Abstract
Introduction: Premise of the present study was to suitably select or modify the constitution of the lipid matrix to achieve significantly high entrapment of hydrophilic drugs within solid lipid nanoparticles (SLNs). Methods and Materials: Isoniazid was selected as a representative hydrophilic drug with a high solubility of 230 mg/ml and a log P of -0.402 at 25°C (determined as per OECD TG 105 and 107 respectively). Three lipids/fatty acids (Glyceryl monostearate, Compritol 888 ATO® and stearic acid) were evaluated out of which Compritol 888 ATO® and stearic acid showed favorable interactions (FTIR and DSC studies) with isoniazid. The two lipids were used alone or in combination for preparing SLNs. Formulation of SLNs by microemulsification, method involved pouring the hot microemulsion into cold water under constant stirring, which may result in expulsion of the hydrophilic drug from the lipid matrix; hence, partitioning of isoniazid from the hot lipid melts into cold water was also determined. Results and Discussion: Results indicate that combining stearic acid with Compritol 888 ATO® in certain ratio (1:4) led to significant entrapment efficiency (EE) of 84.0±1.1%. The formulations were subjected to morphological, physiochemical and in vitro drug release studies. Developed SLNs were found to be stable for 1 year at 4 °C. Conclusion: The study demonstrates the benefit of excipient screening techniques in improving entrapment efficiency of a hydrophilic drug.
Keywords: Solid lipid nanoparticle, isoniazid, entrapment efficiency, lipid combination, excipient selection.
Current Nanoscience
Title:A Method to Prepare Solid Lipid Nanoparticles with Improved Entrapment Efficiency of Hydrophilic Drugs
Volume: 9 Issue: 2
Author(s): Bhandari Rohit and Kaur Indu Pal
Affiliation:
Keywords: Solid lipid nanoparticle, isoniazid, entrapment efficiency, lipid combination, excipient selection.
Abstract: Introduction: Premise of the present study was to suitably select or modify the constitution of the lipid matrix to achieve significantly high entrapment of hydrophilic drugs within solid lipid nanoparticles (SLNs). Methods and Materials: Isoniazid was selected as a representative hydrophilic drug with a high solubility of 230 mg/ml and a log P of -0.402 at 25°C (determined as per OECD TG 105 and 107 respectively). Three lipids/fatty acids (Glyceryl monostearate, Compritol 888 ATO® and stearic acid) were evaluated out of which Compritol 888 ATO® and stearic acid showed favorable interactions (FTIR and DSC studies) with isoniazid. The two lipids were used alone or in combination for preparing SLNs. Formulation of SLNs by microemulsification, method involved pouring the hot microemulsion into cold water under constant stirring, which may result in expulsion of the hydrophilic drug from the lipid matrix; hence, partitioning of isoniazid from the hot lipid melts into cold water was also determined. Results and Discussion: Results indicate that combining stearic acid with Compritol 888 ATO® in certain ratio (1:4) led to significant entrapment efficiency (EE) of 84.0±1.1%. The formulations were subjected to morphological, physiochemical and in vitro drug release studies. Developed SLNs were found to be stable for 1 year at 4 °C. Conclusion: The study demonstrates the benefit of excipient screening techniques in improving entrapment efficiency of a hydrophilic drug.
Export Options
About this article
Cite this article as:
Rohit Bhandari and Pal Kaur Indu, A Method to Prepare Solid Lipid Nanoparticles with Improved Entrapment Efficiency of Hydrophilic Drugs, Current Nanoscience 2013; 9 (2) . https://dx.doi.org/10.2174/1573413711309020008
DOI https://dx.doi.org/10.2174/1573413711309020008 |
Print ISSN 1573-4137 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6786 |
Call for Papers in Thematic Issues
Role of nanomaterials in fabrication of coatings, Machining and Joining
The application of nanoscience has brought about a revolution in the field of mechanical engineering by providing novel materials, boosting manufacturing processes, and generating cutting-edge products. The purpose of this special issue is to investigate the enormous impact that nanoscience has had on mechanical engineering, with a particular emphasis on ...read more
Advanced Inorganic Nanocomposites and Their Emerging Applications
This special issue collection will highlight developments on the recent trends about the synthesis of metal oxides, nanoclusters, biomaterials, 2D nanomaterials, nanocrystals, nanocomposites, etc. and their applications in electrochemical systems, tissue regeneration, energy storage and harvesting, sensors, etc. The novelty of the methods in the chemical synthesis and their characterizations, ...read more
Applicability of Nanotechnology for Performance Enhancement of Clean Energy Technologies
Population growth, industrialization, and improvement in living quality would lead to further increase in energy demand in near future. Regarding the disadvantages of fossil fuels such as fluctuations in their price, high emissions of greenhouse gases and restriction of their sources, it is crucial to use and exploit alternative energy ...read more
Graphene and 2D Materials for Energy Storage and Conversion
This thematic issue will discuss the recent advances in graphene-based nanomaterials for different energy technologies. Graphene possesses a high surface area, and stable structure and exhibits many interesting electronic, optical, and mechanical properties due to its 2D crystal structure. Graphene is of both fundamental interest and suitable for a wide ...read more
Related Journals
- 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
-
Adenovirus Mediated Herpes Simplex Virus-Thymidine Kinase/Ganciclovir Gene Therapy for Resectable Malignant Glioma
Current Gene Therapy Calcium Antagonists: A Ready Prescription for Treating Infectious Diseases?
Current Topics in Medicinal Chemistry Experimental Methods and Transport Models for Drug Delivery Across the Blood-Brain Barrier
Current Pharmaceutical Biotechnology Antifungal Proteins: Potent Candidate for Inhibition of Pathogenic Fungi
Current Bioactive Compounds Nanoformulated Antibiotics: the Next Step for Pathogenic Bacteria Control
Current Medicinal Chemistry Transforming Growth Factor-β Signaling in Motor Neuron Diseases
Current Molecular Medicine Defining and Regulating Acute Inflammatory Lesion Formation during the Pathogenesis of Multiple Sclerosis and Experimental Autoimmune Encephalomyelitis
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 Natural Product-Based Phenolic and Nonphenolic Antimicrobial Food Preservatives and 1,2,3,4-Tetrahydroxybenzene as a Highly Effective Representative: A Review of Patent Literature 2000-2005
Recent Patents on Anti-Infective Drug Discovery Antibodies as Anti-Infective Agents in Medicinal Chemistry
Anti-Infective Agents in Medicinal Chemistry AIDS-Defining Illnesses: A Comparison Between Before and After Commencement of Highly Active Antiretroviral Therapy (HAART)
Current HIV Research When to Start Antiretroviral Therapy in HIV-Associated Tuberculosis
Current Respiratory Medicine Reviews Recent Developments on Endothelin Antagonists as Immunomodulatory Drugs - from Infection to Transplantation Medicine
Recent Patents on Cardiovascular Drug Discovery Acanthamoeba-Bacteria: A Model to Study Host Interaction with Human Pathogens
Current Drug Targets MRI in Normal Myelination: A Pictorial Review
Current Pediatric Reviews Inflammatory Mediators as Potential Therapeutic Targets in the Spine
Current Drug Targets - Inflammation & Allergy Modulation of the Human Gut Microflora Towards Improved Health Using Prebiotics - Assessment of Efficacy
Current Pharmaceutical Design Inflammatory Events Following Subarachnoid Hemorrhage (SAH)
Current Neuropharmacology Eph/ephrin Signaling as a Potential Therapeutic Target After Central Nervous System Injury
Current Pharmaceutical Design Intranasal Fluorescent Nanocrystals for Longitudinal <i>In Vivo</i> Evaluation of Cerebral Microlesions
Pharmaceutical Nanotechnology