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
-
Applications of Endobronchial Ultrasound-Guided Transbronchial Needle Aspiration (EBUS-TBNA) in Pulmonary Disease
Current Respiratory Medicine Reviews Small Molecule Toxins Targeting Tumor Receptors
Current Pharmaceutical Design Characterization of β-Sitosterol for Potential Selective GR Modulation
Protein & Peptide Letters Anticancer Properties of Flavonoids: Roles in Various Stages of Carcinogenesis
Cardiovascular & Hematological Agents in Medicinal Chemistry A Review of Fertility Preservation with Radical Vaginal Trachelectomy and Laparoscopic Pelvic Lymphadenectomy in the Treatment of Early Cervical Cancer
Current Women`s Health Reviews Combined Chemotherapy or Biotherapy with Jasmonates: Targeting Energy Metabolism for Cancer Treatment
Current Pharmaceutical Biotechnology Effects of Highly Active Antiretroviral Therapy on HIV-1-Associated Oral Complications
Current HIV Research Clinical, Molecular- and Cytogenetic Analysis of a Case of Severe Radio- Sensitivity
Current Genomics Spermine Metabolism and Anticancer Therapy
Current Cancer Drug Targets Antioxidant Effects and in vitro Cytotoxicity on Human Cancer Cell Lines of Flavonoid-Rich Flamboyant (<i>Delonix regia</i> (Bojer) Raf.) Flower Extract
Current Pharmaceutical Biotechnology HPV Cervical Infection and Immunodysregulation: Synergistic Risks for Neoplasia-Review
Current Women`s Health Reviews Disordered Interactome of Human Papillomavirus
Current Pharmaceutical Design Microwave-Assisted Domino Cyclization Reactions
Current Microwave Chemistry Exploiting HPV-Induced Carcinogenesis for a Rational Drug Development in Cervical Cancer
Current Cancer Drug Targets Novel Derivatives of Benfluron and Dimefluron Synthesis and Anticancer activity
Letters in Drug Design & Discovery Anticancer Drugs Aimed at E6 and E7 Activity in HPV-Positive Cervical Cancer
Current Cancer Drug Targets From Bortezomib to other Inhibitors of the Proteasome and Beyond
Current Pharmaceutical Design Introduction: MMPs, ADAMs/ADAMTSs Research Products to Achieve Big Dream
Anti-Cancer Agents in Medicinal Chemistry Talazoparib Loaded Solid Lipid Nanoparticles: Preparation, Characterization and Evaluation of the Therapeutic Efficacy In vitro
Current Drug Delivery Anticancer Immunotherapy in Combination with Proapoptotic Therapy
Current Cancer Drug Targets