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.Keywords: Antineoplastic agent, cancer treatment, 4T1 breast cancer cell line, Gd-DTPA-BMA, in vitro cytotoxic evaluation, liposomes.
Current Drug Delivery
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.Export Options
About this article
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 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Applications of Molecular Imaging in Cancer Gene Therapy
Current Gene Therapy A Review of Studies on Targeting Interleukin 4 Receptor for Central Nervous System Malignancy
Current Molecular Medicine Strategies of overcoming the physiological barriers for tumor-targeted nano-sized drug delivery systems
Current Pharmaceutical Design Polyunsaturated Fatty Acids and their Metabolites in Neural Development and Implications for Psychiatric Disorders
Current Psychopharmacology Graphene Oxide-Based Nanocarriers for Cancer Imaging and Drug Delivery
Current Pharmaceutical Design Targeting miR-21 Induces Autophagy and Chemosensitivity of Leukemia Cells
Current Drug Targets Patent Selections
Recent Patents on Anti-Cancer Drug Discovery The Biology of the Sodium Iodide Symporter and its Potential for Targeted Gene Delivery
Current Cancer Drug Targets Double-Faced Role of Human Mesenchymal Stem Cells and their Role/Challenges in Cancer Therapy
Current Stem Cell Research & Therapy Inventions Designed to Enhance Drug Delivery Across Epithelial and Endothelial Cells Through the Paracellular Pathway
Recent Patents on Drug Delivery & Formulation Using the Neurosphere Assay to Quantify Neural Stem Cells In Vivo
Current Pharmaceutical Biotechnology Methylenetetrahydrofolate Reductase (MTHFR): A Novel Target for Cancer Therapy
Current Pharmaceutical Design Pharmacological Activation of Protein Phosphatase 2 A (PP2A): A Novel Strategy to Fight Against Human Malignancies?
Current Medicinal Chemistry Role of Histone Deacetylases (HDACs) in Epilepsy and Epileptogenesis
Current Pharmaceutical Design Transferrin and the Transferrin Receptor: Of Magic Bullets and Other Concerns
Inflammation & Allergy - Drug Targets (Discontinued) Meet Our Editorial Board Member
Protein & Peptide Letters Role of Pancreatic β-Cell Death and Cell Death-Associated Inflammation in Diabetes
Current Molecular Medicine Recent Progress in Discovery and Development of Antimitotic Agents
Anti-Cancer Agents in Medicinal Chemistry Substance P: Structure, Function, and Therapeutics
Current Topics in Medicinal Chemistry Anti-Cancer Effects of Citalopram on Hepatocellular Carcinoma Cells Occur via Cytochrome C Release and the Activation of NF-kB
Anti-Cancer Agents in Medicinal Chemistry