Liposomal formulation of DIMIQ, potential antitumor indolo[2,3-b]quinoline agent and its cytotoxicity on hepatoma Morris 5123 cells

Drug Delivery
Anna JarominLukasz Kaczmarek

Abstract

The cytotoxic and antitumor activity of DIMIQ (5,11-dimethyl-5H-indolo[2,3-b]quinoline), synthetic analog of neocryptolepine, makes this compound a potential antitumor agent. An attempt to obtain liposomal form of DIMIQ.HCl was undertaken in the present study. Standard experimental conditions were chosen and information on the physicochemical parameters of the liposome dispersion containing studied indoloquinoline agent was collected. The effective and efficient encapsulation of DIMIQ.HCl (66.6%) in conventional liposomes (FAT-MLV, DMPC:DMPG 7:3 w/w at pH 7.0), uniformity of the size of liposomal vesicles, and high stability at pH 6.5 were demonstrated. Hemolysis of sheep erythrocytes induced by free form of DIMIQ.HCl was dramatically decreased after addition of liposome-entrapped DIMIQ.HCl. Treatment of hepatoma Morris 5123 cells for 24 hr with different concentrations of both free and its liposomal formulation of DIMIQ.HCl resulted in significant changes in cell morphology accompanied by reduction of cell viability.

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Citations

Sep 15, 2012·Biological & Pharmaceutical Bulletin·Anna JarominArkadiusz Kozubek
Apr 28, 2012·Angewandte Chemie·Ashley L PumphreyTom G Driver
May 12, 2012·Journal of Medicinal Chemistry·Katarzyna SidorykWanda Peczyńska-Czoch
Nov 21, 2009·European Journal of Medicinal Chemistry·Chiao-Li YangCherng-Chyi Tzeng
Jul 27, 2010·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Robert M GenganPalathurai S Mohan

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