Diclofenac sodium microspheres formulation with Eudragit RS100.
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of sustained release diclofenac sodium microspheres using eudragit rs100.
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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T. Mangilal, K.S.K. Rao Patnaik, E. Nagabhushan, P. Shashikala, D. Jayaprakash
World Journal of Pharmaceutical Research:
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Full text available for: Formulation and evaluation of sustained release diclofenac sodium microspheres using eudragit rs100.
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr201612-7391
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The research aims to formulate sustained release microspheres of Diclofenac sodium, an anti-inflammatory drug, using Eudragit RS100 as the polymer. These microspheres are designed to provide a prolonged therapeutic effect by continuously releasing the drug after a single dose. The formulation process involved the O/O emulsion solvent evaporation method, with careful attention to stabilizer concentration and emulsification speeds. Various characterization techniques were employed to assess the microspheres’ performance, including entrapment efficiency, particle size analysis, and in vitro release behavior.
Sustained Release Formulation Techniques
The study utilized the O/O emulsion solvent evaporation method to create the microspheres. This technique is advantageous for improving drug encapsulation efficiency and controlling the release of water-soluble drugs. Various formulations were tested by altering the concentrations of surfactants like Span 80 and adjusting stirring speeds. The resulting microspheres displayed varying sizes and entrapment efficiencies. Among the formulations, the one with a 1% concentration of Span 80 at 1000 RPM yielded the highest entrapment efficiency of 80%, demonstrating the method's effectiveness in producing optimal particles for sustained drug delivery.
Characterization and Release Kinetics
Characterization of the microspheres included particle size determination and encapsulation efficiency assessments, with results indicating that increasing stirring speed reduced the particle size while improving encapsulation efficiency. The in vitro release study showed a steady release profile of Diclofenac sodium, with 100% drug release observed within 12 hours. The Korsmeyer-Peppas model was applied to analyze the release kinetics, revealing that the release mechanism was primarily diffusion controlled. The n value indicated a non-Fickian diffusion mechanism, suggesting a complex interaction between drug and polymer.
Compatibility and Physical Properties
Compatibility studies conducted using FTIR spectroscopy confirmed that no significant interactions existed between Diclofenac sodium and Eudragit RS100, indicating the stability of the formulation. The DSC analysis revealed that the drug was likely in an amorphous state within the polymer matrix, which can enhance its release characteristics. The physical properties, including the solubility and melting point of Diclofenac sodium, were consistent with established standards, ensuring the reliability of the formulation process.
Conclusion
The study successfully formulated sustained release microspheres of Diclofenac sodium using Eudragit RS100 through the O/O emulsion solvent evaporation technique. The optimized formulation demonstrated desirable entrapment efficiency, controlled release kinetics, and excellent compatibility between drug and polymer. The research underscores the potential of Eudragit RS100-based microspheres in achieving sustained therapeutic effects, thus representing a promising approach in drug delivery systems for anti-inflammatory treatments. Through this work, it is evident that the careful selection of method parameters can significantly influence the performance of sustained release formulations.
FAQ section (important questions/answers):
What is the main objective of the study on Diclofenac sodium?
The study aimed to formulate sustained release microspheres of Diclofenac sodium using Eudragit RS100 as a polymer, providing prolonged therapeutic effects after administering a single dose.
How were the microspheres for Diclofenac sodium prepared?
Microspheres were prepared using the O/O emulsion solvent evaporation method, varying stabilizer concentrations and emulsification speeds while maintaining a constant amount of Diclofenac sodium.
What methods characterized the prepared microsphere formulations?
The microspheres were characterized by percentage yield, particle size analysis, entrapment efficiency, in vitro release behavior, DSC, and SEM techniques to analyze their properties.
What were the results regarding the drug release profile?
The in vitro release profile showed a slow and steady release of Diclofenac sodium, with 100% release occurring within 12 hours, following a diffusion-controlled mechanism.
What did the DSC results indicate about Diclofenac sodium?
DSC results showed that the physical state of the drug changed upon formulation, indicating no interaction with the polymer and suggesting it dispersed in an amorphous state.
Which formulation was considered optimal for sustained release?
Formulation F5, containing 1% Span 80 at a speed of 1000 RPM, exhibited the highest entrapment efficiency and the desired cumulative percentage drug release, making it the optimized formulation.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Diclofenac sodium microspheres formulation with Eudragit RS100.”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Drug:
A drug is a chemical substance used in the diagnosis, cure, treatment, or prevention of disease. In the context of this study, Diclofenac sodium is highlighted as an anti-inflammatory agent. Its formulation into microspheres aims to achieve sustained release, enhancing therapeutic efficacy and patient compliance through controlled drug delivery systems.
2) Table:
A table is an organized arrangement of data typically presented in rows and columns. In scientific literature, tables are crucial for summarizing research findings such as particle sizes, yields, and encapsulation efficiencies. They allow for quick comparisons and facilitate understanding of results, which can be essential for readers interpreting the data.
3) Surface:
The surface refers to the outermost layer of an object. In this context, the surface morphology of the microspheres, analyzed via techniques such as Scanning Electron Microscopy (SEM), provides insights into their characteristics like shape and porosity, which significantly impact drug release rates and the stability of the formulation.
4) Medium:
Medium refers to the substance in which a process occurs. For example, in this research, dissolution medium (0.1 N HCl followed by phosphate buffer) plays a crucial role in evaluating the drug release behavior of microspheres. It simulates physiological conditions, influencing how effectively the drug is released and absorbed in the body.
5) Study (Studying):
A study is a systematic investigation aimed at discovering or interpreting facts. This research manuscript investigates the formulation and evaluation of sustained release microspheres containing Diclofenac sodium. It explores how varying formulation parameters affect drug entrapment efficiency and release characteristics, contributing valuable knowledge to pharmaceutical sciences and drug delivery methodologies.
6) Water:
Water is often used as a solvent in pharmaceutical formulations due to its polarity, which aids in dissolving hydrophilic substances. In this study, water's role is critical as it forms part of the microsphere preparation process and is an essential solvent for numerous chemicals, influencing the encapsulation and release of the drug.
7) Powder:
Powder is a dry substance composed of finely divided particles. In pharmaceutical formulations, active pharmaceutical ingredients (APIs) like Diclofenac sodium may be in powder form before processing. The physical properties of powders—including solubility and flowability—affect how they are processed into microspheres and ultimately their effectiveness in drug delivery.
8) Substance:
A substance refers to any material which has a definite chemical composition. The study focuses on specific substances such as Diclofenac sodium and Eudragit RS100. Understanding their properties and interactions is essential to facilitate the formulation process of sustained release microspheres and optimize drug delivery systems for therapeutic purposes.
9) India:
India is the region where the research was conducted, specifically at Osmania University, Hyderabad. The country's diverse pharmaceutical industry focuses on developing effective drug delivery systems. This context emphasizes the relevance and potential global impact of the research on sustained release formulations within the Indian pharmaceutical landscape.
10) Nature:
Nature refers to the inherent qualities or characteristics of a substance. In this research, particular attention is given to the nature of polymer Eudragit RS100, which determines its functionality as a drug carrier. Understanding these properties ensures successful encapsulation of Diclofenac sodium and influences drug release profiles.
11) Reason:
Reason indicates the cause or explanation for phenomena. In this study, various reasons are explored for the observed results in drug entrapment efficiencies and release rates from microspheres. By understanding these reasons, researchers can optimize formulation parameters to improve the performance of sustained release drug delivery systems.
12) Glass:
Glass in the study likely refers to glassware used during experiments. Glass equipment, such as beakers or volumetric flasks, is commonly utilized to prepare solvents and solutions, ensuring the accuracy and precision of measurements needed in formulating microspheres, analyzing drug content, and performing compatibility studies.
13) Biodegradable:
Biodegradable refers to the ability of a substance to decompose naturally by biological processes. Eudragit RS100 is recognized for its biodegradable properties, making it suitable for pharmaceutical applications. This characteristic minimizes environmental impact and enhances patient safety by reducing long-term effects of polymer remnants in the body post-drug release.
14) Surrounding:
Surrounding refers to the external environment where reactions or interactions occur. The surrounding conditions—such as temperature and pH—during microsphere formulation and drug release studies are critical. They can significantly affect how the drug interacts with the polymer and influences the overall effectiveness and safety of the drug delivery system.
15) Discussion:
Discussion encompasses the analytical interpretation of results gathered from experiments. In academic papers, such as this study, the discussion section evaluates the findings against the existing literature, providing insights into the efficacy and implications of the research. It critically assesses the data's relevance and suggests future areas of investigation.
16) Activity:
Activity typically describes the functional performance of a substance, such as its therapeutic effects in this study. The anti-inflammatory activity of Diclofenac sodium is central to its clinical application. Understanding the activity is crucial for validating the formulation's effectiveness and establishing its potential benefits in treating conditions like arthritis.
17) Bitter:
Bitter describes one of the basic taste sensations. In this study, the taste of Diclofenac sodium is acknowledged as slightly bitter. This characteristic can impact patient acceptability and adherence, particularly for oral formulations. Thus, understanding taste profiles may influence the development of more palatable dosage forms.
18) Purity:
Purity indicates the absence of contaminants in a chemical sample. In pharmaceuticals, high purity levels are vital for ensuring safety and efficacy. In this study, purity was assessed through melting point determination. The purity of Diclofenac sodium is crucial for reliable drug formulation and ensuring consistent therapeutic outcomes.
19) Fainting (Fainted):
Faint refers to something that is not strongly noticeable or clear. In the context of Eudragit RS100, it is described as having a faint characteristic odor. While typically not impacting its efficacy, such sensory attributes can be relevant in formulation development and may influence user perception of the final pharmaceutical product.
20) Gold (Golden):
Gold may pertain to its use as a coating material in Scanning Electron Microscopy (SEM), enhancing the visualization of microspheres. Gold is frequently used to conduct electrons effectively, contributing to detailed imaging that provides insights into the surface morphology of microspheres, impacting their performance in drug delivery systems.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Diclofenac sodium microspheres formulation with Eudragit RS100.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Particle size analysis, Sustained release, Diclofenac sodium, Scanning Electron Microscopy, Differential scanning calorimetry, Compatibility studies, Scanning Electron Microscopy (SEM), Percentage yield, Melting point determination, Standard calibration curve, Calibration factor.