Abstract
Solid lipid nanoparticles (SLNs) loaded with Cyclosporine A using glyceryl monostearate (GMS) and glyceryl palmitostearate (GPS) as lipid matrices were prepared by melt-homogenization using high-pressure homogenizer. Various process parameters such as homogenization pressure, homogenization cycles and formulation parameters such as ratio of drug: lipid, emulsifier: lipid and emulsifier: co-emulsifier were optimized using particle size and entrapment efficiencies as the dependent variables. The mean particle size of optimized batches of the GMS SLN and GPS SLN were found to be 131 nm and 158 nm and their entrapment efficiencies were 83 ± 3.08% and 97 ± 2.59% respectively. To improve the handling processing and stability of the prepared SLNs, the SLN dispersions were spray dried and its effect on size and reconstitution parameters were evaluated. The spray drying of SLNs did not significantly alter the size of SLNs and they exhibited good redispersibility. Solid state studies such as Infra Red Spectroscopy and Differential Scanning Calorimetry indicated absence of any chemical interaction between Cyclosporine A and the lipids. Scanning Electron Microscopy of optimized formulations showed spherical shape with smooth and non porous surface. In vitro release studies revealed that GMS based SLNs released the drug faster (41.12% in 20 hours) than GPS SLNs (7.958% in 20 hours). Release of Cyclosporine A from GMS SLN followed Higuchi equation better than first order while release from GPS SLN followed first order better than Higuchi model.
Keywords: Solid lipid nanoparticles, glyceryl monostearate, glyceryl palmitostearate, cyclosporine A, formulation, optimization, infra-red, DSC, In vitro release study
Current Drug Delivery
Title: Cyclosporine A Loaded Solid Lipid Nanoparticles: Optimization of Formulation, Process Variable and Characterization
Volume: 5 Issue: 1
Author(s): Krutika K. Sawant, Jigisha K. Varia and Shamsunder S. Dodiya
Affiliation:
Keywords: Solid lipid nanoparticles, glyceryl monostearate, glyceryl palmitostearate, cyclosporine A, formulation, optimization, infra-red, DSC, In vitro release study
Abstract: Solid lipid nanoparticles (SLNs) loaded with Cyclosporine A using glyceryl monostearate (GMS) and glyceryl palmitostearate (GPS) as lipid matrices were prepared by melt-homogenization using high-pressure homogenizer. Various process parameters such as homogenization pressure, homogenization cycles and formulation parameters such as ratio of drug: lipid, emulsifier: lipid and emulsifier: co-emulsifier were optimized using particle size and entrapment efficiencies as the dependent variables. The mean particle size of optimized batches of the GMS SLN and GPS SLN were found to be 131 nm and 158 nm and their entrapment efficiencies were 83 ± 3.08% and 97 ± 2.59% respectively. To improve the handling processing and stability of the prepared SLNs, the SLN dispersions were spray dried and its effect on size and reconstitution parameters were evaluated. The spray drying of SLNs did not significantly alter the size of SLNs and they exhibited good redispersibility. Solid state studies such as Infra Red Spectroscopy and Differential Scanning Calorimetry indicated absence of any chemical interaction between Cyclosporine A and the lipids. Scanning Electron Microscopy of optimized formulations showed spherical shape with smooth and non porous surface. In vitro release studies revealed that GMS based SLNs released the drug faster (41.12% in 20 hours) than GPS SLNs (7.958% in 20 hours). Release of Cyclosporine A from GMS SLN followed Higuchi equation better than first order while release from GPS SLN followed first order better than Higuchi model.
Export Options
About this article
Cite this article as:
Sawant K. Krutika, Varia K. Jigisha and Dodiya S. Shamsunder, Cyclosporine A Loaded Solid Lipid Nanoparticles: Optimization of Formulation, Process Variable and Characterization, Current Drug Delivery 2008; 5 (1) . https://dx.doi.org/10.2174/156720108783331069
DOI https://dx.doi.org/10.2174/156720108783331069 |
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
-
Potential Application of Network Descriptions for Understanding Conformational Changes and Protonation States of ABC Transporters
Current Pharmaceutical Design Statins: Are They All the Same?
Current Drug Therapy Neuroinflammation and the Immune-Kynurenine Pathway in Anxiety Disorders
Current Neuropharmacology Drug-Induced Hypothermia in Stroke Models: Does it Always Protect?
CNS & Neurological Disorders - Drug Targets Class IV Antiarrhythmic Agents: New Compounds Using an Old Strategy
Current Pharmaceutical Design Immunological Targets in Inflammation from the Small Molecule Perspective
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Heme Oxygenase-1 Dysregulation in the Brain: Implications for HIVAssociated Neurocognitive Disorders
Current HIV Research Inhibition of Early Upstream Events in Prodromal Alzheimer’s Disease by Use of Targeted Antioxidants
Current Aging Science Roles of Chemokine CXCL12 and its Receptors in Ischemic Stroke
Current Drug Targets On the Origin of Cortical Dopamine: Is it a Co-Transmitter in Noradrenergic Neurons?
Current Neuropharmacology Current Opinions and Perspectives on the Role of Immune System in the Pathogenesis of Parkinson's Disease
Current Pharmaceutical Design The Corticotropin-Releasing Factor (CRF) Family of Neuropeptides in Inflammation: Potential Therapeutic Applications
Current Medicinal Chemistry Computer-Aided Drug Design of Bioactive Natural Products
Current Topics in Medicinal Chemistry Relationship of Neurofilament Light (NfL) and Cognitive Performance in a Sample of Mexican Americans with Normal Cognition, Mild Cognitive Impairment and Dementia
Current Alzheimer Research Editorial [ Hot Topic: Drugs Targets in Parkinson's Disease:Where Are We and Where should We Go? (Guest Editor: Mark R. Cookson)]
CNS & Neurological Disorders - Drug Targets The Effects of PDE Inhibitors on Multiple Sclerosis: a Review of <i>in vitro</i> and <i>in vivo</i> Models
Current Pharmaceutical Design Do Histamine receptor 3 antagonists have a place in the therapy for schizophrenia?
Current Pharmaceutical Design Population Pharmacokinetics of Phenytoin Based on NONMEM in Patients with Intracranial Tumor During the First Week of Post-Craniotomy
Current Drug Metabolism Obstructive Sleep Apnea and Stroke
Current Respiratory Medicine Reviews Type 2 Diabetes and Risk for Functional Decline and Disability in Older Persons
Current Diabetes Reviews