Abstract
We here report the successful utilization of estrogen receptor (ER) for the delivery of anticancer drug doxorubicin (DOX) encapsulated within pegylated liposome for the treatment of breast cancer. Estrone (ES) was anchored as ligand on to stealth liposome (ES-SL-DOX) for targeting to ERs. In vitro cytotoxicity study was conducted on ER positive and negative breast carcinoma cells. The fluorescent microscopy studies were performed with estrone anchored stealth liposome (ES-SL) loaded with 6-carboxyfluorescein (6-CF). Pharmacokinetic, tissue distribution studies and tumor growth inhibition were carried out followed by intravenous (i.v.) administration of liposomal formulations. ES-SL-DOX demonstrated strongest cytotoxicity to the ER positive cell lines as compared to non-targeted formulations i.e. SL-DOX and plain DOX confirming that ES-SL-DOX was effectively taken up by cells expressing ERs. The half-life (t1/2) of SLDOX and ES-SL-DOX was about 9 and 13 fold higher than that of the free DOX, respectively. Accumulation of ES-SLDOX in the tumor tissue was 24.27 and 6.04 times higher as compared to free DOX and SL-DOX respectively, after 8 h. ES-SL-DOX at a dose of 5 mg DOX/kg resulted in effective retardation of tumor growth. These findings support that estrogen receptor(s) may be utilized as potential target for chemotherapy of cancers and estrone anchored stealth liposomes could be one of the promising solutions for the delivery of anticancer agent to breast tumors with reduced side-effects.
Keywords: Estrone, doxorubicin, breast cancer, targeting, stealth liposomes
Current Cancer Drug Targets
Title: A Novel Cancer Targeting Approach Based on Estrone Anchored Stealth Liposome for Site-Specific Breast Cancer Therapy
Volume: 10 Issue: 3
Author(s): S.R. Paliwal, R. Paliwal, N. Mishra, A. Mehta and S.P. Vyas
Affiliation:
Keywords: Estrone, doxorubicin, breast cancer, targeting, stealth liposomes
Abstract: We here report the successful utilization of estrogen receptor (ER) for the delivery of anticancer drug doxorubicin (DOX) encapsulated within pegylated liposome for the treatment of breast cancer. Estrone (ES) was anchored as ligand on to stealth liposome (ES-SL-DOX) for targeting to ERs. In vitro cytotoxicity study was conducted on ER positive and negative breast carcinoma cells. The fluorescent microscopy studies were performed with estrone anchored stealth liposome (ES-SL) loaded with 6-carboxyfluorescein (6-CF). Pharmacokinetic, tissue distribution studies and tumor growth inhibition were carried out followed by intravenous (i.v.) administration of liposomal formulations. ES-SL-DOX demonstrated strongest cytotoxicity to the ER positive cell lines as compared to non-targeted formulations i.e. SL-DOX and plain DOX confirming that ES-SL-DOX was effectively taken up by cells expressing ERs. The half-life (t1/2) of SLDOX and ES-SL-DOX was about 9 and 13 fold higher than that of the free DOX, respectively. Accumulation of ES-SLDOX in the tumor tissue was 24.27 and 6.04 times higher as compared to free DOX and SL-DOX respectively, after 8 h. ES-SL-DOX at a dose of 5 mg DOX/kg resulted in effective retardation of tumor growth. These findings support that estrogen receptor(s) may be utilized as potential target for chemotherapy of cancers and estrone anchored stealth liposomes could be one of the promising solutions for the delivery of anticancer agent to breast tumors with reduced side-effects.
Export Options
About this article
Cite this article as:
Paliwal S.R., Paliwal R., Mishra N., Mehta A. and Vyas S.P., A Novel Cancer Targeting Approach Based on Estrone Anchored Stealth Liposome for Site-Specific Breast Cancer Therapy, Current Cancer Drug Targets 2010; 10 (3) . https://dx.doi.org/10.2174/156800910791190210
DOI https://dx.doi.org/10.2174/156800910791190210 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
-
Genetics and Bioenergetics of Mitochondria Influencing the Etiology and Pharmacology of Steroidal Hormones
Current Pharmacogenomics New Trends and Advances in Oral and Maxillofacial Imaging
Current Medical Imaging Patent Selections
Recent Patents on Nanomedicine Antioxidant Supplementation on Cancer Risk and During Cancer Therapy: An Update
Current Topics in Medicinal Chemistry Acid-extrusion from Tissue: The Interplay Between Membrane Transporters and pH Buffers
Current Pharmaceutical Design PET Radioligands for In Vivo Visualization of Neuroinflammation
Current Pharmaceutical Design Recent Progress in Discovery and Development of Antimitotic Agents
Anti-Cancer Agents in Medicinal Chemistry Non-invasive Biodiversified Sensors: A Modernized Screening Technology for Cancer
Current Pharmaceutical Design Pharmacologic Evidence of Green Tea in Targeting Tyrosine Kinases
Current Reviews in Clinical and Experimental Pharmacology Signal Transduction by the Cytoplasmic Domain of NEUREGULIN-1 and its Roles During Neuronal Aging
Current Signal Transduction Therapy New Insights into Neoangiogenesis and Breast Cancer Development and Progression
Current Angiogenesis (Discontinued) Role of CHK2 Inhibitors in the Cellular Responses to Ionizing Radiation
Mini-Reviews in Medicinal Chemistry Use of Anti-Infective Drugs in Rheumatology
Anti-Infective Agents in Medicinal Chemistry Neuropeptide Y Induces Cardiomyocyte Hypertrophy <i>via</i> Attenuating miR-29a-3p in Neonatal Rat Cardiomyocytes
Protein & Peptide Letters Update on the Principles and Novel Local and Systemic Therapies for the Treatment of Non-Infectious Uveitis
Inflammation & Allergy - Drug Targets (Discontinued) The Pharmacogenomics “Side-effect” of TP53/EGFR in Non-small Cell Lung Cancer Accompanied with Atorvastatin Therapy: A Functional Network Analysis
Anti-Cancer Agents in Medicinal Chemistry Next Generation Tyrosine Kinase Inhibitor (TKI): Afatinib
Recent Patents on Anti-Cancer Drug Discovery Renin-angiotensin System Blockers and Modulation of Radiation-Induced Brain Injury
Current Drug Targets Nutritional Antioxidants and Adaptive Cell Responses: An Update
Current Molecular Medicine Pyrrolo[2,1-c][1,4]benzodiazepine as a Scaffold for the Design and Synthesis of Anti- Tumour Drugs
Anti-Cancer Agents in Medicinal Chemistry