A novel micellar PEGylated hyperbranched polyester as a prospective drug delivery system for paclitaxel |
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Authors: | Kontoyianni Christina Sideratou Zili Theodossiou Theodossis Tziveleka Leto-Aikaterini Tsiourvas Dimitris Paleos Constantinos M |
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Affiliation: | Institute of Physical Chemistry, NCSR "Demokritos", 15310 Aghia Paraskevi, Attiki, Greece. |
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Abstract: | A hyperbranched aliphatic polyester has been functionalized with PEG chains to afford a novel water-soluble BH40-PEG polymer which exhibits unimolecular micellar properties, and is therefore appropriate for application as a drug-delivery system. The solubility of the anticancer drug paclitaxel was enhanced by a factor of 35, 110, 230, and 355 in aqueous solutions of BH40-PEG of 10, 30, 60, and 90 mg x mL(-1), respectively. More than 50% of the drug is released at a steady rate and release is almost complete within 10 h. The toxicity of BH40-PEG was assessed in vitro with A549 human lung carcinoma cells and found to be nontoxic for 3 h incubation up to a 1.75 mg x mL(-1) concentration while LD50 was 3.5 mg x mL(-1). Finally, it was efficiently internalized in cells, primarily in the absence of foetal bovine serum, while confocal microscopy revealed the preferential localization of the compound in cell nuclei. [Figure: see text]. |
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Keywords: | drug delivery systems hyperbranched paclitaxel PEGylation polyesters |
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