Abstract
A folate-poly(ethylene glycol) conjugate capable of covalent coupling to primary amines present at the surface of polyplexes was developed. Coating of poly(dimethylaminomethyl methacrylate (pDMAEMA)-based polyplexes with this folate-pEG conjugate led to a sharp decrease of the ζ-potential, and a small increase in particle size. The size of the particles in isotonic medium did not change markedly in time demonstrating that rather stable particles were formed. The in vitro cellular toxicity of the pEGylated polyplexes with and without folate ligands was lowered considerably compared to uncoated polyplexes. The toxicity observed for the targeted pEGylated polyplexes was slightly higher than that of corresponding untargeted polyplexes, which might indicate an increased cellular association of targeted polyplexes. Transfection of OVCAR-3 cells in vitro was markedly increased compared to untargeted pEGylated polyplexes, suggesting targeted gene delivery. © Elsevier Science B.V. All rights reserved.
| Original language | English |
|---|---|
| Pages (from-to) | 167-176 |
| Number of pages | 10 |
| Journal | Journal of Controlled Release |
| Volume | 87 |
| Issue number | 1-3 |
| DOIs | |
| Publication status | Published - 21 Feb 2003 |
Keywords
- Folate
- Gene delivery
- pEG
- Polyplex
- Tumor targeting
- copolymer
- folic acid derivative
- macrogol
- methacrylic acid methyl ester
- cell line
- conference paper
- controlled study
- cytotoxicity
- drug analysis
- drug coating
- drug delivery system
- drug synthesis
- drug targeting
- female
- gene delivery system
- genetic transfection
- human
- human cell
- in vitro study
- ovary cancer
- particle size
- priority journal
- zeta potential