title: Star-shaped drug carriers for doxorubicin with POEGMA and POEtOxMA brush-like shells: a structural, physical, and biological comparison.
abstract: The synthesis of amphiphilic star-shaped poly(ε-caprolactone)-block-poly(oligo(ethylene glycol)methacrylate)s ([PCL(18)-b-POEGMA](4)) and poly(ε-caprolactone)-block-poly(oligo(2-ethyl-2-oxazoline)methacrylate)s ([PCL(18)-b-POEtOxMA](4)) is presented. Unimolecular behavior in aqueous systems is observed with the tendency to form loose aggregates for both hydrophilic shell types. The comparison of OEGMA and OEtOxMA reveals that the molar mass of the macromonomer in the hydrophilic shell rather than the mere length is the crucial factor to form an efficiently stabilizing hydrophilic shell. A hydrophilic/lipophilic balance of 0.8 is shown to stabilize unimolecular micelles in water. An extensive in vitro biological evaluation shows neither blood nor cytotoxicity. The applicability of the polymers as drug delivery systems was proven by the encapsulation of the anticancer drug doxorubicin, whose cytotoxic effect was retarded in comparison to the free drug.
authors.affiliation: Laboratory of Organic and Macromolecular Chemistry, Friedrich Schiller University Jena, Germany.
authors.forename: Katrin
authors.initials: K
authors.lastname: Knop
authors.forename: David
authors.initials: D
authors.lastname: Pretzel
authors.forename: Annett
authors.initials: A
authors.lastname: Urbanek
authors.forename: Tobias
authors.initials: T
authors.lastname: Rudolph
authors.forename: Daniel H
authors.initials: DH
authors.lastname: Scharf
authors.forename: Anja
authors.initials: A
authors.lastname: Schallon
authors.forename: Michael
authors.initials: M
authors.lastname: Wagner
authors.forename: Stephanie
authors.initials: S
authors.lastname: Schubert
authors.forename: Michael
authors.initials: M
authors.lastname: Kiehntopf
authors.forename: Axel A
authors.initials: AA
authors.lastname: Brakhage
authors.forename: Felix H
authors.initials: FH
authors.lastname: Schacher
authors.forename: Ulrich S
authors.initials: US
authors.lastname: Schubert
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004317:Doxorubicin / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004337:Drug Carriers; D004339:Drug Compounding; D004912:Erythrocytes / Q000187:drug effects; D006461:Hemolysis; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D061986:MCF-7 Cells; D008422:Materials Testing; D008968:Molecular Conformation; D053769:Nanocapsules / Q000737:chemistry; D010080:Oxazoles / Q000138:chemical synthesis; D010316:Particle Size; D015539:Platelet Activation / Q000187:drug effects; D011091:Polyesters / Q000737:chemistry; D011092:Polyethylene Glycols / Q000138:chemical synthesis*; D011109:Polymethacrylic Acids / Q000138:chemical synthesis*; D012996:Solutions; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D053769:Nanocapsules; D010080:Oxazoles; D011091:Polyesters; D011109:Polymethacrylic Acids; D012996:Solutions; D013501:Surface-Active Agents; C016240:polycaprolactone; D011092:Polyethylene Glycols; D004317:Doxorubicin