTIVEPOLYMERSHELMUTRINGSDORFInstituteofOrganicChemistry,UniversityofMainz,65Mainz,J.-J.-Becher-Weg,GermanySYNOPSISAlthoughtheconceptofusingpharmacologicallyactivemacromo

2、lecularcom-poundsasdrugsisstillregardedwithmuchskepticismforboththeoreticalandpracticalreasons,interestinthisfieldhasgrowninrecentyearsbecauseoftheopportunitytotakeadvantageofthespecificpropertiesofpolymericmaterials.Forlowmolecularweightdrugs,changesin

3、structureoftenleadtoalossofspecificactivity.Ontheotherhand,thepropertiesofmacromoleculardrugsdependonthestructureofthepolymerusedandthiscanbevariedoverawiderangebythein-corporationofcomonomerunits,bytheapplicationofpolymer-analogousreactions,orbyrelated

4、structuralchanges.Anewmodelispresentedforpharmacologicallyactivepolymerswhichincorporatesthepossibilityforcontinuousvariationin(a)solubilityandtoxicity,(b)fixationandremovalofactivematerial,and(c)bodydistribution.Usingthenewmodelasaguide,examplesofthesy

5、nthesisandstudyofthebiologicalactivityofvariousmacromoleculardrugsarepresentedinordertoemphasizetheimportanceofthiscooperativeeffortbetweenpolymerresearchandtherapeuticproblems.INTRODUCTIONTheinvestigationofbiomaterialsisoneofthenewestandmostexcit-ingar

6、easofpolymerchemistry.Especiallyinterestingareinvestigationsofpharmacologicallyactivepolymersrepresentingmacromoleculeswhichbythemselvesmaybeactiveasdrugsoralternativelymaybeusedascarriersfornormalpharmaceuticalagents.Althoughpolymersarealreadywidelyuse

7、dintheareaofbiomedicalengineering,e.g.,toconstructartificialreplacementsforhumanorgans[11ortoprovidebiochemicalfunctions[2],thefieldofpolymericdrugsisstillsubjecttoconsiderableskepticism.Morepointshavebeenraisedagainsttheuseofpharmacologicallyactivepoly

8、mersthanintheirfavor.Neverthe-less,muchhasbeenaccomplishedinrecentyearsasshownbythegrowingnumberofpapersandreviewsarticlesinthisarea[3-71.Originally,oneofthemainideasbehindthepossibleuseofpharma-cologicallyactivepolymerswasthehop