A Lipo-PEG-PEI complex for encapsulating curcumin that enhances its antitumor effects on curcumin-sensitive and curcumin-resistance cells

A cationic liposome-PEG-PEI complex (LPPC) was used as a carrier for the encapsulation of hydrophobic curcumin to give curcumin/LPPC. Curcumin/LPPC had an average size less than 270 nm and a zeta potential of approximately 40 mV. The LPPC encapsulation efficiency for curcumin was about 45%. The authors found it surprising that the cytotoxic activity of the curcumin/LPPC was fivefold higher than curcumin when tested on curcumin-sensitive cells and 20-fold more active against curcumin-resistant cells. Curcumin/LPPC treatment caused a cell cycle arrest at G2/M phase, which rapidly resulted in apoptosis. The increased cytotoxic activity of curcumin/LPPC is likely attributable to its rapid accumulation in the cell. In vivo, administration of curcumin/LPPC inhibited about 60 – 90% of tumor growth in mice bearing CT-26 or B16F10 cells. These results demonstrate LPPC encapsulation technology is able to enhance the effects of antitumor drugs. Use of this technology may provide a new tool for cancer therapy, especially for drug-resistant cancer.From the Clinical EditorThis team of investigators used a cationic liposome-PEG-PEI complex (LPPC) to encapsulate curcumin. The different delivery method resulted in the five-fold increase of cytotoxic activity against curcumin-sensitive cells and twenty-fold against curcumin-resistant cells.

Graphical AbstractWe recently report a polycationic liposome containing PEI and PEG complex (LPPC) for its application. In this study, LPPC was used as a carrier for the encapsulation of curcumin to give curcumin/LPPC for cancer therapy. DOPC and DLPC lipids were mixed with curcumin. The lipids mixture was coated onto a round bottom flask by a rotary evaporator to yield a thin lipid film. Then PEG-PEI solution was added into the container and vigorously resuspended to form curcumin/LPPC. Curcumin/LPPC could enhance the cytotoxicity and rapidly penetrate into curcumin-senstive and –resistance cells. Curcumin/LPPC also significantly inhibited the tumor growth in mice bearing colon or melanoma tumor.Figure optionsDownload high-quality image (120 K)Download as PowerPoint slide