Abstract
Solid dispersions of Fluvastatin with polyvinylpyrrolidone (PVP), eudragit RS100 (Eud), and chitosan (CS) as drug carrier matrices, were prepared using different techniques in order to evaluate their effect on Fluvastatin stability during storage. The characterization of the three different systems was performed with the use of differential scanning calorimetry (DSC) and wide angle X-ray diffractometry (WAXD). It was revealed that amorphization of the drug occurred in all of the solid dispersions of Fluvastatin as a result of drug dissolution into polymer matrices and due to physical interactions (hydrogen bonding) between the polymer matrix and Fluvastatin. This was established through the use of FTIR spectroscopy. SEM and micro-Raman spectroscopy showed that Fluvastatin was interspersed to the polymer matrices in the form of molecular dispersion and nanodispersion, too. The finding that completely different polymer matrices, used here as drug carriers, produce completely different dissolution profiles for each one of the solid dispersions, suggests that each matrix follows a different drug release mechanism. Hydrogen bonding interactions as in the case of CS/Fluva solid dispersions lead to controlled release profiles. All formulations were subjected to accelerated aging in order to evaluate Fluvastatin stability. From by-products analysis it was found that Fluvastatin is very unstable during storage and anti-isomer as well as lactones are the main formed by-products. On the other hand, solid dispersions due to the evolved interactions of their reactive groups with Fluvastatin provide a sufficient physical and chemical stability. The extent of interactions seems to play the most important role in the drug stabilization.
Keywords: Fluvastatin, solid dispersions, PVP, Chitosan, Eudragit, physical and chemical stability
Current Drug Delivery
Title: Improvement in Chemical and Physical Stability of Fluvastatin Drug Through Hydrogen Bonding Interactions with Different Polymer Matrices
Volume: 6 Issue: 1
Author(s): G. Z. Papageorgiou, S. Papadimitriou, E. Karavas, E. Georgarakis, A. Docoslis and D. Bikiaris
Affiliation:
Keywords: Fluvastatin, solid dispersions, PVP, Chitosan, Eudragit, physical and chemical stability
Abstract: Solid dispersions of Fluvastatin with polyvinylpyrrolidone (PVP), eudragit RS100 (Eud), and chitosan (CS) as drug carrier matrices, were prepared using different techniques in order to evaluate their effect on Fluvastatin stability during storage. The characterization of the three different systems was performed with the use of differential scanning calorimetry (DSC) and wide angle X-ray diffractometry (WAXD). It was revealed that amorphization of the drug occurred in all of the solid dispersions of Fluvastatin as a result of drug dissolution into polymer matrices and due to physical interactions (hydrogen bonding) between the polymer matrix and Fluvastatin. This was established through the use of FTIR spectroscopy. SEM and micro-Raman spectroscopy showed that Fluvastatin was interspersed to the polymer matrices in the form of molecular dispersion and nanodispersion, too. The finding that completely different polymer matrices, used here as drug carriers, produce completely different dissolution profiles for each one of the solid dispersions, suggests that each matrix follows a different drug release mechanism. Hydrogen bonding interactions as in the case of CS/Fluva solid dispersions lead to controlled release profiles. All formulations were subjected to accelerated aging in order to evaluate Fluvastatin stability. From by-products analysis it was found that Fluvastatin is very unstable during storage and anti-isomer as well as lactones are the main formed by-products. On the other hand, solid dispersions due to the evolved interactions of their reactive groups with Fluvastatin provide a sufficient physical and chemical stability. The extent of interactions seems to play the most important role in the drug stabilization.
Export Options
About this article
Cite this article as:
Papageorgiou Z. G., Papadimitriou S., Karavas E., Georgarakis E., Docoslis A. and Bikiaris D., Improvement in Chemical and Physical Stability of Fluvastatin Drug Through Hydrogen Bonding Interactions with Different Polymer Matrices, Current Drug Delivery 2009; 6 (1) . https://dx.doi.org/10.2174/156720109787048230
DOI https://dx.doi.org/10.2174/156720109787048230 |
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
-
Anti-dementia drugs-related changes in gait performance while single and dual tasking in patients with Alzheimer disease: a meta-analysis
Current Alzheimer Research Recent Updates on Development of Drug Molecules for Human African Trypanosomiasis
Current Topics in Medicinal Chemistry Cannabinoid System as a Potential Target for Drug Development in the Treatment of Cardiovascular Disease
Current Vascular Pharmacology Cerebrovascular Profile Assessment in Parkinson's Disease Patients
CNS & Neurological Disorders - Drug Targets Brain Targeted Drug Delivery: Factors, Approaches and Patents
Recent Patents on Nanomedicine Genetically-Modified Human Pluripotent Stem Cells: New Hopes for the Understanding and the Treatment of Neurological Diseases?
Current Gene Therapy Evaluation of the Effect of Nimodipine o.d. (Extended Release) vs Nimodipine t.i.d. in the Treatment of Peripheral Vertigo
Current Drug Delivery The Role and Impact of SNPs in Pharmacogenomics and Personalized Medicine
Current Drug Metabolism Cytokine-Purine Interactions in Traumatic Stress, Behavioral Depression,and Sickness
CNS & Neurological Disorders - Drug Targets Oleic Acid in Olive Oil: From a Metabolic Framework Toward a Clinical Perspective
Current Pharmaceutical Design Fibroblast Growth Factor-Inducible 14: Multiple Roles in Tumor Metastasis
Current Molecular Medicine Mucoadhesive Nanoparticulate System for Oral Drug Delivery: A Review
Current Drug Therapy E-Pharmacophore and Molecular Dynamics Study of Flavonols and Dihydroflavonols as Inhibitors Against DiHydroOrotate DeHydrogenase
Combinatorial Chemistry & High Throughput Screening A Review Focused on Molecular Mechanisms of Anxiolytic Effect of <i>Valerina officinalis</i> L. in Connection with Its Phytochemistry through <i>in vitro/in vivo</i> Studies
Current Pharmaceutical Design Heat Shock Proteins as Suppressors of Accumulation of Toxic Prefibrillar Intermediates and Misfolded Proteins in Neurodegenerative Diseases
Current Pharmaceutical Biotechnology Various Non-Injectable Delivery Systems for the Treatment of Diabetes Mellitus
Endocrine, Metabolic & Immune Disorders - Drug Targets Anti PD-1 and PDL-1 Immunotherapy in the Treatment of Advanced Non- Small Cell Lung Cancer (NSCLC): A Review on Toxicity Profile and its Management
Current Drug Safety Disease-Specific iPS Cell Models in Neuroscience
Current Molecular Medicine Nitric Oxide Modulation of the Basal Ganglia Circuitry: Therapeutic Implication for Parkinson's Disease and Other Motor Disorders
CNS & Neurological Disorders - Drug Targets Allosteric Regulators of the Proteasome: Potential Drugs and a Novel Approach for Drug Design
Current Medicinal Chemistry