期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 70, 期 3, 页码 741-748出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2008.07.017
关键词
Polymeric micelles; Triptolide; Anti-tumor; Immuno-modulation; Sarcoma 180-bearing mice; A2780 cells
资金
- National Basic Research Program of China [2006CB933301]
Triptolide (TP) possesses both anti-tumor and immuno-suppressive activities. Its immuno-suppressive activity may be disadvantageous for the therapy of cancers. A novel polymeric micelle system containing TP (TP-PM) was constructed by the solvent evaporation method using methoxypolyethylene glycolpoly(D,L-lactic acid)-block copolymer as the carrier, and was characterised using photon correlation spectroscopy, transmission electron microscopy and high performance liquid chromatography. The antitumour and immuno-modulation effects of TP-PM were evaluated in sarcoma 180-bearing mice and A2780 cells. Results demonstrated that TP-PM had an average diameter of 78.9 nm, encapsulation efficiency of 66.7%, core-shell morphology and a long-term stability. TP-PM could significantly inhibit tumour growth via intravenous injections at the dose levels of 0.0375, 0.075 and 0.15 mg/kg, and their inhibition rates were 42.5%, 46.0% and 49.9%, respectively; they showed similar cytotoxicity against A2780 cells compared to that of TP, Simultaneously, TP-PM had no effect on the thymus index, spleen index, spleen lymphocyte proliferation and the TNF-alpha and IL-2 levels in serum as compared with TP. Therefore, TP encapsulated in polymeric micelles does not demonstrate immuno-suppressive activity but does not lose its anti-tumour effect. These results show that polymeric micelles are a promising carrier for cancer therapy using TP. (C) 2008 Elsevier B.V. All rights reserved.
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