The Power of Shielding: Low Toxicity and High Transfection Performance of Cationic Graft Copolymers Containing Poly(2-oxazoline) Side Chains

Abstract New type of carriers based on grafted poly(ionic liquid)s was designed for delivery of ionically attached salicylates (Sal). Choline derived ionic liquid monomeric units were successfully introduced with various content in the side chains by the controlled radical polymerization. Properly high amounts of ionic pharmaceutics in the polymer systems were achieved by the well-fitted length and grafting degree of the side chains. In aqueous solution the graft copolymers were self-assembled into the spherical superstructures with sizes up to 73 nm. Delivery studies showed “burst” release within 4 h, after that it was slower yielding ~70% of released drug within 80 h. Proposed nanocarriers supported low toxicity against human cells (NHDF and BEAS-2B), anti-inflammation activity evaluated with the use of pro-inflammatory interleukins (IL-6 and IL-8) and antibacterial activities towards E. coli. Adjustment of ionic drug content by structural parameters of graft copolymers, including grafting degree and graft length, are advantageous to tailor nanocarriers with self-assembly properties in aqueous media. Effective release process by ionic exchange and biological activity with low toxicity are promising for further development of this type of drug delivery (DDS).

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Synthesis of poly(N-tert-butylaziridine) macromonomers and graft copolymers with uniform side chains

Macromolecular Chemistry and Physics ◽

10.1002/macp.1995.021961015 ◽

1995 ◽

Vol 196 (10) ◽

pp. 3253-3266 ◽

Cited By ~ 2

Author(s):

Darina C. Christova ◽

Rumiana S. Velichkova

Keyword(s):

Graft Copolymers ◽

Side Chains

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Synthesis and characterization of amphiphilic graft copolymers with hydrophobic poly(α-methylstyrene) backbone and hydrophilic poly(n-vinylpyrrolidone) side chains

e-Polymers ◽

10.1515/epoly.2012.12.1.117 ◽

2012 ◽

Vol 12 (1) ◽

Author(s):

Fatima Zohra Sebba ◽

Seghier Ould Kada ◽

Mohamed Benaicha ◽

Nerjesse Nemiche

Keyword(s):

Graft Copolymer ◽

Graft Copolymers ◽

Radical Copolymerization ◽

Side Chains ◽

Free Radical Copolymerization ◽

Good Efficiency ◽

Molecular Weights ◽

Grafting Reaction ◽

Viscosity Variation ◽

End Capping

AbstractIn this study, 2-oxopropylmethacrylate-terminated poly(N-vinyl-2- pyrrolidone) is produced by cationic polymerization using HClO4 as an initiator. Termination (end capping) step is accomplished using 2- hydroxypropylmethacrylate (2HPMA) and the polymer product has different chain lengths of molecular weight averages ranging from 672 to 3049 g/mol. The study also synthesised amphipathic graft copolymers having hydrophobic poly(α- methylstyrene) as a backbone chain and hydrophilic poly(N-vinyl-2-pyrrolidone) (PVP) as side chains of various lengths. The copolymer synthesis was accomplished by free radical copolymerization of ω-oxopropylmethacrylate PVP in the presence of α-methyl styrene initiated with benzoyl peroxide. Measurements of the dynamic viscosity of the polymer solution (20% weight of macromonomers in ethanol) show that the viscosity is proportional to the average molecular weights M̅n . However, a reverse behaviour of the viscosity variation with regard to M̅n is observed for graft copolymer samples. The viscosity variation with respect to the graft copolymer mass must be due to steric effects, which are strongly pronounced in grafted copolymer chains. Appearance of the number of side chains attached to poly(α-methylstyrene) backbone reveals that the grafting reaction has occurred with good efficiency.

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