Details

Autor(en) / Beteiligte

• NAKAMURA, Junichi
• NAKAJIMA, Naoki
• MATSUMURA, Kazuaki
• HYON, Suong-Hyu

Titel

Water-soluble Taxol Conjugates with Dextran and Targets Tumor Cells by Folic Acid Immobilization

Ist Teil von

• Anticancer research, 2010-03, Vol.30 (3), p.903-909

Ort / Verlag

Attiki: International Institute of Anticancer Research

Erscheinungsjahr

2010

Quelle

MEDLINE

Beschreibungen/Notizen

• Paclitaxel (taxol) is a very effective anticancer drug. However, the solution used to enhance the water solubility of paclitaxel, a mixture of polyoxyethylene castor oil (Cremphor EL) and dehydrated ethanol, causes irritation. Our aim is to develop a water-soluble taxol with a high anticancer effect. Taxol derivatives (conjugation with aminated dextran, Dex-TXL) were synthesized for the water-solublization of taxol and folic acid (FA) was ionically and covalently conjugated with Dex-TXL. In addition, their anticancer activity was investigated in vitro with KB cells (a folate receptor-overexpressing carcinoma cell line of the oral cavity). The high solubility of Dex-TXL conjugates (2700 times higher than that of intact taxol) needed no additional Cremophor EL or dehydrated ethanol. Dex-TXL showed 2-3 times greater anticancer effect when conjugated with FA. These results suggest that conjugation with dextran and FA could bring about an improvement in taxol anticancer therapy.