The Open Drug Delivery Journal




(Discontinued)

ISSN: 1874-1266 ― Volume 5, 2014

In Vitro Evaluation of the Activity of Gemcitabine-Loaded Pegylated Unilamellar Liposomes Against Papillary Thyroid Cancer Cells


The Open Drug Delivery Journal, 2010, 4: 55-62

Margherita Vono, Donato Cosco, Christian Celia, Donatella Paolino, Marilena Celano, Diego Russo, Massimo Fresta

Department of Pharmacobiological Sciences, University “Magna Græcia” of Catanzaro, Campus Universitario “S. Venuta” - Building of BioSciences, Viale Salvatore Venuta, I-88100 Germaneto (CZ), Italy

Electronic publication date 24/8/2010
[DOI: 10.2174/1874126601004010055]




Abstract:

Papillary carcinoma is the most common form of malignant thyroid tumor. At present, a subset of these tumors are poorly responsive to the current treatment. Gemcitabine is a pyrimidine analog active against different types of solid tumors, but its use is limited by its short half-life. To improve the therapeutic effectiveness of this drug, gemcitabine-loaded unilamellar pegylated liposomes were prepared and investigated against two human papillary thyroid carcinoma cell lines, i.e. TPC-1 and B-CPAP cells. The pH gradient drug encapsulation followed by the membrane extrusion technique were used to achieve unilamellar liposomes characterized by a mean size of ~200 nm, a polydispersity index of 0.02 and a zeta potential of -1.7 mV. The gemcitabine was released from liposomes following a biphasic profile. The liposomal encapsulated gemcitabine showed an increased cytotoxic activity compared to the free drug against both thyroid carcinoma cell lines, as a consequence of the better drug internalization favored by the vesicular device. These findings demonstrate the advantage of channeling gemcitabine by liposomes suggesting a promising role for such a pharmaceutical formulation in the treatment of refractory papillary thyroid carcinoma.


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