Abstract
Objectives: This study aimed to develop and evaluate chitosan (CTS) solid dispersion particulate matrix (SDPM) for sustained oral delivery of ketorolac tromethamine (KT). Methods: SDPM formulations were prepared by freeze drying method and characterized for their effectiveness and biological activities via in vitro and in vivo assessment. Key findings: Powder’s flowability and bioadhesion of SDPM increased compared to KT-CTS physical mixtures and the raw materials. DSC analysis proved that the extent of drug crystallinity in matrix particles reduced as the amount of CTS content increased. FT-IR spectroscopy suggested drug-polymer interaction that was prominent in SDPM (1:7). In vitro drug release and simulated plasma profiles showed the superiority of SDPM (1:7) in sustaining drug release up to 12h. The optimized formula was stable during the storage time whereas the similarity factor (f2) for in vitro release data before and at the end of the study was 92%. Furthermore, in vivo bioactivity studies confirmed that the ulcerogenic property of SDPM (1:7) remarkably decreased compared to the standard drug while the analgesic and anti-inflammatory properties were maintained. Conclusion: Results suggested freeze-dried chitosan based SDPM (1:7) as a potential candidate for sustained oral administration of KT.
Keywords: Bioadhesion, Chitosan, Convolution, Freeze-drying, Ketorolac tromethamine, Solid dispersion.
Current Drug Delivery
Title:Development and Evaluation of Sustained Oral Ketorolac Tromethamine Particulate Matrix via Bioadhesive Chitosan Based Freeze-Dried Solid Dispersions
Volume: 13 Issue: 2
Author(s): Bazigha K. Abdul Rasool, Uday Sajad Aziz, Eman Abu-Gharbieh and Saeed A. Khan
Affiliation:
Keywords: Bioadhesion, Chitosan, Convolution, Freeze-drying, Ketorolac tromethamine, Solid dispersion.
Abstract: Objectives: This study aimed to develop and evaluate chitosan (CTS) solid dispersion particulate matrix (SDPM) for sustained oral delivery of ketorolac tromethamine (KT). Methods: SDPM formulations were prepared by freeze drying method and characterized for their effectiveness and biological activities via in vitro and in vivo assessment. Key findings: Powder’s flowability and bioadhesion of SDPM increased compared to KT-CTS physical mixtures and the raw materials. DSC analysis proved that the extent of drug crystallinity in matrix particles reduced as the amount of CTS content increased. FT-IR spectroscopy suggested drug-polymer interaction that was prominent in SDPM (1:7). In vitro drug release and simulated plasma profiles showed the superiority of SDPM (1:7) in sustaining drug release up to 12h. The optimized formula was stable during the storage time whereas the similarity factor (f2) for in vitro release data before and at the end of the study was 92%. Furthermore, in vivo bioactivity studies confirmed that the ulcerogenic property of SDPM (1:7) remarkably decreased compared to the standard drug while the analgesic and anti-inflammatory properties were maintained. Conclusion: Results suggested freeze-dried chitosan based SDPM (1:7) as a potential candidate for sustained oral administration of KT.
Export Options
About this article
Cite this article as:
K. Abdul Rasool Bazigha, Sajad Aziz Uday, Abu-Gharbieh Eman and A. Khan Saeed, Development and Evaluation of Sustained Oral Ketorolac Tromethamine Particulate Matrix via Bioadhesive Chitosan Based Freeze-Dried Solid Dispersions, Current Drug Delivery 2016; 13 (2) . https://dx.doi.org/10.2174/1567201812666151012114006
DOI https://dx.doi.org/10.2174/1567201812666151012114006 |
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
-
Investigation of Cytotoxic Effects of Oxymetazoline on Lungs in a Rat Model of Rhinitis Medicamentosa
Current Molecular Pharmacology The Airway Neurogenic Inflammation: Clinical and Pharmacological Implications
Inflammation & Allergy - Drug Targets (Discontinued) Air Pollution Exposure and Blood Pressure: An Updated Review of the Literature
Current Pharmaceutical Design Antidiabetic Effect of Spearmint in Streptozotocin-Induced Diabetic Rats
Endocrine, Metabolic & Immune Disorders - Drug Targets Pharmacological Management of No Reflow During Percutaneous Coronary Intervention
Current Vascular Pharmacology Brain Perfusion In Sepsis
Current Vascular Pharmacology Metabolic Effects of Renal Denervation
Current Clinical Pharmacology Recurrent Gastrointestinal Bleeding in a Patient with Eisenmenger Syndrome Using Bosentan
Current Drug Safety TRPV1: On the Road to Pain Relief
Current Molecular Pharmacology Acute and Long-Term Effects of Cannabis Use: A Review
Current Pharmaceutical Design Role of Adiponectin in Obesity, Hypertension, and Metabolic Syndrome
Current Hypertension Reviews Role of Ischemic Blood-Brain Barrier on Amyloid Plaques Development in Alzheimers Disease Brain
Current Neurovascular Research Endothelial Function and Pathogenesis of Endothelial Dysfunction
Current Immunology Reviews (Discontinued) 19F: A Versatile Reporter for Non-Invasive Physiology and Pharmacology Using Magnetic Resonance
Current Medicinal Chemistry Imaging Subclinical Atherosclerosis: Where Do We Stand?
Current Cardiology Reviews L-Arginine in the Prevention and Treatment of Cardiovascular Disease: From Basic to Clinical Research Studies
Vascular Disease Prevention (Discontinued) Oxidative Stress Induced Mitochondrial DNA Deletion as a Hallmark forthe Drug Development in the Context of the Cerebrovascular Diseases
Recent Patents on Cardiovascular Drug Discovery Lack of Evidence for Deterioration in Endothelial Function Following Ticagrelor Treatment Cessation
Current Vascular Pharmacology Current Pharmacological Approach to Restore Endothelial Dysfunction
Cardiovascular & Hematological Agents in Medicinal Chemistry Recent Patents on Emerging Therapeutics for the Treatment of Glaucoma, Age Related Macular Degeneration and Uveitis
Recent Patents on Biomedical Engineering (Discontinued)