Abstract
The present study was aimed at developing a sustained release formulation of Nimodipine (NIM) nanoparticles using the biodegradable polymers, poly (lactide-co-glycolide) (PLGA 50:50 and 85:15) as carrier. NIM is a widely used calcium channel blocker which has to be administered as an intravenous infusion for a prolonged period of 1-2 weeks in the treatment of cerebral vasospasm. A sustained release biodegradable formulation would serve to replace this conventional therapy of continuous intravenous administration. PLGA nanoparticles were prepared by a modified precipitation method using high pressure homogenizer at 10, 000 to 14,000 psi. A 32 factorial design was applied for optimization of the formulation parameters and for studying the effect of two independent variables [drug: polymer ratio and concentration of surfactant (Pluronic F 127)] on entrapment efficiency and mean particle size (response variables). Contour plots were plotted which gave a visual representation of the two variables on the dependent variables and also indicated nonlinear relationship between them. The nanoparticles had particle size of 131±1.9 nm for PLGA 50:50 and196±2.2 nm for PLGA 85:15. Scanning Electron Microscopy studies indicated that nanoparticles had spherical shape with a regular surface. The nanoparticles had high entrapment efficiency (96.42±2.09 % for PLGA 50:50 and 94.50±1.25 % for PLGA 85:15). DSC thermograms indicated that NIM was dispersed as an amorphous state in the nanoparticles. In vitro drug release from the lyophilized nanoparticles showed 94.35 ± 3.8 % NIM release from PLGA (50:50) nanoparticles and 63.32 ± 4.6 % release from PLGA (85:15) nanoparticles in 25 days. The release was first ordered and fickian diffusion kinetics in both the cases. These preliminary results indicate that NIM loaded PLGA nanoparticles could be effective in sustaining its release for a prolonged period. However, further studies are needed to confirm its performance in vivo.
Keywords: Nimodipine, PLGA, nanoparticles, 32 factorial design, sustained release
Current Drug Delivery
Title: Nimodipine Loaded PLGA Nanoparticles: Formulation Optimization Using Factorial Design,Characterization and In Vitro Evaluation
Volume: 4 Issue: 3
Author(s): Ashish K. Mehta, Khushwant S. Yadav and Krutika K. Sawant
Affiliation:
Keywords: Nimodipine, PLGA, nanoparticles, 32 factorial design, sustained release
Abstract: The present study was aimed at developing a sustained release formulation of Nimodipine (NIM) nanoparticles using the biodegradable polymers, poly (lactide-co-glycolide) (PLGA 50:50 and 85:15) as carrier. NIM is a widely used calcium channel blocker which has to be administered as an intravenous infusion for a prolonged period of 1-2 weeks in the treatment of cerebral vasospasm. A sustained release biodegradable formulation would serve to replace this conventional therapy of continuous intravenous administration. PLGA nanoparticles were prepared by a modified precipitation method using high pressure homogenizer at 10, 000 to 14,000 psi. A 32 factorial design was applied for optimization of the formulation parameters and for studying the effect of two independent variables [drug: polymer ratio and concentration of surfactant (Pluronic F 127)] on entrapment efficiency and mean particle size (response variables). Contour plots were plotted which gave a visual representation of the two variables on the dependent variables and also indicated nonlinear relationship between them. The nanoparticles had particle size of 131±1.9 nm for PLGA 50:50 and196±2.2 nm for PLGA 85:15. Scanning Electron Microscopy studies indicated that nanoparticles had spherical shape with a regular surface. The nanoparticles had high entrapment efficiency (96.42±2.09 % for PLGA 50:50 and 94.50±1.25 % for PLGA 85:15). DSC thermograms indicated that NIM was dispersed as an amorphous state in the nanoparticles. In vitro drug release from the lyophilized nanoparticles showed 94.35 ± 3.8 % NIM release from PLGA (50:50) nanoparticles and 63.32 ± 4.6 % release from PLGA (85:15) nanoparticles in 25 days. The release was first ordered and fickian diffusion kinetics in both the cases. These preliminary results indicate that NIM loaded PLGA nanoparticles could be effective in sustaining its release for a prolonged period. However, further studies are needed to confirm its performance in vivo.
Export Options
About this article
Cite this article as:
Ashish K. Mehta , Khushwant S. Yadav and Krutika K. Sawant , Nimodipine Loaded PLGA Nanoparticles: Formulation Optimization Using Factorial Design,Characterization and In Vitro Evaluation, Current Drug Delivery 2007; 4 (3) . https://dx.doi.org/10.2174/156720107781023929
DOI https://dx.doi.org/10.2174/156720107781023929 |
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
-
The Effect of Anti-B-cell Therapy on the Development of Atherosclerosis in Patients with Rheumatoid Arthritis
Current Pharmaceutical Design Nanocellulose and its Composites for Biomedical Applications
Current Medicinal Chemistry The Coronary Circulation in Cyanotic Congenital Heart Disease
Current Cardiology Reviews Progressive Brain Damage and Alterations in Dendritic Arborization after Collagenase-Induced Intracerebral Hemorrhage in Rats
Current Neurovascular Research Editorial [(Hot Topic Novel Drug Therapies in the Treatment of SAH) Guest Editors: Surya Karri and Christopher S. Ogilvy]
Current Drug Safety Pathology and Development - Developmental Systems for Target Validation and Drug Screening in Osteoarthritis
Drug Design Reviews - Online (Discontinued) The Yin and Yang of BK Channels in Epilepsy
CNS & Neurological Disorders - Drug Targets Cyclooxygenase-2 and Prostaglandin E2 are Associated with Middle Cerebral Artery Occlusion and Hemorrhage in Patients with Moyamoya Disease
Current Neurovascular Research Noninvasive Diagnosis of Chemotherapy Related Cardiotoxicity
Current Cardiology Reviews Biologic Agents in the Treatment of Psoriasis
Recent Patents on Inflammation & Allergy Drug Discovery Mast Cells: Pivotal Players in Cardiovascular Diseases
Current Cardiology Reviews Inflammatory Events Following Subarachnoid Hemorrhage (SAH)
Current Neuropharmacology Matrix Metalloproteinases in Vascular Disease - A Potential Therapeutic Target?
Current Vascular Pharmacology Mast Cell Chymase and Tryptase as Targets for Cardiovascular and Metabolic Diseases
Current Pharmaceutical Design Whole Milk and Full-Fat Dairy Products and Hypertensive Risks
Current Hypertension Reviews Therapeutic Value of Statins for Vascular Remodeling
Current Vascular Pharmacology The Potential of Hydrogen for Improving Mental Disorders
Current Pharmaceutical Design Meet Our Co-Editor
Cardiovascular & Hematological Agents in Medicinal Chemistry The Role of Venous Abnormalities in Neurological Disease
Reviews on Recent Clinical Trials Genetic Variability of Matrix Metalloproteinase Genes in Cardiovascular Disease
Current Topics in Medicinal Chemistry