Liposomes Containing Gadodiamide: Preparation, Physicochemical Characterization, and In Vitro Cytotoxic Evaluation

The aim of this study was to develop, characterize and assess the cytotoxic activity of pHsensitive (pHL-Gd), stealth pH-sensitive (SpHL-Gd), and conventional (convL-Gd) liposomes containing gadodiamide (Gd-DTPA-BMA). Formulations were prepared by reverse-phase evaporation method and their physicoch...

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Bibliographic Details
Published in:	Current drug delivery Vol. 14; no. 4; p. 566
Main Authors:	Maia, Ana Luiza Chaves, Fernandes, Christian, de Oliveira, Cynthia Nara Pereira, Teixeira, Claudia Salviano, Oliveira, Mariana Silva, Soares, Daniel Cristian Ferreira, Ramaldes, Gilson Andrade
Format:	Journal Article
Language:	English
Published:	United Arab Emirates 01-06-2017
Subjects:	Cell Line, Tumor Drug Delivery Systems Gadolinium DTPA - chemistry Humans Liposomes Particle Size Polyethylene Glycols Antineoplastic agent cancer treatment 4T1 breast cancer cell line liposomes in vitro cytotoxic evaluation Gd-DTPA-BMA
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Summary:	The aim of this study was to develop, characterize and assess the cytotoxic activity of pHsensitive (pHL-Gd), stealth pH-sensitive (SpHL-Gd), and conventional (convL-Gd) liposomes containing gadodiamide (Gd-DTPA-BMA). Formulations were prepared by reverse-phase evaporation method and their physicochemical properties were evaluated by means of particle size, zeta potential, and Gd-DTPA-BMA entrapment. SpHL-Gd was considered being the most promising liposome, since it combines stealth and fusogenic characteristics that might contribute to achieve higher therapeutic efficiency. Their drug encapsulation percentages have been optimized satisfactorily. The addition of Gd-DTPA-BMA at 125 μmol/mL in the SpHL-Gd preparation allowed obtaining liposomes with appropriate encapsulation percentage (20.3 ± 0.1%) and entrapment (25.4 ± 0.1 μmol/mL). The cytotoxic studies on the 4T1 breast cancer cell line demonstrated that liposomes-loaded with Gd-DTPA-BMA inhibited cancer cell. pHL-Gd and SpHL-Gd liposomes showed higher activity than convL-Gd and free Gd-DTPA-BMA, indicating that the pH-sensitive characteristic was important to improve intracellular delivery. The presence of polyethylene glycol (PEG) in the SpHL-Gd formulation did not affect the pH-sensitivity and internalization. Therefore, the results of this study suggest the feasibility of liposomes containing Gd-DTPA-BMA as a new promising controlled delivery system.
ISSN:	1875-5704
DOI:	10.2174/1567201813666160907095404