Formulation and in vitro evaluation of floating microspheres of atomoxetine hcl
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and in vitro evaluation of floating microspheres of atomoxetine hcl
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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S.Swathi, Potlapally Laxmi, Azeez Mohammad, G.Shirisha
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and in vitro evaluation of floating microspheres of atomoxetine hcl
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
This research focused on the development and evaluation of floating microspheres containing Atomoxetine Hcl, aimed at prolonging gastric residence time and enhancing drug bioavailability for the treatment of Attention Deficit Hyperactivity Disorder (ADHD). Atomoxetine Hcl exhibits good oral absorption but has a bioavailability of only 63% and a half-life of approximately five to six hours. The study explores the formulation of floating microspheres using ethyl cellulose and other biocompatible polymers through a non-aqueous solvent evaporation method. The primary goal was to optimize the formulation for sustained drug release, improving the bioavailability of Atomoxetine Hcl.
Floating Microspheres Fabrication
The floating microspheres were prepared using a non-aqueous solvent evaporation method with varying proportions of Atomoxetine Hcl and ethyl cellulose. The prepared microspheres were characterized for critical parameters such as size, entrapment efficiency, and buoyancy. The results demonstrated that increasing the concentration of ethyl cellulose enhanced both the entrapment efficiency and particle size of the microspheres. This indicates that the choice and concentration of polymer directly affect the properties of the floating microspheres, critical for achieving prolonged gastric residence and sustained release of the drug.
Drug Release and Buoyancy Studies
In-vitro buoyancy studies were performed to evaluate the ability of the microspheres to float in simulated gastric fluid (SGF), revealing that microspheres with higher polymer concentrations exhibited lower buoyancy. This behavior was attributed to reduced porosity resulting from increased viscosity, which slowed the solvent evaporation process. Furthermore, the release studies showed that higher polymer concentrations led to reduced drug release over time, with formulation F1 demonstrating successful drug release retention for up to 12 hours. The characterization of the release kinetics indicated that the release followed Peppas and Higuchi models, suggesting a controlled release mechanism.
Micromeritic Properties and Characterization
The microspheres demonstrated acceptable micromeritic properties, essential for ensuring proper flow and handling during manufacturing and drug delivery. Parameters such as bulk density, tapped density, Carr’s compressibility index, Hausner’s ratio, and angle of repose were evaluated, confirming that the formulations had favorable flow characteristics. Additionally, the percentage yield of various formulations was calculated, indicating effective material recovery throughout the preparation process. Understanding these properties is crucial for developing efficient drug delivery systems, especially for formulations designed to remain in the stomach for extended periods.
Conclusion
The study successfully developed and characterized floating microspheres of Atomoxetine Hcl, illustrating the potential of biocompatible polymers like ethyl cellulose in enhancing drug formulations. The findings indicate that these microspheres can significantly improve the oral bioavailability and therapeutic efficacy of Atomoxetine Hcl through sustained drug release and increased gastric residence time. Overall, the research emphasizes the viability of floating microspheres in optimizing drug delivery systems, ultimately contributing to better patient outcomes through reduced dosing frequency and improved therapeutic effectiveness.
FAQ section (important questions/answers):
What is the purpose of formulating floating microspheres of Atomoxetine HCl?
The primary goal is to prolong gastric residence time and enhance oral bioavailability by using a floating, sustained-release microsphere system, which helps optimize drug delivery, especially since Atomoxetine is mainly absorbed in the stomach and upper gastrointestinal tract.
What method was used to prepare the floating microspheres?
Floating microspheres were prepared using the non-aqueous solvent evaporation method, in which a drug-polymer solution was dissolved and then poured into a dispersion medium containing liquid paraffin, allowing for the solvent to evaporate and microspheres to form.
How does ethyl cellulose affect the characteristics of the microspheres?
Increasing the concentration of ethyl cellulose improved the entrapment efficiency and particle size of the microspheres. Higher polymer concentration increases viscosity, which affects the microspheres' characteristics like buoyancy and drug release rates.
What were the key findings from the in-vitro drug release studies?
The in-vitro drug release studies demonstrated that higher concentrations of polymer reduced drug release rates. The formulation F1 achieved a substantial delayed release of Atomoxetine HCl over a 12-hour period, showcasing effective sustained-release properties.
What results were observed regarding the buoyancy of the microspheres?
In-vitro buoyancy studies indicated that microspheres with lower polymer concentrations exhibited better buoyancy, whereas higher polymer concentrations led to reduced buoyancy due to decreased porosity and increased viscosity affecting solvent evaporation.
What is the significance of the kinetic modeling results?
The kinetic modeling results identified the Peppas model as the best fit for release data of F1 and F2, while F3 and F4 were best described by the Higuchi matrix model, helping in understanding the release mechanism of the drug from microspheres.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Formulation and in vitro evaluation of floating microspheres of atomoxetine hcl”. 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:
In this context, a drug refers to Atomoxetine HCl, a medication used for treating Attention-Deficit/Hyperactivity Disorder (ADHD). Its formulation into floating microspheres aims to enhance oral bioavailability and gastric retention, which are critical factors in effective medication delivery and therapeutic response.
2) Table:
Tables are employed to systematically present data results, including micromeritic properties of floating microspheres and the results of in-vitro drug release studies. They facilitate easy comprehension and comparison of different formulations, showcasing variations in parameters such as particle size, entrapment efficiency, and buoyancy percentages.
3) Surface:
Surface refers to the outer layer of microspheres where interactions occur with the surrounding medium. The surface characteristics influence drug release and buoyancy properties of the formulated microspheres, impacting the drug's absorption in the gastric environment and therefore contributing to the drug's bioavailability.
4) Science (Scientific):
Science is integral to the research and development of pharmaceutical formulations, including the study of drug- polymer interactions, formulation processes, and biological response. It encompasses principles from chemistry, biology, and material science to innovate effective drug delivery systems and improve therapeutic outcomes.
5) Medium:
In the context of this research, medium refers to the simulated gastric fluid (SGF) used during the in-vitro studies to assess the buoyancy and drug release characteristics of the microspheres. The choice of medium is crucial, as it mimics physiological conditions for accurate evaluation.
6) Study (Studying):
The study outlines the formulation and evaluation of Atomoxetine HCl microspheres, showcasing methodologies such as drug entrapment efficiency, particle size analysis, and in-vitro drug release tests. Its findings contribute to understanding how to enhance the pharmacokinetic properties of the medication.
7) Andhra (Āndhra, Amdhra):
Andhra Pradesh is the Indian state where the research is conducted. Its mention highlights the geographical context of the study, indicating where the formulation research is taking place and aligning with local pharmaceutical industries and educational institutions that facilitate such research.
8) India:
India signifies the country where this research was performed. It provides context for the pharmaceutical regulations, market availability of Atomoxetine HCl, and the academic landscape that lends itself to innovative pharmaceutical research and development, bridging traditional methods with modern science.
9) Powder:
Powder refers to the form in which the drug and excipients are processed during microsphere preparation. The properties of the powder, including flowability and particle size, affect the efficiency of microsphere formation and ultimately influence the drug's release kinetics in the gastrointestinal tract.
10) Filling (Filled):
Filled pertains to the dosage form that contains the active drug, Atomoxetine HCl, within the microspheres prepared during the study. This encapsulation is essential to achieve controlled release and targeted delivery, ultimately enhancing the therapeutic effect and minimizing side effects.
11) Life:
Life in this context relates to the pharmacokinetic parameter 'half-life,' which for Atomoxetine HCl is approximately 5-6 hours. Understanding a drug's half-life is crucial for dosing regimen design and evaluating how long the drug remains effective in the body, impacting treatment strategies.
12) New Delhi:
New Delhi, as the capital city of India, represents locations pertinent to pharmaceutical companies and laboratories involved in drug research. It also connects to regulatory bodies governing drug approval and oversight, playing a significant role in the pharmaceutical landscape.
13) Discussion:
Discussion is the section of the research paper where results are interpreted, evaluated, and compared to existing literature. It offers critical insights into the significance of findings, exploring implications for clinical applications, and contributing to the discourse within pharmaceutical science.
14) Shirisha (Śirīṣa, Sirīsa, Śirīṣa, Sirisa, Shirisa, Sirisha):
Shirisha is one of the contributors to this study, indicating teamwork and collaboration in pharmaceutical research. Individual contributions are vital for advancing the study and developing effective drug formulations, highlighting the importance of interdisciplinary efforts in scientific research.
15) Crushing:
Crushing refers to the process of breaking down microspheres to extract entrapped drug for evaluation purposes. This process is essential for measuring the drug entrapment efficiency, reflecting the effectiveness of the microsphere formulation and influencing the assessment of drug release behavior.
16) Purity:
Purity is a measure of the quality of the Atomoxetine HCl used in the study, which is essential to ensure that the drug's composition is free from contaminants. High purity levels are critical in pharmaceutical formulations to guarantee safety and efficacy for therapeutic use.
17) Nature:
Nature refers to the physical and chemical characteristics of the polymers and other compounds used in the microsphere formulation. Understanding the nature of these materials is essential for predicting their behavior in drug release, stability, and interaction with the drug.
18) Laxmi:
Laxmi is a co-author of the study, contributing to the collaborative effort in the research team. The inclusion of multiple researchers emphasizes teamwork in scientific inquiry, helping to balance various roles and expertise required to conduct comprehensive pharmaceutical research.
19) Delhi:
Delhi, synonymous with New Delhi, denotes the capital city of India, highlighting its role as a hub for pharmaceutical innovation, education, and regulatory practices. This geographical context supports the research's relevance within the local pharmaceutical landscape and regulatory frameworks.
20) Water:
Water is a solvent referenced in the solubility profile of Atomoxetine HCl. The solubility of the drug in water is a key property impacting its formulation and release characteristics. Adequate solubility is essential for achieving the desired bioavailability in the target gastrointestinal region.