Abstract
Background: Lipiodol (iodized poppy seed oil) accumulates predominately in the tumor rather than in the liver tissue [1, 2]. Therefore, mixing anticancer drugs with Lipiodol may enhance the antitumor effect by increasing the local drug concentration.
Objective: In this pilot study, we made use of Lipiodol as a potential carrier of three promising antitumor metal complexes (tris(8-quinolato)gallium(III) (KP46), tetrachlorobis(indazole)ruthenate(III) (KP1019) and the hydrolysis product of KP1019, mer,trans-[RuCl3(H2O)(Hind)2].
Methods: The stability of the drugs in Lipiodol and the release profile into the aqueous phase were examined independently by three different analytical techniques (high pressure liquid chromatography, HPLC; atom absorption spectroscopy, AAS; and electron spray ionization mass spectrometry, ESI-MS).
Results: The complexes were stable and remained in the Lipiodol emulsion over 3 days. In contrast to KP1019 and KP46, evaluation of Lipiodol emulsions of mer,trans-[RuCl3 (H2O) (Hind) 2] was not possible due to the insolubility of the compound in Lipiodol. KP1019 released rapidly into the aqueous phase in the first week and after 1 month it was not possible to detect the complex in the emulsion. KP46 showed a gradual release with the time resulting in the release of about 6.4 % of KP46 into the aqueous phase after 1 month of incubation.
Conclusion: The initial results show that Lipiodol can be successfully employed as a carrier of anticancer Ru- or Ga-complexes. Furthermore, advantages can overcome the poor water solubility of the metal complexes, opening new perspectives for the use of Lipiodol emulsions in molecular imaging and cancer therapy as theragnostic agents.
Keywords: Antitumor metal complexes, drug targeting, gallium, Lipiodol emulsions, ruthenium, theragnostic agents.
Current Drug Delivery
Title:Studies of KP46 and KP1019 and the Hydrolysis Product of KP1019 in Lipiodol Emulsions: Preparation and Initial Characterizations as Potential Theragnostic Agents
Volume: 15 Issue: 1
Author(s): Irena Pashkunova-Martic*, Berta Cebrian Losantos, Norbert Kandler and Bernhard Keppler
Affiliation:
- Institute of Inorganic Chemistry, University of Vienna, Wahringer Strasse 42, A-1090 Vienna,Austria
Keywords: Antitumor metal complexes, drug targeting, gallium, Lipiodol emulsions, ruthenium, theragnostic agents.
Abstract: Background: Lipiodol (iodized poppy seed oil) accumulates predominately in the tumor rather than in the liver tissue [1, 2]. Therefore, mixing anticancer drugs with Lipiodol may enhance the antitumor effect by increasing the local drug concentration.
Objective: In this pilot study, we made use of Lipiodol as a potential carrier of three promising antitumor metal complexes (tris(8-quinolato)gallium(III) (KP46), tetrachlorobis(indazole)ruthenate(III) (KP1019) and the hydrolysis product of KP1019, mer,trans-[RuCl3(H2O)(Hind)2].
Methods: The stability of the drugs in Lipiodol and the release profile into the aqueous phase were examined independently by three different analytical techniques (high pressure liquid chromatography, HPLC; atom absorption spectroscopy, AAS; and electron spray ionization mass spectrometry, ESI-MS).
Results: The complexes were stable and remained in the Lipiodol emulsion over 3 days. In contrast to KP1019 and KP46, evaluation of Lipiodol emulsions of mer,trans-[RuCl3 (H2O) (Hind) 2] was not possible due to the insolubility of the compound in Lipiodol. KP1019 released rapidly into the aqueous phase in the first week and after 1 month it was not possible to detect the complex in the emulsion. KP46 showed a gradual release with the time resulting in the release of about 6.4 % of KP46 into the aqueous phase after 1 month of incubation.
Conclusion: The initial results show that Lipiodol can be successfully employed as a carrier of anticancer Ru- or Ga-complexes. Furthermore, advantages can overcome the poor water solubility of the metal complexes, opening new perspectives for the use of Lipiodol emulsions in molecular imaging and cancer therapy as theragnostic agents.
Export Options
About this article
Cite this article as:
Pashkunova-Martic Irena*, Losantos Cebrian Berta, Kandler Norbert and Keppler Bernhard, Studies of KP46 and KP1019 and the Hydrolysis Product of KP1019 in Lipiodol Emulsions: Preparation and Initial Characterizations as Potential Theragnostic Agents, Current Drug Delivery 2018; 15 (1) . https://dx.doi.org/10.2174/1567201813666161220153702
DOI https://dx.doi.org/10.2174/1567201813666161220153702 |
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
-
Chemotherapeutic Agents That Induce Mitochondrial Apoptosis
Current Cancer Drug Targets Lectin Microarrays: A Powerful Tool for Glycan-Based Biomarker Discovery
Combinatorial Chemistry & High Throughput Screening Psychotherapy Through Video Game to Target Illness Related Problematic Behaviors of Children with Brain Tumor
Current Medical Imaging Time Recall; Future Concept of Chronomodulating Chemotherapy for Cancer
Current Pharmaceutical Biotechnology The State-of-Art in Angiogenic Properties of Latex from Different Plant Species
Current Angiogenesis (Discontinued) Hypoxic Tumor Microenvironment and Cancer Cell Differentiation
Current Molecular Medicine Synthesis and Biological Evaluation of Novel Osthol Derivatives as Potent Cytotoxic Agents
Medicinal Chemistry Low Grade Inflammation as a Common Pathogenetic Denominator in Age-Related Diseases: Novel Drug Targets for Anti-Ageing Strategies and Successful Ageing Achievement
Current Pharmaceutical Design Protein Extracts from Somaclonal Mistletoe (Viscum Album L.) Callus with Increased Tumor Cytotoxic Activity in Vitro
Current Bioactive Compounds Analogs of Cinnamic Acid Benzyl Amide As Nonclassical Inhibitors of Activated JAK2 Kinase
Current Cancer Drug Targets Small Molecule Kinase Inhibitors as Anti-Cancer Therapeutics
Mini-Reviews in Medicinal Chemistry The Efficacy and Mechanism of Proteasome Inhibitors in Solid Tumor Treatment
Recent Patents on Anti-Cancer Drug Discovery Anticancer Natural Coumarins as Lead Compounds for the Discovery of New Drugs
Current Topics in Medicinal Chemistry Editorial [Low Grade Inflammation as a Common Pathogenetic Denominator in Age-Related Diseases: Novel Drug Targets for Anti-Ageing Strategies and Successful Ageing Achievement. PART I. (Executive Editors: Calogero Caruso Thea Magrone and Emilio Jirilllo)]
Current Pharmaceutical Design Editorial (Thematic Issue: Oncoviruses and Head and Neck Cancer: An Impending Facts)
Recent Patents on Biomarkers Wnt/β-Catenin/LEF-1 Signaling in Chronic Lymphocytic Leukemia (CLL): A Target for Current and Potential Therapeutic Options
Current Cancer Drug Targets MicroRNAs as Potential Diagnostic and Prognostic Biomarkers in Hepatocellular Carcinoma
Current Drug Targets Emergence of Nanomedicine as Cancer Targeted Magic Bullets: Recent Development and Need to Address the Toxicity Apprehension
Current Drug Discovery Technologies Sugar-Borate Esters – Potential Chemical Agents in Prostate Cancer Chemoprevention
Anti-Cancer Agents in Medicinal Chemistry Targeting the Expression of Anti-Apoptotic Proteins by Antisense Oligonucleotides
Current Drug Targets