Details

Autor(en) / Beteiligte

• Shuai, Xintao
• Ai, Hua
• Nasongkla, Norased
• Kim, Saejeong
• Gao, Jinming

Titel

Micellar carriers based on block copolymers of poly(ε-caprolactone) and poly(ethylene glycol) for doxorubicin delivery

Ist Teil von

• Journal of controlled release, 2004-08, Vol.98 (3), p.415-426

Ort / Verlag

Amsterdam: Elsevier B.V

Erscheinungsjahr

2004

Quelle

MEDLINE

Beschreibungen/Notizen

• Diblock copolymers of poly(ε-caprolactone) (PCL) and monomethoxy poly(ethylene glycol) (MPEG) with various compositions were synthesized. The amphiphilic block copolymers self-assembled into nanoscopic micelles and their hydrophobic cores encapsulated doxorubicin (DOX) in aqueous solutions. The micelle diameter increased from 22.9 to 104.9 nm with the increasing PCL block length (2.5–24.7 kDa) in the copolymer composition. Hemolytic studies showed that free DOX caused 11% hemolysis at 200 μg ml −1, while no hemolysis was detected with DOX-loaded micelles at the same drug concentration. An in vitro study at 37 °C demonstrated that DOX-release from micelles at pH 5.0 was much faster than that at pH 7.4. Confocal laser scanning microscopy (CLSM) demonstrated that DOX-loaded micelles accumulated mostly in cytoplasm instead of cell nuclei, in contrast to free DOX. Consistent with the in vitro release and CLSM results, a cytotoxicity study demonstrated that DOX-loaded micelles exhibited time-delayed cytotoxicity in human MCF-7 breast cancer cells.