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Current Drug Delivery

Author(s): Isabella Orienti*, Timothy P. Cripe, Mark A. Currier, Cristina Cavallari, Gabriella Teti and Mirella Falconi

DOI: 10.2174/1567201816666191002100745

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

Page: [807 - 817] Pages: 11

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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.

Graphical Abstract

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