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A nanoparticle-based system, composed of the gallium(III) complex of a minimally substituted corrole that is coated by transferrin as a targeting vehicle ( NPs), has been used for pre-clinical evaluation of its efficacy against human metastatic castration-resistant prostate cancer (mCRPC) tumor xenografts. All mice ( = 9) responded to a dose of 10 mg/kg, with a remarkable tumor growth inhibition of 400% following 2 weeks of treatment; Ames and hERG tests excluded potential concerns regarding mutagenicity and cardiotoxicity, respectively. Also demonstrated is the potential application of these NPs as sonodynamic agents for the preclinical treatment of pancreatic cancer. 10 mg/kg NPs combined with exposure to ultrasound waves (2 min of 1 MHz 0.1 w/cm twice a week) induced up to 77% tumor shrinkage. Consistently, tumor/tissue distribution and serum levels of NPs in mice revealed high tumor specificity, favorable pharmacokinetics, fast absorption, slower redistribution, and very slow drug clearance.