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A Cationic Nanomicellar Complex of the Quaternary Amphiphilic Amine RC16+ with Fenretinide as a New Multitasking System for Antitumor Therapy

[ Vol. 16 , Issue. 9 ]

Author(s):

Isabella Orienti*, Timothy P. Cripe, Mark A. Currier, Cristina Cavallari, Gabriella Teti and Mirella Falconi   Pages 807 - 817 ( 11 )

Abstract:


Objectives: This study investigated the antitumor effect of a new nanomicellar complex obtained by combining the antitumor agent fenretinide with a quaternary amphiphilic amine RC16+ also endowed with antitumor activity.

Methods: The complex (Fen-RC16+) strongly improved the aqueous solubility of fenretinide (from 1,71 ± 0.08 μg/ml, pure fenretinide to 1500 ± 164 μg /ml, Fen-RC16+ complex) and provided a cytotoxic effect on SH-SY5Y neuroblastoma cell lines resulting from the intrinsic activity of both the complex components. Moreover, the mean size of the nanomicellar complex (ranging from 20 ± 1.97 nm to 40 ± 3.05 nm) was suitable for accumulation to the tumor site by the enhanced permeability and retention effect and the positive charge provided by the quaternary RC16+ induced adsorption of the complex on the tumor cell surface improving the intracellular concentration of fenretinide.

Results: All these characteristics made the Fen-RC16+ complex a multitasking system for antitumor therapy.

Conclusion: Indeed its in vivo activity, evaluated on SH-SY5Y xenografts, was strong, and the tumor growth did not resume after the treatment withdrawal.

Keywords:

Cationic nanomicelles, quaternary amphiphilic amine RC16+, fenretinide, ionic interactions, tumor cell, antitumor activity.

Affiliation:

Department of Pharmacy and Biotechnology, University of Bologna, Via S. Donato 19/2, Bologna, Center for Childhood Cancer and Blood Diseases, Nationwide Children’s Hospital, Columbus, Ohio, Center for Childhood Cancer and Blood Diseases, Nationwide Children’s Hospital, Columbus, Ohio, Department of Pharmacy and Biotechnology, University of Bologna, Via S. Donato 19/2, Bologna, Department for Biomedical and Neuromotor Sciences (DIBINEM), University of Bologna, via Irnerio 48, Bologna, Department for Biomedical and Neuromotor Sciences (DIBINEM), University of Bologna, via Irnerio 48, Bologna



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