Preparation and characterization of folate-targeted pEG-coated pDMAEMA-based polyplexes

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 sma...

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Bibliographic Details
Published in:Journal of controlled release 2003-02, Vol.87 (1), p.167-176
Main Authors: van Steenis, J.H, van Maarseveen, E.M, Verbaan, F.J, Verrijk, R, Crommelin, D.J.A, Storm, G, Hennink, W.E
Format: Article
Language:English
Subjects:
Biological and medical sciences
Drug Delivery Systems - methods
Folate
Folic Acid - administration & dosage
Folic Acid - chemical synthesis
Folic Acid - pharmacokinetics
Gene delivery
General pharmacology
Humans
Medical sciences
Methacrylates - administration & dosage
Methacrylates - chemical synthesis
Methacrylates - pharmacokinetics
Nylons - chemical synthesis
Nylons - pharmacokinetics
Particle Size
pEG
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyethylene Glycols - administration & dosage
Polyethylene Glycols - chemical synthesis
Polyethylene Glycols - pharmacokinetics
Polyplex
Transfection - methods
Tumor Cells, Cultured
Tumor targeting
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Summary: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.
ISSN:0168-3659
1873-4995
DOI:10.1016/S0168-3659(02)00361-9