All-trans retinoic acid (ATRA) is an anti-tumor compound, exerting different anti-cancer effects on different types of cancer cells. Unfortunately, retinoids are also characterized by certain side effects following systemic administration, such as the burning of skin and general malaise. The highly variable degree of bioavailability of ATRA plus its tendency to induce its own destruction through metabolic degradation following oral treatment necessitate the development of alternative formulations. The aim of this work is to evaluate the physico-chemical properties of unilamellar, ATRA-containing liposomes and to investigate the cytotoxic activity of this potential nanomedicine on human thyroid carcinoma cells. Liposomes made up of DPPC/Chol/DSPE-mPEG2000 (6:3:1 molar ratio), characterized by a mean diameter of similar to 200 nm, a polydispersity index of 0.1 and a negative surface charge, were used as ATRA-carriers and their antiproliferative efficacy was investigated in comparison with the free drug on three different human thyroid carcinoma cell lines (PTC-1, B-CPAP, and FRO) through MTT-testing. The liposomes protected the ATRA against photodegradation and increased its antiproliferative properties due to the improvement of its cellular uptake. ATRA-loaded liposomes could be a novel formulation useful for the treatment of anaplastic thyroid carcinoma. (C) 2016 Elsevier B.V. All rights reserved.

Anticancer activity of all-trans retinoic acid-loaded liposomes on human thyroid carcinoma cells

Mare R;Paolino D;Fresta M;Cosco D
2017-01-01

Abstract

All-trans retinoic acid (ATRA) is an anti-tumor compound, exerting different anti-cancer effects on different types of cancer cells. Unfortunately, retinoids are also characterized by certain side effects following systemic administration, such as the burning of skin and general malaise. The highly variable degree of bioavailability of ATRA plus its tendency to induce its own destruction through metabolic degradation following oral treatment necessitate the development of alternative formulations. The aim of this work is to evaluate the physico-chemical properties of unilamellar, ATRA-containing liposomes and to investigate the cytotoxic activity of this potential nanomedicine on human thyroid carcinoma cells. Liposomes made up of DPPC/Chol/DSPE-mPEG2000 (6:3:1 molar ratio), characterized by a mean diameter of similar to 200 nm, a polydispersity index of 0.1 and a negative surface charge, were used as ATRA-carriers and their antiproliferative efficacy was investigated in comparison with the free drug on three different human thyroid carcinoma cell lines (PTC-1, B-CPAP, and FRO) through MTT-testing. The liposomes protected the ATRA against photodegradation and increased its antiproliferative properties due to the improvement of its cellular uptake. ATRA-loaded liposomes could be a novel formulation useful for the treatment of anaplastic thyroid carcinoma. (C) 2016 Elsevier B.V. All rights reserved.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.12317/5457
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