A Novel Micellar PEGylated Hyperbranched Polyester as a Prospective Drug Delivery System for Paclitaxel

✍ Scribed by Christina Kontoyianni; Zili Sideratou; Theodossis Theodossiou; Leto-Aikaterini Tziveleka; Dimitris Tsiourvas; Constantinos M. Paleos

• Publisher: John Wiley and Sons
• Year: 2008
• Tongue: English
• Weight: 374 KB
• Volume: 8
• Category: Article
• ISSN: 1616-5187
• DOI: 10.1002/mabi.200800015

✦ Synopsis

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 · 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 · mL^−1^ concentration while LD~50~ was 3.5 mg · 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.

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