title: Reversibly PEGylated nanocarrier for cisplatin delivery.
abstract: A star-shaped copolymer bearing a shell of poly(ethylene glycol) (PEG) chains was designed as a carrier of cisplatin. The proposed strategy was based on synthesis of a PEGylating agent and the incorporation of cisplatin as a reversible linker for PEG modification of the star macromolecules. The attachment of PEG chains to the stars and their release under physiological conditions, as well as the changes in particle size and mobility upon drug loading, was evidenced by diffusion ordered NMR spectroscopy (DOSY). The results demonstrated that PEGylation reduced inter-stars cross-linking and increased the stability of the nanocolloidal solution. The formation of PEG shell resulted in higher drug payload and improved drug release profile of the nanoconjugates. The in vitro bioassay in a panel of human tumor cell lines confirmed that the PEGylated conjugates exhibited superior growth inhibitory activity compared to the cisplatin-loaded nonPEGylated carrier.
authors: Institute of Polymers, Bulgarian Academy of Sciences, Acad. Georgi Bonchev Str. Bl.103, 1113 Sofia, Bulgaria. ajfa_jest@abv.bg
authors: Ekaterina
authors: E
authors: Stoyanova
authors: Violeta
authors: V
authors: Mitova
authors: Pavletta
authors: P
authors: Shestakova
authors: Agnieszka
authors: A
authors: Kowalczuk
authors: Georgi
authors: G
authors: Momekov
authors: Denitsa
authors: D
authors: Momekova
authors: Andrzej
authors: A
authors: Marcinkowski
authors: Neli
authors: N
authors: Koseva
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor / Q000187:drug effects; D002945:Cisplatin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000737:chemistry* / Q000494:pharmacology*; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D009682:Magnetic Resonance Spectroscopy; D018625:Microscopy, Atomic Force; D058726:Nanoconjugates / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D058726:Nanoconjugates; D011092:Polyethylene Glycols; D002945:Cisplatin