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
-
Cancer Gene Therapy Utilizing Interleukin-13 Receptor α2 Chain
Current Gene Therapy Imaging of Hypoxia Using PET and MRI
Current Pharmaceutical Biotechnology Angiotensin II, Cell Proliferation and Angiogenesis Regulator: Biologic and Therapeutic Implications in Cancer
Current Vascular Pharmacology Plant Coumestans: Recent Advances and Future Perspectives in Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry 3D-QSAR and Docking Studies of 4-morpholinopyrrolopyrimidine Derivatives as Potent mTOR Inhibitors
Letters in Drug Design & Discovery Natural and Synthetic Agents Targeting Inflammation and Angiogenesis for Chemoprevention of Prostate Cancer
Current Cancer Drug Targets Hypomethylation and Activation of Syncytin-1 Gene in Endometriotic Tissue
Current Pharmaceutical Design Bispecific Antibodies: An Innovative Arsenal to Hunt, Grab and Destroy Cancer Cells
Current Pharmaceutical Biotechnology Targeting Opioid and Neurokinin-1 Receptors to Treat Alcoholism
Current Medicinal Chemistry Recent Advances in Radiation Therapy of Cancer Cells: A Step towards an Experimental and Systems Biology Framework
Current Radiopharmaceuticals CNS Drug Delivery Systems: Novel Approaches
Recent Patents on Drug Delivery & Formulation Vasotrophic Regulation of Age-Dependent Hypoxic Cerebrovascular Remodeling
Current Vascular Pharmacology Recent Findings on the Application of Toll-like Receptors Agonists in Cancer Therapy
Current Medicinal Chemistry Effective Treatment of Human Lung Cancer by Targeting Tissue Factor with a Factor VII-Targeted Photodynamic Therapy
Current Cancer Drug Targets Role of Progastrins and Gastrins and Their Receptors in GI and Pancreatic Cancers: Targets for Treatment
Current Pharmaceutical Design Therapeutic Challenges in Neuroendocrine Tumors
Anti-Cancer Agents in Medicinal Chemistry Virtual Screening of Acetylcholinesterase Inhibitors Based on Machine Learning Combined with Molecule Docking Methods
Current Bioinformatics Mitosis-Targeting Natural Products for Cancer Prevention and Therapy
Current Drug Targets Mouse Induced Glioma-Initiating Cell Models and Therapeutic Targets
Anti-Cancer Agents in Medicinal Chemistry In Vivo Optical Imaging in Gene & Cell Therapy
Current Gene Therapy