Abstract
Background: Chemotherapy still encounters a serious drawback, the lack of selectivity of anticancer drugs toward neoplastic cells, thus, the normal cells are affected by the cytotoxic action of the drugs. This causes a narrow therapeutic index in most anticancer drugs.
Objective: We describe the preparation of pullulan-tocopherol succinate-folic acid (Pu-TS-FA) micelles for the first time to targeted delivery of Epirubicin (EPI) to Hela and MCF-7 cell lines.
Methods: We confirmed the structure of conjugate using spectroscopic methods. The degree of substitution for both folic acid and tocopherol succinate was calculated using 1HNMR. We prepared the micelles via direct dissolution method. All the physicochemical properties of micelles including size, zeta potential, polydispersity index (PDI), critical micelle concentration (CMC), entrapment efficiency (EE %) and release efficiency (RE24%) were determined. The morphology of particles was studied using transmission electron microscopy (TEM), and the in-vitro cell cytotoxicity of EPI loaded micelles was studied using MTT assay on MCF-7 and Hela cell lines.
Results: The optimized micelles showed the particle size of 149.5 nm, the zeta potential of -6.49 mV, a polydispersity index of 0.259 ± 0.07, LE% of 88 %, and RE24% of 63 ± 2.45 % with a relatively low CMC 194.87 µg/ml. TEM showed the relatively uniform spherical structure for particles and in vitro MTT assay showed that EPI loaded micelles were more toxic on Hela cell line than MCF7 as expected.
Conclusion: Since the Pu-TS-FA micelle could improve the anticancer activity of epirubicin and would be a promising candidate for EPI treatment of cancers.
Keywords: Pullulan, polymeric micelles, targeted drug delivery, folic acid, -tocopherol succinate, epirubicin (EPI).
Current Drug Delivery
Title:Folic acid Targeted Polymeric Micelles Based on Tocopherol Succinate- Pulluan as an Effective Carrier for Epirubicin: Preparation, Characterization and In-vitro Cytotoxicity Assessment
Volume: 15 Issue: 2
Author(s): Farshid Hassanzadeh, Mozhdeh Mehdifar, Jaleh Varshosaz, Ghadam Ali Khodarahmi and Mahboubeh Rostami*
Affiliation:
- Novel Drug Delivery Systems Research Centre and Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan,Iran
Keywords: Pullulan, polymeric micelles, targeted drug delivery, folic acid, -tocopherol succinate, epirubicin (EPI).
Abstract: Background: Chemotherapy still encounters a serious drawback, the lack of selectivity of anticancer drugs toward neoplastic cells, thus, the normal cells are affected by the cytotoxic action of the drugs. This causes a narrow therapeutic index in most anticancer drugs.
Objective: We describe the preparation of pullulan-tocopherol succinate-folic acid (Pu-TS-FA) micelles for the first time to targeted delivery of Epirubicin (EPI) to Hela and MCF-7 cell lines.
Methods: We confirmed the structure of conjugate using spectroscopic methods. The degree of substitution for both folic acid and tocopherol succinate was calculated using 1HNMR. We prepared the micelles via direct dissolution method. All the physicochemical properties of micelles including size, zeta potential, polydispersity index (PDI), critical micelle concentration (CMC), entrapment efficiency (EE %) and release efficiency (RE24%) were determined. The morphology of particles was studied using transmission electron microscopy (TEM), and the in-vitro cell cytotoxicity of EPI loaded micelles was studied using MTT assay on MCF-7 and Hela cell lines.
Results: The optimized micelles showed the particle size of 149.5 nm, the zeta potential of -6.49 mV, a polydispersity index of 0.259 ± 0.07, LE% of 88 %, and RE24% of 63 ± 2.45 % with a relatively low CMC 194.87 µg/ml. TEM showed the relatively uniform spherical structure for particles and in vitro MTT assay showed that EPI loaded micelles were more toxic on Hela cell line than MCF7 as expected.
Conclusion: Since the Pu-TS-FA micelle could improve the anticancer activity of epirubicin and would be a promising candidate for EPI treatment of cancers.
Export Options
About this article
Cite this article as:
Hassanzadeh Farshid , Mehdifar Mozhdeh, Varshosaz Jaleh , Khodarahmi Ali Ghadam and Rostami Mahboubeh*, Folic acid Targeted Polymeric Micelles Based on Tocopherol Succinate- Pulluan as an Effective Carrier for Epirubicin: Preparation, Characterization and In-vitro Cytotoxicity Assessment, Current Drug Delivery 2018; 15 (2) . https://dx.doi.org/10.2174/1567201814666170602074149
DOI https://dx.doi.org/10.2174/1567201814666170602074149 |
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
-
Ganoderma lucidum: A Potential for Biotechnological Production of Anti-Cancer and Immunomodulatory Drugs
Recent Patents on Anti-Cancer Drug Discovery Emerging Roles for Modulation of microRNA Signatures in Cancer Chemoprevention
Current Cancer Drug Targets Alpha-Terpineol as Antitumor Candidate in Pre-Clinical Studies
Anti-Cancer Agents in Medicinal Chemistry Relaxin Receptors - New Drug Targets for Multiple Disease States
Current Drug Targets Antiinflammatory Activity of Melatonin in Central Nervous System
Current Neuropharmacology Pathology Associated Memory Deficits in Swedish Mutant Genome-Based Amyloid Precursor Protein Transgenic Mice
Current Aging Science Sphingolipid Metabolism and Drug Resistance in Hematological Malignancies
Anti-Cancer Agents in Medicinal Chemistry Natural Antibodies: Protecting Role of IgM in Glioblastoma and Brain Tumours
Current Pharmaceutical Design Pro-apoptotic Activity of BH3-only Proteins and BH3 Mimetics: from Theory to Potential Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Targeting Hsp90 in Non-Cancerous Maladies
Current Topics in Medicinal Chemistry Peptide Nucleic Acids with a Structurally Biased Backbone: Effects of Conformational Constraints and Stereochemistry
Current Topics in Medicinal Chemistry How to Manage the Infectious Risk under Anti-TNF in Inflammatory Bowel Disease
Current Drug Targets Targeting Protein Degradation in Cancer Treatment
Current Chemical Biology Polymer Membrane and Cell Models for Drug Discovery
Combinatorial Chemistry & High Throughput Screening Some Wild-Growing Plant Species from Serbia and Montenegro as the Potential Sources of Drugs
Current Pharmaceutical Design Radiosensitizing Potential of Epigenetic Anticancer Drugs
Anti-Cancer Agents in Medicinal Chemistry Novel Checkpoint 1 Inhibitors
Recent Patents on Anti-Cancer Drug Discovery Anti-Proliferative, Anti-Inflammatory, Anti-Ulcerogenic and Wound Healing Properties of Chitosan
Current Bioactive Compounds Overview of Base Excision Repair Biochemistry
Current Molecular Pharmacology The Ubiquitin-Proteasome System (UPS) and the Mechanism of Action of Bortezomib
Current Pharmaceutical Design