Abstract
The purpose of this preliminary study was to investigate the physico-chemical properties of nimesulide precipitated by continuous supercritical antisolvent (SAS) from different organic solvents like acetone, chloroform and dichloromethane at 40°C and 80, 85 and 88 bar, respectively. Scanning electron microscopy, differential scanning calorimetry, X-Ray diffractometry and in vitro dissolution tests were employed to study how the technological process and the solvent nature would affect the final product. SAS-processed nimesulide particles showed dramatic morphological change in crystalline structure if compared to native nimesulide, resulting in needle and thin rods shaped crystals. The solid state analysis showed that using chloroform or dichloromethane as a solvent the drug solid state remained substantially unchanged, whilst if using acetone the applied method caused a transition from the starting form I to the meta-stable form II. So as to identify which process was responsible for this result, nimesulide was further precipitated from the same solvent by conventional evaporation method (RV-sample). On the basis of this comparison, the solvent was found to be responsible for the re-organization into the different polymorphic form and the potential of the SAS process to produce micronic needle shaped particles, with an enhanced dissolution rate if compared to the to the pure drug, was ascertained. Finally, the stability of the nimesulide form II, checked by DSC analysis, was ruled on over a period of 15 months.
Keywords: Supercritical antisolvent technique, nimesulide, polymorphism, stability studies
Current Drug Delivery
Title: Supercritical Antisolvent Precipitation of Nimesulide: Preliminary Experiments
Volume: 4 Issue: 3
Author(s): M. Moneghini, B. Perissutti, F. Vecchione, I. Kikic, P. Alessi, A. Cortesi and F. Princivalle
Affiliation:
Keywords: Supercritical antisolvent technique, nimesulide, polymorphism, stability studies
Abstract: The purpose of this preliminary study was to investigate the physico-chemical properties of nimesulide precipitated by continuous supercritical antisolvent (SAS) from different organic solvents like acetone, chloroform and dichloromethane at 40°C and 80, 85 and 88 bar, respectively. Scanning electron microscopy, differential scanning calorimetry, X-Ray diffractometry and in vitro dissolution tests were employed to study how the technological process and the solvent nature would affect the final product. SAS-processed nimesulide particles showed dramatic morphological change in crystalline structure if compared to native nimesulide, resulting in needle and thin rods shaped crystals. The solid state analysis showed that using chloroform or dichloromethane as a solvent the drug solid state remained substantially unchanged, whilst if using acetone the applied method caused a transition from the starting form I to the meta-stable form II. So as to identify which process was responsible for this result, nimesulide was further precipitated from the same solvent by conventional evaporation method (RV-sample). On the basis of this comparison, the solvent was found to be responsible for the re-organization into the different polymorphic form and the potential of the SAS process to produce micronic needle shaped particles, with an enhanced dissolution rate if compared to the to the pure drug, was ascertained. Finally, the stability of the nimesulide form II, checked by DSC analysis, was ruled on over a period of 15 months.
Export Options
About this article
Cite this article as:
M. Moneghini , B. Perissutti , F. Vecchione , I. Kikic , P. Alessi , A. Cortesi and F. Princivalle , Supercritical Antisolvent Precipitation of Nimesulide: Preliminary Experiments, Current Drug Delivery 2007; 4 (3) . https://dx.doi.org/10.2174/156720107781023901
DOI https://dx.doi.org/10.2174/156720107781023901 |
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
-
Vascular Damage in Obesity and Diabetes: Highlighting Links Between Endothelial Dysfunction and Metabolic Disease in Zebrafish and Man
Current Vascular Pharmacology Editorial: Exploring Lipid-related Treatment Options for the Treatment of NASH
Current Vascular Pharmacology Immune Deviation Strategies in the Therapy of Psoriasis
Current Drug Targets - Inflammation & Allergy Saint John on Patmos: Revelations of the Role of Antineutrophil Cytoplasmic Antibody (ANCA) in Vasculitis
Current Medicinal Chemistry Cytokines and Hormones in the Regulation of Hypoxia Inducible Factor-1α (HIF-1α)
Cardiovascular & Hematological Agents in Medicinal Chemistry EDITORIAL (Hot Topic: Beyond Reproductive Effects of Sex Steroids)
Mini-Reviews in Medicinal Chemistry Dendrimer Based Anti-Infective and Anti-Inflammatory Drugs
Recent Patents on Anti-Infective Drug Discovery Cortical Consequences of HIV-1 Tat Exposure in Rats are Enhanced by Chronic Cocaine
Current HIV Research Analgesics in Pregnancy: An Update on Use, Safety and Pharmacokinetic Changes in Drug Disposition
Current Pharmaceutical Design Glycolipid Antigen – Mediated Invariant NKT Cell Activation in Microbial Immunity
Current Immunology Reviews (Discontinued) Epidermal Stem Cells - Role in Normal, Wounded and Pathological Psoriatic and Cancer Skin
Current Stem Cell Research & Therapy Modification of Decoy Oligodeoxynucleotides to Achieve the Stability and Therapeutic Efficacy
Current Topics in Medicinal Chemistry Neurolological Disorders and Neuroprotection After Heart Surgery
Recent Patents on CNS Drug Discovery (Discontinued) Selective Acetyl- and Butyrylcholinesterase Inhibitors Reduce Amyloid-β Ex Vivo Activation of Peripheral Chemo-cytokines From Alzheimer's Disease Subjects: Exploring the Cholinergic Anti-inflammatory Pathway
Current Alzheimer Research Current Treatment Concepts of Philadelphia-Negative MPN
Current Cancer Drug Targets Protease-Activated Receptor 2: Are Common Functions in Glial and Immune Cells Linked to Inflammation-Related CNS Disorders?
Current Drug Targets Hematologic Abnormalities in the Antiphospholipid Syndrome
Current Rheumatology Reviews The Role of Vitamin D in the Pathogenesis of NOD Mouse Diabetes
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) A Review of Chinese Herbal Medicine for the Treatment of Chronic Heart Failure
Current Pharmaceutical Design Prostaglandin E<sub>2</sub> Receptor 4 (EP4): A Promising Therapeutic Target for the Treatment of Cancer and Inflammatory Diseases
Current Chemical Biology