1: J Control Release. 2007 Mar 12;118(1):136-44. Epub 2006 Dec 12.

Copolymers of epsilon-caprolactone and quaternized epsilon-caprolactone as gene
carriers.

Vroman B, Mazza M, Fernandez MR, Jerome R, Preat V.

Unite de Pharmacie Galenique, Universite Catholique de Louvain, Avenue E.
Mounier 73.20, 1200 Brussels, Belgium.

New copolymers of epsilon-caprolactone (CL) and gamma-bromo-epsilon-caprolactone
quaternized by pyridine (Py+CL) were investigated as non-viral vectors for gene
delivery. Copolymers with two molar compositions (50 Py+CL/50 CL and 80 Py+CL/20
CL), each with a diblock or a random structure, were used to prepare
nanoparticulate complexes with DNA. Average size and surface charge of the
complexes and extent of the complexation were measured. The DNA condensation by
the copolymers was analysed by a gel retardation assay. Cytotoxicity and
transfection efficiency of the copolymers were also evaluated in HeLa cells and
compared with polyethylenimine 50 kDa. The size of the polyplexes was
approximately 200 nm. The zeta potential first increased with the copolymer/DNA
charge ratio and became positive for charge ratios in the 2-4 range depending on
the type of copolymer. DNA was completely condensed within the nanoparticles and
the degree of interaction was very high. Cytotoxicity and transfection
efficiency were found to be comparable to polyethylenimine 50 kDa. The
experimental results suggest that the novel copolymers can be used as novel gene
delivery vectors.

PMID: 17258343 [PubMed - in process]

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