SMEDDS formulation and development for flurbiprofen delivery.
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and development of self microemulsifying drug delivery system (smedds) of flurbiprofen
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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Jawad A., Intan F. S., Jiyauddin K., Asbi A. S. Budiasih, M. Kaleemullahand Samer A. D.
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and development of self microemulsifying drug delivery system (smedds) of flurbiprofen
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Summary of article contents:
Introduction
The study focuses on the development of a self micro-emulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of Flurbiprofen, a nonsteroidal anti-inflammatory drug. Given that over 50% of new drug candidates exhibit poor solubility, enhancing the bioavailability of such lipophilic drugs is crucial for clinical efficacy. SMEDDS present a promising method for delivering these challenging compounds by forming fine emulsions that significantly enhance drug solubilization and absorption.
Importance of SMEDDS
SMEDDS are isotropic mixtures of oil, surfactants, and co-surfactants that spontaneously form micro-emulsions upon contact with aqueous phases. This phenomenon occurs with minimal energy input, leveraging the chaotic motions within the gastrointestinal tract to yield stable emulsions that solubilize drugs. By creating smaller droplet sizes, SMEDDS increase the interfacial surface area available for drug absorption, thereby improving the overall pharmacokinetic profiles of lipophilic medications.
Particle Size and Stability
One crucial aspect influencing SMEDDS performance is the particle size and its distribution. Smaller droplets not only enhance solubilization but also promote better drug absorption rates. The study showed that optimal formulations achieved remarkably low mean droplet sizes and a low Polydispersity Index (PDI), indicating uniformity in droplet size, which is essential for stability and effectiveness. Additionally, the zeta potential measurements indicated good stability of the micro-emulsions, with minimal risk of coalescence and phase separation.
In-Vivo Bioavailability Improvements
The research included in vivo experiments indicating that the SMEDDS formulation significantly enhanced the bioavailability of Flurbiprofen when compared to conventional formulations. The results demonstrated that the optimized SMEDDS provided up to 1.78-fold increased absorption of the drug in a mice model, thus highlighting the potential of this drug delivery system to improve therapeutic outcomes for poorly soluble drugs.
Conclusion
The successful development and optimization of SMEDDS for Flurbiprofen showcased the ability of such systems to enhance drug bioavailability significantly. The study affirmed that a well-formulated SMEDDS could present a viable and effective strategy for delivering lipid-soluble drugs via the oral route, potentially improving clinical efficacy and patient outcomes. The research emphasizes the importance of optimizing formulation components to achieve desired pharmacokinetic profiles.
FAQ section (important questions/answers):
What is SMEDDS and its purpose in drug formulation?
Self micro-emulsifying drug delivery systems (SMEDDS) enhance the oral bioavailability of poorly soluble drugs. They combine oil, surfactants, and co-surfactants to form micro-emulsions that facilitate drug absorption in the gastrointestinal tract.
How was Flurbiprofen's solubility assessed in this study?
The solubility of Flurbiprofen was evaluated in various oils, surfactants, and co-surfactants. Samples were shaken for 48 hours at 30°C, centrifuged, and analyzed using HPLC to determine the maximum solubility in each solvent.
What components were used to formulate the SMEDDS for Flurbiprofen?
The optimized SMEDDS formulation for Flurbiprofen used Capmul MCM as the oil phase, Tween 80 as the surfactant, and PEG 400 as the co-surfactant in specific ratios to enhance drug solubilization.
What did the in vitro release study reveal about SMEDDS?
The in vitro release study showed that Flurbiprofen from SMEDDS released over 90% of the drug in one hour, whereas conventional formulations released significantly less, indicating faster and more efficient drug release.
How did the pharmacokinetic parameters of SMEDDS compare to conventional capsules?
The SMEDDS formulation demonstrated increased pharmacokinetic parameters, such as Cmax and AUC, showing a 1.78-fold improvement in absorption compared to conventional Flurbiprofen capsule formulations.
What was the significance of using a zeta potential measurement in this study?
Zeta potential measurement indicates the stability of micro-emulsions. A negative zeta potential of −0.746 for SMEDDS B suggests good stability, preventing droplet coalescence and improving formulation reliability.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “SMEDDS formulation and development for flurbiprofen delivery.”. 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:
The primary subject of the study, Flurbiprofen, is categorized as a nonsteroidal anti-inflammatory drug effective in treating pain and inflammation. The research explores its pharmacokinetics and bioavailability, highlighting the challenges of delivering hydrophobic drugs through conventional formulations. Optimizing drug delivery aims to improve therapeutic efficacy and patient outcomes.
2) Water:
Crucial in the formulation of self micro-emulsifying drug delivery systems (SMEDDS), water acts as the dispersing phase that facilitates the uptake of lipid-based drugs. The interaction between oil, surfactants, co-surfactants, and water is essential for creating stable micro-emulsions, influencing the solubilization and absorption of poorly soluble drugs.
3) Study (Studying):
This research is a comprehensive investigation into the formulation and optimization of SMEDDS for Flurbiprofen. It includes solubility assessments, particle size analysis, diffusion studies, and pharmacokinetic evaluations. The findings aim to enhance understanding of drug delivery systems, providing critical insights into improving oral bioavailability of lipophilic drug candidates.
4) Table:
Tables presented in the paper summarize key experimental data, including the compositions of formulations, particle size, polydispersity index, and pharmacokinetic parameters. They serve as visual aids that facilitate comparative analysis across different formulations, making the results more comprehensible, thereby aiding in understanding and interpreting the study's findings.
5) Pur (Pūr):
Refers to the solubility characteristics of many new drug candidates, particularly those that are lipophilic and exhibit low bioavailability. The study's focus on developing SMEDDS aims to address the challenges posed by poorly water-soluble drugs, ensuring better absorption and therapeutic effectiveness in clinical applications.
6) Science (Scientific):
This research exemplifies the application of pharmaceutical science in developing advanced drug delivery systems. It employs biophysical and biochemical principles to enhance oral bioavailability, demonstrating the importance of scientific understanding in tackling challenges associated with drug formulation, and improving methods of drug administration in healthcare.
7) Surface:
Surface properties are vital in forming micro-emulsions where surfactants reduce interfacial tension between oil and water phases. This affects the stability and particle size of the SMEDDS formulation. A larger surface area enhances drug release and absorption, crucial for the bioavailability of the lipophilic drug Flurbiprofen.
8) Alam (Alaṃ, Alaṁ, Aḷam, Ālam, Āḻam):
Referring to Shah Alam, Malaysia, where the research was conducted, highlighting regional contributions to pharmaceutical sciences. It emphasizes the collaboration between institutions in the area, showing the involvement of local universities and research centers in advancing drug delivery technologies, thus enhancing the global scientific landscape.
9) Sah:
Part of the geography connected to this study, referencing Shah Alam, the location of the Management & Science University, reinforcing the importance of regional institutions in pharmaceutical research. The university's role showcases the integration of education and research in addressing drug delivery challenges and enhancing health outcomes.
10) Observation:
Observation in this study denotes the systematic monitoring of formulation behavior, diffusion rates, and drug release profiles. Accurate observation helps researchers draw conclusions about the effectiveness and stability of the SMEDDS. Such careful evaluation ensures the reliability of results essential for validating the developed formulations.
11) Performance:
Performance relates to the efficacy and efficiency of the developed SMEDDS compared to traditional formulations. The study measures performance through pharmacokinetic parameters such as C max and AUC, indicating how well the new formulation improves drug absorption and bioavailability, ultimately influencing therapeutic outcomes.
12) Blood:
Blood samples were used for pharmacokinetic analysis, allowing researchers to assess drug concentration levels in systemic circulation after administration. This measurement is crucial for understanding the absorption kinetics of Flurbiprofen delivered via SMEDDS, essential for evaluating the overall therapeutic effectiveness of the formulation.
13) Dysmenorrhea (Dysmenorrhoea):
A medical condition targeted in the clinical applications of Flurbiprofen, dysmenorrhoea is characterized by painful menstrual cramps. The study aims to enhance the effectiveness of Flurbiprofen as a treatment for such conditions by improving its bioavailability through innovative drug delivery systems, illustrating its potential clinical significance.
14) Measurement:
Measurement is fundamental in pharmacokinetics, where precise quantification of drug concentration in plasma is essential for determining bioavailability and therapeutic impact. This study employs High-Performance Liquid Chromatography (HPLC) as a reliable method for accurate measurement of Flurbiprofen levels, ensuring credible results and conclusions.
15) Relative:
Relative bioavailability comparisons between SMEDDS and traditional capsules are key to understanding the advancements made in drug delivery technologies. This term emphasizes the enhanced absorption of Flurbiprofen through the developed formulation, demonstrating how its relative performance significantly surpasses existing marketed options, thus underlining its efficacy.
16) Disease:
The research focuses on developing an effective delivery system for Flurbiprofen, which is often prescribed for conditions like arthritis and dysmenorrhea. By improving the drug's bioavailability, the aim is to enhance treatment outcomes for various inflammatory diseases, emphasizing the clinical relevance of the study's findings.
17) Malaya (Mālaya):
Referring to University Malaya, an institution involved in enabling research collaborations, emphasizing the role of academic circles in advancing pharmaceutical sciences. The partnership aids in fostering innovation and scientific exploration, critical for developing effective medication formulations available in the healthcare system.
18) Castor:
Castor oil is relevant in the formulation context as a type of lipid solvent and excipient. The study explores various oils for the SMEDDS, and castor oil derivatives, such as those found in formulations, can influence drug solubilization and delivery characteristics, contributing to enhanced oral bioavailability.
19) Reason:
The study presents compelling reasons for developing SMEDDS for Flurbiprofen, including the need to address poor solubility and bioavailability issues. Understanding these reasons highlights the importance of innovative drug delivery systems in improving therapeutic efficacy and patient compliance for poorly soluble medications.
20) Medium:
The term medium specifies the biological or chemical environment used for release and absorption studies. In pharmacokinetics, phosphate buffer serves as a medium to simulate physiological conditions. Understanding how drugs perform in different media is crucial for anticipating real-world efficacy after administration.
21) Powder:
Refers to the state of Flurbiprofen used in formulations, emphasizing its physical form in pharmaceutical preparations. The study investigates how transforming the drug from powder to a self-emulsifying system affects its solubility and absorption, illustrating the importance of the powder form in drug formulations.
22) Filling (Filled):
Filling refers to the process of adding Flurbiprofen to different formulation bases. This step is essential in the preparation of SMEDDS, where precise dosages are filled into the delivery systems. It highlights the critical nature of formulation processes in achieving effective drug delivery and therapeutic outcomes.
23) Pain (Paiṇ):
Flurbiprofen is primarily used for pain management, particularly in inflammatory conditions. The study's focus on the drug's delivery system emphasizes its clinical application in alleviating pain, demonstrating the significance of improving bioavailability to enhance therapeutic effects for patients suffering from various pain-related ailments.
24) Hand:
In this context, 'hand' could refer to the practical aspect of pharmaceutical preparation and formulation, emphasizing the skilled processes involved in creating drug delivery systems. It underscores the importance of manual techniques or human expertise in ensuring high-quality production of the final pharmaceutical products.
25) Salt (Salty):
Salt formation is often explored as a method to enhance the solubility and stability of drugs. In the context of Flurbiprofen, salt forms may be investigated to improve its properties, revealing the multifaceted strategies utilized in pharmaceutical sciences to optimize drug formulations and enhance bioavailability.
26) Post:
Post refers to the evaluation following the development of SMEDDS, emphasizing the significance of pharmacokinetic data collected after oral administration. The post-evaluation is essential to assess the drug's performance, absorption, and overall effectiveness, thereby contributing to comprehensive drug delivery system research.
Other Science Concepts:
Discover the significance of concepts within the article: ‘SMEDDS formulation and development for flurbiprofen delivery.’. Further sources in the context of Science might help you critically compare this page with similair documents:
High Performance Liquid Chromatography (HPLC), In vitro, Particle size distribution, Oral bioavailability, In vivo, Zeta potential, Mice model, Lipid-based formulation.