Self-assembling water-soluble polymethacrylate-MTX conjugates: The significance of macromolecules architecture on drug conjugation efficiency, the final shape of particles, and drug release.

Self-assembling water-soluble polymethacrylate-MTX conjugates: The significance of macromolecules architecture on drug conjugation efficiency, the final shape of particles, and drug release. J Biomed Mater Res B Appl Biomater. 2019 Feb 18;: Authors: Bernaczek K, Mielańczyk A, Mielańczyk Ł, Neugebauer D, Grzywna ZJ Abstract Water-soluble polymer-methotrexate (MTX) conjugates were obtained via efficient carbodiimide-mediated amidation (E = 17-100%). Binding abilities between water-soluble V-shaped or star-shaped copolymers and MTX were studied by isothermal titration calorimetry spectroscopic (UV-vis, NMR) and microscopic (scanning electron microscopy and transmission electron microscopy) techniques. The efficiency of the amidation reaction has depended on the amount of pendant amino alcohol groups and zeta potential (ZP) values of polymeric carries. The sizes of aggregates formed by polymer-drug conjugates in water increased with the number of copolymer arms (202-774 nm at 37°C). Moreover, the conjugates with the high amount of bounded MTX molecules (nMTX  > 78) exhibited negative ZP values. The drug release experiments revealed that the amount of the released MTX depends on pH and can be controlled via shape, topology, and composition of polymeric carrier. Preliminary cytotoxicity studies of V-shaped-MTX conjugate on human immortalized nontumorigenic keratinocyte (HaCaT) cells indicated cytocompatibility of the compo...
Source: Biomed Res - Category: Research Authors: Tags: J Biomed Mater Res B Appl Biomater Source Type: research