Poly((N-vinylpyrrolidone)-block-poly(vinyl acetate)) (PVP-b-PVAc) block copolymers of varying molecular weight and hydrophobic block lengths were synthesized via controlled radical polymerization and investigated as carriers for the solubilization of highly hydrophobic riminophenazine compounds. These compounds have recently been shown to exhibit a strong activity against a variety of cancer types. PVP-b-PVAc self-assembles into polymer vesicles in aqueous media, and the dialysis method was used to load the water-insoluble drug (clofazimine) into these polymer vesicles. The polymer vesicles were characterized by 1H NMR spectroscopy to confirm vesicle formation and the incorporation of the anticancer drugs into the polymer vesicles. Dynamic light scattering was used to determine the particle size and particle size distribution of the drug-loaded vesicles as well as the stability of the vesicles under physiological conditions. The size of the polymer vesicles did not increase upon loading with clofazimine, and the particle size of 180-200 nm and the narrow particle size distribution were maintained. The morphology of the vesicles was examined by transmission electron microscopy. The polymer vesicles had a relatively high drug loading capacity of 20 wt %. In vitro cytotoxicity studies of PVP-b-PVAc and drug-loaded PVP-b-PVAc were performed against MDA-MB-231 multidrug-resistant breast epithelial cancer cells and MCF12A nontumorigenic breast epithelial cells. In vitro experiments demonstrated that the PVP-b-PVAc drug carrier showed no cytotoxicity, which confirms the biocompatibility of the PVP-b-PVAc drug carrier. The results indicate that the present PVP-b-PVAc block copolymer could be a potential candidate as a drug carrier for hydrophobic drugs.
Poly(N-vinylpyrrolidone)-block-poly(vinyl acetate) (PVP-b-PVAc) block copolymers of varying molar mass and hydrophobic block lengths were synthesized by xanthate-mediated radical polymerization. In order to control the molar mass of the hydrophilic PVP block, a xanthate chain transfer agent, S-(2-cyano-2-propyl) O-ethyl xanthate, was used. The PVP-b-PVAc block copolymer is composed of a hydrophilic and hydrophobic segment, and has the ability to self-assemble in aqueous solution. The PVP-b-PVAc block copolymers were characterized by 1H NMR spectroscopy to confirm their self-assembly in water. The critical micelle concentration was determined by fluorescence spectroscopy. A combination of dynamic light scattering, transmission electron microscopy, and static light scattering was used to further characterize the self-assembly of the block copolymers in water.
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