Abstract
Present research investigates the formulation of stavudine loaded biodegradable microspheres from different grades of Poly (D, L Lactide-co-glycolide) as a depot system for parenteral delivery. Prolonged release of stavudine facilitates reduction in symptoms of HIV infection and delay AIDS progression by reducing viral load to undetectable levels. Microspheres were prepared from PLGA 85:15 and PLGA 50:50 (RESOMER® 505H) by solvent evaporation technique with different drug/polymer ratios (1:4, 1:10, 1:20, 1:50, 1:100) and a polymer solution/vehicle ratio of 1:2. The effects of various formulation variables like polymer type and concentration, surfactant concentration and drug to polymer ratio on the characteristics of microspheres were evaluated. All the formulations of microspheres were evaluated for yield, entrapment efficiency, particle size and in vitro release studies. Microspheres were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), residual solvent analysis and confocal laser scanning microscopy (CLSM). Microspheres showed excellent surface topography with uniform distribution and structural integrity of the drug. Resulting microspheres showed the maximum entrapment efficiency of 68.0 ± 1.62% and mean particle diameter below 100μ. Drug release kinetics data were obtained from various kinetic models and can be explained both by “Higuchi Kinetic” and “Korsmeyer-Peppas equation”. These equations showed that release was due to diffusion and polymer relaxation. Drug release from microspheres exhibited the characteristic release pattern of a monolithic matrix system with a maximum of 80-90% drug release in 6-8 weeks demonstrating the feasibility of prolonged delivery of stavudine using biodegradable microspheres for parenteral depot system.
Keywords: AIDS, microspheres, biodegradable polymer, stavudine, poly (D, L Lactide-co-glycolide), prolonged release, parenteral delivery, salvage therapy, Korsmeyer-Peppas, Higuchi Kinetic
Current Drug Delivery
Title: Development and Evaluation of Stavudine Loaded Injectable Polymeric Particulate Systems
Volume: 8 Issue: 4
Author(s): Saurabh Srivastava and V. R. Sinha
Affiliation:
Keywords: AIDS, microspheres, biodegradable polymer, stavudine, poly (D, L Lactide-co-glycolide), prolonged release, parenteral delivery, salvage therapy, Korsmeyer-Peppas, Higuchi Kinetic
Abstract: Present research investigates the formulation of stavudine loaded biodegradable microspheres from different grades of Poly (D, L Lactide-co-glycolide) as a depot system for parenteral delivery. Prolonged release of stavudine facilitates reduction in symptoms of HIV infection and delay AIDS progression by reducing viral load to undetectable levels. Microspheres were prepared from PLGA 85:15 and PLGA 50:50 (RESOMER® 505H) by solvent evaporation technique with different drug/polymer ratios (1:4, 1:10, 1:20, 1:50, 1:100) and a polymer solution/vehicle ratio of 1:2. The effects of various formulation variables like polymer type and concentration, surfactant concentration and drug to polymer ratio on the characteristics of microspheres were evaluated. All the formulations of microspheres were evaluated for yield, entrapment efficiency, particle size and in vitro release studies. Microspheres were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), residual solvent analysis and confocal laser scanning microscopy (CLSM). Microspheres showed excellent surface topography with uniform distribution and structural integrity of the drug. Resulting microspheres showed the maximum entrapment efficiency of 68.0 ± 1.62% and mean particle diameter below 100μ. Drug release kinetics data were obtained from various kinetic models and can be explained both by “Higuchi Kinetic” and “Korsmeyer-Peppas equation”. These equations showed that release was due to diffusion and polymer relaxation. Drug release from microspheres exhibited the characteristic release pattern of a monolithic matrix system with a maximum of 80-90% drug release in 6-8 weeks demonstrating the feasibility of prolonged delivery of stavudine using biodegradable microspheres for parenteral depot system.
Export Options
About this article
Cite this article as:
Srivastava Saurabh and R. Sinha V., Development and Evaluation of Stavudine Loaded Injectable Polymeric Particulate Systems, Current Drug Delivery 2011; 8 (4) . https://dx.doi.org/10.2174/156720111795767933
DOI https://dx.doi.org/10.2174/156720111795767933 |
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
-
Association of Cerebrospinal Fluid Adiponectin Levels With Cerebral Glucose Metabolism In Mild Cognitive Impairment: A Pilot Study
Current Alzheimer Research What is the Real Efficacy of Beta-Blockers for the Treatment of Essential Hypertension?
Current Pharmaceutical Design Independent Relationship of Osteocalcin Circulating Levels with Obesity, Type 2 Diabetes, Hypertension, and HDL Cholesterol
Endocrine, Metabolic & Immune Disorders - Drug Targets Multimodality Imaging of CXCR4 in Cancer: Current Status towards Clinical Translation
Current Molecular Medicine Tyre Pressure Monitoring System - Machine Learning Approach
Recent Patents on Signal Processing (Discontinued) Neonatal Brain Hemorrhage (NBH) of Prematurity: Translational Mechanisms of the Vascular-Neural Network
Current Medicinal Chemistry Meet Our Editor-in-Chief
Current Cardiology Reviews Cardiovascular Disease: What's All the AGE/RAGE About?
Cardiovascular & Hematological Disorders-Drug Targets Renal Denervation Therapy: Can it Contribute to Better Blood Pressure Control in Hypertension?
Current Vascular Pharmacology Impact of Lean and Fat Mass on Disease Activity and Function in Spondyloarthritis
Current Rheumatology Reviews Therapeutic Use of Snake Venom Components: A Voyage from Ancient to Modern India
Mini-Reviews in Organic Chemistry Recent Applications of Nanomaterials Based on Electrochemical Drug Analysis
Current Analytical Chemistry Animal Models for Studying Neointima Formation
Current Vascular Pharmacology Current Inhibition Concepts of Zinc Metallopeptidases Involved in Blood Pressure Regulation
Current Enzyme Inhibition Nitric Oxide Related Therapeutic Phenomenon: A Challenging Task
Current Pharmaceutical Design Fine Tuning Therapeutic Targeting of the Sphingolipid Biosynthetic Pathway to Treat Atherosclerosis
Current Vascular Pharmacology The Clopidogrel-PPI Interaction: An Updated Mini-Review
Current Vascular Pharmacology Roles of Cardiovascular Risk Factors in Endothelial Nitric Oxide Synthase Regulation: An Update
Current Pharmaceutical Design Empyema and Bronchopleural Fistula Following Lung Resection
Current Respiratory Medicine Reviews Conference Report: 9th Clinical Trials on Alzheimer's Disease (CTAD): Marriott Marquis San Diego Marina, San Diego, CA, USA December 8-10, 2016
CNS & Neurological Disorders - Drug Targets