Abstract
(3-Chloro-7-methoxyfuro[2,3-b]-quinolin-4-yl)-(4-methoxyphenyl)amine (CYL), a chemotherapeutic agent, is an analogue of amsacrine. The water insolubility of CYL limits its delivery and thus its application. The aim of the study was to utilize solid lipid nanoparticles (SLNs) to improve the delivery of CYL, and investigate its biodistribution behavior in an animal model. Characterizations of SLNs were evaluated including the particle size, zeta potential and entrapment efficiency. An in vivo study was used to investigate the pharmacokinetics and biodistribution behaviors. We established a rapid and sensitive high-performance liquid chromatographic (HPLC) technique with electrochemical detection to determine CYL, and the limit of detection was 40 ng/ml. We found that particle sizes of CYL-loaded SLNs were about 25%~33% larger then empty SLNs. The entrapment efficiency (E%) of CYL embedded in the SLN matrix was about 80%~98%. Moreover, the E% of SLNs incorporating glyceryl monostearate (GMS) significantly increased by about 11%~17% and the polydispersity index dropped 0.3~0.39. An in vivo pharmacokinetics study of intravenous CYL displayed linear plasma pharmacokinetics and fit a two-compartment model. The biodistribution behavior demonstrated that CYL-loaded tristearin(TS)- GMS SLNs mainly accumulated in the heart, lungs, liver, pancreas, and kidneys.
Keywords: (3-chloro-7-methoxyfuro[2, 3-b]-quinolin-4-yl)-(4-methoxyphenyl)amine (CYL), biodistribution, glyceryl monostearate, highperformance liquid chromatography, pharmacokinetics, solid lipid nanoparticles (SLNs)
Current Nanoscience
Title:A New Antitumor Agent, (3-chloro-7-methoxyfuro[2,3-b]-quinolin-4-yl)-(4-methoxyphenyl) amine, Loaded in Solid Lipid Nanoparticles: Characterization and Pharmacokinetics
Volume: 8 Issue: 2
Author(s): Yi-Ping Fang, Pao-Chu Wu, Cherng-Chyi Tzeng, Yeh-Long Chen, Huei-Lan Lin and Yi-Hung Tsai
Affiliation:
Keywords: (3-chloro-7-methoxyfuro[2, 3-b]-quinolin-4-yl)-(4-methoxyphenyl)amine (CYL), biodistribution, glyceryl monostearate, highperformance liquid chromatography, pharmacokinetics, solid lipid nanoparticles (SLNs)
Abstract: (3-Chloro-7-methoxyfuro[2,3-b]-quinolin-4-yl)-(4-methoxyphenyl)amine (CYL), a chemotherapeutic agent, is an analogue of amsacrine. The water insolubility of CYL limits its delivery and thus its application. The aim of the study was to utilize solid lipid nanoparticles (SLNs) to improve the delivery of CYL, and investigate its biodistribution behavior in an animal model. Characterizations of SLNs were evaluated including the particle size, zeta potential and entrapment efficiency. An in vivo study was used to investigate the pharmacokinetics and biodistribution behaviors. We established a rapid and sensitive high-performance liquid chromatographic (HPLC) technique with electrochemical detection to determine CYL, and the limit of detection was 40 ng/ml. We found that particle sizes of CYL-loaded SLNs were about 25%~33% larger then empty SLNs. The entrapment efficiency (E%) of CYL embedded in the SLN matrix was about 80%~98%. Moreover, the E% of SLNs incorporating glyceryl monostearate (GMS) significantly increased by about 11%~17% and the polydispersity index dropped 0.3~0.39. An in vivo pharmacokinetics study of intravenous CYL displayed linear plasma pharmacokinetics and fit a two-compartment model. The biodistribution behavior demonstrated that CYL-loaded tristearin(TS)- GMS SLNs mainly accumulated in the heart, lungs, liver, pancreas, and kidneys.
Export Options
About this article
Cite this article as:
Fang Yi-Ping, Wu Pao-Chu, Tzeng Cherng-Chyi, Chen Yeh-Long, Lin Huei-Lan and Tsai Yi-Hung, A New Antitumor Agent, (3-chloro-7-methoxyfuro[2,3-b]-quinolin-4-yl)-(4-methoxyphenyl) amine, Loaded in Solid Lipid Nanoparticles: Characterization and Pharmacokinetics, Current Nanoscience 2012; 8 (2) . https://dx.doi.org/10.2174/157341312800167669
DOI https://dx.doi.org/10.2174/157341312800167669 |
Print ISSN 1573-4137 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6786 |
Call for Papers in Thematic Issues
Role of nanomaterials in fabrication of coatings, Machining and Joining
The application of nanoscience has brought about a revolution in the field of mechanical engineering by providing novel materials, boosting manufacturing processes, and generating cutting-edge products. The purpose of this special issue is to investigate the enormous impact that nanoscience has had on mechanical engineering, with a particular emphasis on ...read more
Advanced Inorganic Nanocomposites and Their Emerging Applications
This special issue collection will highlight developments on the recent trends about the synthesis of metal oxides, nanoclusters, biomaterials, 2D nanomaterials, nanocrystals, nanocomposites, etc. and their applications in electrochemical systems, tissue regeneration, energy storage and harvesting, sensors, etc. The novelty of the methods in the chemical synthesis and their characterizations, ...read more
Applicability of Nanotechnology for Performance Enhancement of Clean Energy Technologies
Population growth, industrialization, and improvement in living quality would lead to further increase in energy demand in near future. Regarding the disadvantages of fossil fuels such as fluctuations in their price, high emissions of greenhouse gases and restriction of their sources, it is crucial to use and exploit alternative energy ...read more
Graphene and 2D Materials for Energy Storage and Conversion
This thematic issue will discuss the recent advances in graphene-based nanomaterials for different energy technologies. Graphene possesses a high surface area, and stable structure and exhibits many interesting electronic, optical, and mechanical properties due to its 2D crystal structure. Graphene is of both fundamental interest and suitable for a wide ...read more
Related Journals
- 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
-
Patent Annotations
Recent Patents on Anti-Cancer Drug Discovery Development of Novel, Highly Cytotoxic Fusion Constructs Containing Granzyme B: Unique Mechanisms and Functions
Current Pharmaceutical Design Clinical Use of Rituximab in Patients with HIV Related Lymphoma and Multicentric Castlemans Disease
Current Drug Delivery Targeting CXCR4 in HIV Cell-Entry Inhibition.
Mini-Reviews in Medicinal Chemistry Drug Delivery Systems for Brain Tumor Therapy
Current Pharmaceutical Design Vascular Endothelial Growth Factor (VEGF) as a Target of Bevacizumab in Cancer: From the Biology to the Clinic
Current Medicinal Chemistry Metronomic Therapy for Multi Relapsed/Refractory Lymphoma. A Pilot Study
Current Angiogenesis (Discontinued) Hormone Responsive Breast Cancer and BRCA1 Mutation: Mechanism, Regulation and Iron-mediated Effects
Current Pharmaceutical Biotechnology Monoclonal Antobodies: Application in Radiopharmacy
Current Radiopharmaceuticals Targeted Tumor Therapies at a Glance
Current Drug Targets The Role of Major Histocompatibility Complex Polymorphisms in the Incidence and Outcome of Non-Hodgkin Lymphoma
Current Immunology Reviews (Discontinued) Recents Patents for Isolating, Delivering and Tracking Adult Stem Cells in Regenerative Medicine
Recent Patents on Drug Delivery & Formulation GnRH-Analogues for Ovarian Protection in Childhood Cancer Patients: How Adult Hypotheses are Relevant in Prepubertal Females
Current Drug Targets Clonetics
Current Drug Metabolism Recombinant Immunotoxins for the Treatment of Chemoresistant Hematologic Malignancies
Current Pharmaceutical Design Cervical Cancer During Pregnancy – An Approach to Diagnosis and Management
Current Women`s Health Reviews Tyrosine Kinases as Therapeutic Targets in BCR-ABL Negative Chronic Myeloproliferative Disorders
Current Drug Targets Second Generation Proteasome Inhibitors: Carfilzomib and Immunoproteasome-Specific Inhibitors (IPSIs)
Current Cancer Drug Targets Bugs and Drugs: Oncolytic Virotherapy in Combination with Chemotherapy
Current Pharmaceutical Biotechnology Marine Natural Products and Related Compounds as Anticancer Agents: an Overview of their Clinical Status
Anti-Cancer Agents in Medicinal Chemistry