Carboplatin nanocapsules: a highly cytotoxic, phospholipid-based formulation of carboplatin
Platinum-based drugs are widely used in cancer chemotherapy. However, their clinical use is limited by systemic toxicity, rapid blood clearance, and the occurrence of resistance. Our research is aimed at increasing the therapeutic index of these drugs by encapsulation in a lipid formulation. Previou...
Saved in:
Published in | Molecular cancer therapeutics Vol. 5; no. 8; pp. 2007 - 2012 |
---|---|
Main Authors | , , , , |
Format | Journal Article |
Language | English |
Published |
United States
American Association for Cancer Research
01.08.2006
|
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | Platinum-based drugs are widely used in cancer chemotherapy. However, their clinical use is limited by systemic toxicity,
rapid blood clearance, and the occurrence of resistance. Our research is aimed at increasing the therapeutic index of these
drugs by encapsulation in a lipid formulation. Previously, we developed a method for efficient encapsulation of cisplatin
in a lipid formulation, yielding cisplatin nanocapsules. Here, we show that carboplatin, a cisplatin-derived anticancer drug
with different chemical properties, can be efficiently encapsulated in a lipid formulation by a similar method. The carboplatin
nanocapsules exhibit a very high cytotoxicity in vitro : the IC 50 value of carboplatin nanocapsules is up to a 1,000-fold lower than that of conventional carboplatin when tested on a panel
of carcinoma cell lines. Cellular platinum content analysis and confocal fluorescent imaging of the interaction of the carboplatin
nanocapsules with IGROV-1 cells indicate that the improved cytotoxicity is due to increased platinum accumulation in the cells,
resulting from uptake of the formulation by endocytosis. [Mol Cancer Ther 2006;5(8):2007–12] |
---|---|
Bibliography: | ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-1 content type line 23 |
ISSN: | 1535-7163 1538-8514 |
DOI: | 10.1158/1535-7163.MCT-06-0089 |