Microparticle formulation and evaluation via amphiphilic crystallization
optimization of process parameter
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of microparticles formed by amphiphillic crystallization technique
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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Subtitle: optimization of process parameter
Original source:
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Ujwala S. Desai, Dhaval B. Bhavsar
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and evaluation of microparticles formed by amphiphillic crystallization technique
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The study focuses on developing a crystallization process to produce microparticles of aceclofenac, a drug known for its low solubility, aimed at enhancing its bioavailability. Traditional methods for creating particles often involve micronization, which can result in poor control over particle size and shape, impacting drug performance. The researchers explored amphiphilic crystallization using poly(ethylene glycol) 400 (PEG 400) as a solvent to facilitate the formation of microparticles with controlled size distribution and improved solubility.
Influence of PEG 400 on Solubility
The investigation revealed that the solubility of aceclofenac increased significantly with higher concentrations of PEG 400 in water. A logarithmic relationship was observed, indicating that as PEG concentration rose, solubility improved markedly. This demonstrated PEG 400's suitability as a solvent for dissolving hydrophobic drugs, facilitating a practical means to enhance solubility and subsequently drug bioavailability.
Particle Size Reduction through Antisolvent Crystallization
The research established that the process of antisolvent crystallization effectively reduced the particle size of aceclofenac microparticles. Employing central composite design experiments, the study found that factors such as surfactant concentration and stirring speed had significant impacts on the particle size distribution. Increased supersaturation due to higher surfactant concentration led to more nucleation events, resulting in smaller particles. This reduction in particle size enhances dissolution, as smaller particles provide a larger surface area for solvation.
Assessment of Drug Release Profiles
In vitro drug release studies demonstrated that the formulated microparticles exhibited superior release profiles compared to unprocessed aceclofenac. The processed samples achieved a release rate of over 75% within 30 minutes, indicating enhanced drug bioavailability. This rapid dissolution can be attributed to the improved solubility of the microparticles, stemming from their smaller size and high surface area. Consequently, the study validated the efficiency of the amphiphilic crystallization technique in optimizing drug release characteristics.
Conclusion
The study successfully established PEG 400 as an effective medium for the amphiphilic crystallization of aceclofenac, resulting in microparticles with improved solubility and drug release profiles. By optimizing factors influencing particle size distribution, the research introduced a novel and environmentally friendly method for producing pharmaceutical formulations with enhanced bioavailability. Future studies will explore the application of this technique to other drug substances, potentially broadening its utility in pharmaceutical manufacturing.
FAQ section (important questions/answers):
What was the objective of the study on aceclofenac microparticles?
The objective was to develop a crystallization process for producing aceclofenac microparticles with controlled particle size distribution, aiming to enhance solubility and maximize oral bioavailability through nanosized crystalline forms.
How does PEG 400 improve the solubility of aceclofenac?
PEG 400 increases the solubility of aceclofenac significantly. A logarithmic relationship was found, showing solubility improved dramatically with higher concentrations of PEG in water, enabling better precipitation of crystals during antisolvent crystallization.
What techniques were used to characterize the microparticles produced?
The microparticles were characterized using X-ray powder diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, and particle size measurement techniques to assess their physicochemical properties.
What were the key findings regarding particle size and yield?
The studies indicated that increased supersaturation led to smaller microparticle sizes and higher yields, which ranged from 80% to 90%. The average particle size was notably reduced from 200 µm to approximately 4-6 µm.
How did the drug release profiles compare to unprocessed aceclofenac?
The in vitro dissolution profiles demonstrated that all batches of processed aceclofenac exhibited significantly improved drug release rates compared to unprocessed forms, with up to 75% release achieved within 30 minutes.
What advantages does amphiphilic crystallization offer for drug processing?
Amphiphilic crystallization provides a novel, environmentally friendly technique without the need for traditional crystallization inhibitors. It effectively controls particle size distribution and improves solubility, enhancing the bioavailability of poorly soluble drugs.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Microparticle formulation and evaluation via amphiphilic crystallization”. 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, treatment, or prevention of diseases. In this context, aceclofenac is the drug of interest, which is known for its anti-inflammatory properties. The formulation of drugs into microparticles enhances their solubility and bioavailability, significantly impacting therapeutic effectiveness.
2) Table:
In scientific research, a table is a structured arrangement of data, often used for organizing quantitative information. Here, tables are utilized to present experimental results, such as responses from formulations, particle sizes, drug content, and yields, helping to facilitate clear data analysis and comprehension in the study.
3) Water:
Water acts as both a solvent and an antisolvent in crystallization processes. In the study, it interacts with poly(ethylene glycol) to form a solution in which aceclofenac can be crystallized. Additionally, it plays a crucial role in the solubilization of hydrophobic compounds, influencing the drug's final formulation.
4) Surface:
Surface properties significantly affect the dissolution rates and bioavailability of drugs. In the context of microparticles, the particle surface area increases, allowing for enhanced contact with solvents, which leads to improved solubility and faster drug release compared to larger unprocessed drug crystals.
5) Study (Studying):
A study refers to a structured investigation designed to generate knowledge about a specific subject. In this context, the study investigates the formulation and evaluation of aceclofenac microparticles, with a focus on the impacts of process parameters on particle size, solubility, and drug release characteristics.
6) Powder:
Powder is a solid substance composed of finely divided particles. In pharmaceuticals, the properties of the powder, including flowability and particle size distribution, are critical for formulating solid dosage forms. The study analyzes the produced microparticles' powder characteristics to ensure suitable properties for further applications.
7) Noise:
In statistical analysis and experimental design, noise refers to the variability or random errors that may obscure true relationships between variables. In this research, minimizing noise is essential to enhance the reliability of data, ensuring that observed effects are attributed to actual differences in experimental conditions rather than random fluctuations.
8) Glass:
Glass is often used in laboratory settings for various applications, including sample preparation and storage. The beakers and vials mentioned in the study highlight the use of glassware for mixing, crystallization, and containing solutions, ensuring chemical stability and preventing contamination during experiments.
9) Medium:
In the context of this research, medium refers to the solvent system used for crystallization processes. Poly(ethylene glycol) (PEG) is described as an environmentally benign medium, offering favorable conditions for solubilizing aceclofenac, thereby facilitating the successful production of microparticles with controlled properties.
10) Substance:
A substance is a particular kind of matter with uniform properties. Here, aceclofenac is the active pharmaceutical substance being formulated into microparticles. The study investigates the relationship between the properties of the substance and the various formulation parameters affecting its bioavailability and therapeutic efficacy.
11) Relative:
Relative is a term that signifies a comparison between two or more entities. In the study, various parameters such as solubility and particle size are measured relative to their respective theoretical values, helping to evaluate the effectiveness of the amphiphilic crystallization method in achieving desired outcomes.
12) Reason:
Reason refers to the underlying rationale or justification behind specific observations or results. The study discusses reasons for variations in particle size and solubility, attributing them to factors like supersaturation and stirring speed, which influence crystallization dynamics and ultimately affect drug performance.
13) Measurement:
Measurement is the process of obtaining the magnitude of a quantity. In this study, precise measurements of solubility, particle size, and drug content are crucial for evaluating the formulations. These quantitative assessments ensure consistency and reliability in the characterization of the developed microparticles.
14) Transformation (Transform, Transforming):
Transform refers to a change in form, appearance, or structure. In the context of this research, the transformation of aceclofenac from its bulk crystalline form to microparticles enhances its solubility and dissolution rate, thereby altering its bioavailability profile and improving therapeutic effectiveness.
15) India:
India is the country where the research was conducted, specifically at a pharmacy college in Pune, Maharashtra. The location emphasizes the growing importance of pharmaceutical research within India’s healthcare system and its efforts in developing advanced drug formulation techniques to improve patient outcomes.
16) Maharashtra (Mahārāṣṭra, Maha-rashtra):
Maharashtra is a state in India, hosting the research study at a pharmacy college in Pune. Understanding the regional context is essential as it often influences research priorities, collaboration opportunities, and access to resources critical for advancing pharmaceutical sciences and public health strategies.
17) Education:
Education refers to the academic and practical training provided to individuals in various fields, including pharmacy. The study conducted at an educational institution highlights the importance of academic research in contributing innovative solutions, developing professionals capable of formulating effective drug therapies.
18) Composite:
Composite typically refers to a material made from combining two or more different substances. In this study, the term 'composite' appears in the context of the central composite design (CCD) used for optimizing crystallization parameters, representing a structured experimental design to identify the best formulation conditions.
19) Pune:
Pune is a city in Maharashtra, India, known for its educational institutions and pharmaceutical industry. The research conducted in Pune reflects the city’s role in advancing pharmaceutical sciences and innovation, contributing to drug formulation methods that enhance the efficacy and safety of therapeutic agents.
20) Wall:
In the study, the wall of the beaker plays a crucial role during the controlled addition of antisolvent (water). This method is essential for ensuring an optimal mixing action without causing immediate nucleation, which can lead to uncontrolled particle growth and an unfavorable particle size distribution.
21) Observation:
Observation is the act of viewing or monitoring phenomena to gather information. Throughout this study, various observations, such as changes in solubility or particle size, are reported, enabling researchers to infer relationships between formulation parameters and the physicochemical properties of the final product.
22) Discussion:
Discussion is a critical component of research that interprets results and relates findings to theoretical concepts. In this study, the discussion section allows for the analysis of the implications of results related to particle size, drug release, and solubility, ultimately leading to conclusions about the formulation techniques employed.
23) Developing:
Developing refers to the process of creating or improving something. The study focuses on developing a novel amphiphilic crystallization method, enhancing the solubility and bioavailability of aceclofenac, which is essential for optimizing drug formulations to ensure effective treatment outcomes in patients.
24) Knowledge:
Knowledge is the understanding and awareness gained through experience or education. This study contributes to the knowledge base of pharmaceutical sciences by exploring new formulation techniques and their effects on drug solubility and bioavailability, providing insight for future research and development efforts.
25) Toxicity:
Toxicity refers to the degree to which a substance can harm organisms. The study emphasizes using PEG as a safe alternative to conventional organic solvents, demonstrating its low toxicity in pharmaceutical applications. Understanding toxicity is crucial for ensuring the safety of drug formulations for patients.
26) Species:
In scientific contexts, species refers to a group of organisms sharing common characteristics. In pharmaceutical studies, it may refer to the models or subjects used for testing. Understanding species differences helps in determining the applicability of certain findings in drug formulation development and testing.
27) Falling:
Falling is a term that generally denotes descent, but in this study, it might refer to the falling performance or effectiveness of a drug formulation if not properly developed. Keeping performance metrics optimal is crucial for the successful delivery of therapeutic agents to patients.
28) Nature:
Nature refers to the inherent characteristics and qualities of substances. In this context, the nature of aceclofenac, including its physical and chemical properties, significantly affects its solubility and bioavailability, necessitating innovative formulation strategies to enhance its therapeutic functionality.
29) Food:
Food here relates to the safety and regulatory considerations in pharmaceuticals. The study cites that PEG is on the Food and Drug Administration's 'generally regarded as safe' list, signifying its suitability for potential use in drug formulation without posing significant safety risks to patients.
30) Line:
Line can refer to a series or continuum in scientific data presentation. In this study, the term may emphasize trends observed in results, such as solubility versus concentration or yield versus parameters, forming a crucial basis for understanding the implications of the research findings.
31) Gold (Golden):
In laboratory settings, gold may refer to the materials used in instrumentation, such as gold-palladium coating during SEM analysis. This coating is critical for enhancing the quality of imaging data, enabling detailed examination of microparticle morphology and providing insights into their surface features.
32) Pur (Pūr):
Poor refers to inadequate or insufficient conditions. In the context of this study, poor control of crystal characteristics during traditional processes like milling can lead to undesirable outcomes. The research aims to address these issues through improved methods that yield better-defined particle properties.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Microparticle formulation and evaluation via amphiphilic crystallization’. Further sources in the context of Science might help you critically compare this page with similair documents:
In vitro, Zeta potential, Scanning Electron Microscopy (SEM), Fourier transform Infrared Spectroscopy (FTIR).