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

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

Volume: 14 Issue: 4

Author(s): Ana Luiza Chaves Maia, Christian Fernandes, Cynthia Nara Pereira de Oliveira, Claudia Salviano Teixeira, Mariana Silva Oliveira, Daniel Cristian Ferreira Soares*Gilson Andrade Ramaldes

Affiliation:

• Federal University of Itajubá, Rua Irmã Ivone Drumond, 200, Distrito Industrial II, 35903-087, Itabira, Minas Gerais,Brazil

Keywords: Antineoplastic agent, cancer treatment, 4T1 breast cancer cell line, Gd-DTPA-BMA, in vitro cytotoxic evaluation, liposomes.

Abstract: Background: 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).

Methods: 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).

Results: 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.

Conclusion: 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.

Cite this article as:

Maia Luiza Chaves Ana, Fernandes Christian, de Oliveira Nara Pereira Cynthia, Teixeira Salviano Claudia, Oliveira Silva Mariana, Soares Cristian Ferreira Daniel*, Ramaldes Andrade Gilson, Liposomes Containing Gadodiamide: Preparation, Physicochemical Characterization, and In Vitro Cytotoxic Evaluation, Current Drug Delivery 2017; 14 (4) . https://dx.doi.org/10.2174/1567201813666160907095404

DOI https://dx.doi.org/10.2174/1567201813666160907095404	Print ISSN 1567-2018
Publisher Name Bentham Science Publisher	Online ISSN 1875-5704