Anticancer efficacy of a novel propofol–linoleic acid-loaded escheriosomal formulation against murine hepatocellular carcinoma

Abstract

Aim: The preparation and characterization of a novel escheriosomal nanoparticle formulation of a potent anticancer conjugate, 2,6-diisopropylphenol-linoleic acid (2,6P–LA), and evaluation of its anticancer efficacy against diethyl nitrosamine-induced hepatocellular carcinoma (HCC) in BALB/c mice. Materials & methods: Escheriosomized 2,6P–LA nanoparticles were characterized for size, zeta-potential, entrapment efficiency, release kinetics and in vivo toxicity. Their anticancer potential was evaluated on the basis of survival, DNA fragmentation, caspase-3 activation, western blot analysis of apoptotic factors and histopathological changes in hepatocytes of treated animals. Results: The escheriosomized 2,6P–LA nanoparticles exhibited low toxicity, biocompatibility and bioavailability. As revealed by apoptosis induction, survival rate, expression profiles of Bax, Bcl-2 and caspase-9, escheriosomized 2,6P–LA nanoparticles were more effective in the treatment of HCC than the free form of 2,6P–LA in experimental animals. Conclusion: 2,6P–LA-bearing escheriosome nanoparticles are effective in suppressing HCC in mice. Original submitted 17 January 2012; Revised submitted 27 August 2012; Published online 14 January 2013