Journal name: World Journal of Pharmaceutical Research
Original article title: Glipizide loaded floating microsphere
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: formulation and evaluation
Original source:
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Dr. Radhika Parasuram Rajam and Chetan Borkhataria
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Glipizide loaded floating microsphere
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
Diabetes has emerged as a significant health concern globally, with projections suggesting an increase in affected individuals to 366 million by 2030. Effective management and treatment options are imperative, leading to the exploration of advanced drug delivery systems. Among these innovations, Floating Drug Delivery Systems (FDDS) have gained attention for their ability to prolong the gastric residence time of drugs, especially for those that exhibit issues with solubility or absorption in the gastrointestinal tract. This study focuses on the formulation and evaluation of a gastro-retentive floating drug delivery system for glipizide, a medication commonly used in managing Type II diabetes.
Formulation of Floating Microspheres
The main objective of the study was to create glipizide-loaded floating microspheres to enhance bioavailability by retaining the drug within the stomach for controlled release. The study investigated eight different formulations using polymers such as Hydroxypropylmethylcellulose (HPMC) and Eudragit RS100. These microspheres were prepared using the emulsion solvent diffusion method, aiming for a drug-to-polymer ratio of 1:7. Characterization of the microspheres demonstrated their hollow structure and satisfactory buoyancy, as their densities were below that of gastric fluid, resulting in floating times exceeding 12 hours.
Drug Release Characteristics
The in-vitro drug release studies were conducted in 0.1 N hydrochloric acid, revealing varied release rates across formulations. Specific formulations displayed controlled drug release, with particular attention to the selected F4 formulation that achieved a release of 94.68% over 12 hours. The study indicated that upon increasing the proportion of HPMC, the percentage drug release improved, while also maintaining adequate buoyancy. Kinetic analysis showed that drug release primarily followed zero-order kinetics, indicating a consistent drug release rate over time.
In-Vivo Efficacy
In-vivo evaluations conducted on Wistar rats showcased the hypoglycemic effects of the floating microspheres compared to pure glipizide. The floating microspheres exhibited a slower and more sustained reduction in blood glucose levels, maintaining significant hypoglycemic effects over a longer duration, from 2 to 12 hours following administration. This extended effect underscores the advantage of the controlled release system, demonstrating that the floating formulation can effectively manage glucose levels while minimizing side effects associated with rapid release formulations.
Conclusion
The study successfully developed glipizide-loaded floating microspheres, demonstrating promising pharmacotechnical properties including excellent floatability, prolonged gastric retention, and sustained drug release. The findings confirm that such delivery systems could enhance the effectiveness of glipizide in diabetes management by ensuring more consistent therapeutic effects and reducing the need for frequent dosing. Overall, this research affirms the potential of floating microspheres as a viable strategy for improving oral drug delivery, particularly for drugs requiring prolonged gastric retention.
FAQ section (important questions/answers):
What is the purpose of glipizide floating microspheres?
The purpose is to create a gastro-retentive drug delivery system for glipizide. This system aims to prolong gastric retention, control the drug release, and improve bioavailability, thereby managing diabetes more effectively.
Which polymers were used in the formulation of microspheres?
Hydroxypropylmethylcellulose (HPMC) and Eudragit RS100 were used as polymers. These polymers help achieve the desired floating properties and controlled drug release of glipizide from the microspheres.
What was the method used to prepare the floating microspheres?
The floating microspheres were prepared using the emulsion solvent diffusion technique. This method ensures the formation of hollow microspheres that exhibit buoyancy and controlled drug release characteristics essential for effective drug delivery.
What were the results regarding the buoyancy of the microspheres?
The microspheres showed excellent buoyancy, with densities lower than gastric fluid. The densities ranged from 0.475 to 0.975 gm/cm3, allowing prolonged floating times of over 12 hours in gastric conditions.
How did the in-vitro drug release profile perform?
The best formulation (F4) achieved about 94.68% drug release in 12 hours. This indicates that the microspheres effectively control the drug release rate, enhancing the therapeutic effects of glipizide.
What were the findings from the in-vivo studies on Wistar rats?
In-vivo studies showed that glipizide floating microspheres maintained significant hypoglycemic effects for 12 hours, compared to rapid reductions with pure glipizide. This highlights sustained release and better glucose control using the microsphere formulation.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Glipizide loaded floating microsphere”. 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:
Drug refers to a chemical substance used for medical treatment, which in this context is glipizide, an anti-diabetic agent. It plays a crucial role as the therapeutic agent being formulated into floating microspheres to enhance its bioavailability and controlled release, particularly for diabetes management.
2) Study (Studying):
Study pertains to the research conducted to develop a controlled drug delivery system for glipizide. This involves investigating various formulations and determining their effectiveness through in vitro and in vivo experiments, which is essential for validating the success of the developed microspheres in therapeutic applications.
3) Blood:
Blood is the vital fluid in the body whose glucose levels are monitored in the context of diabetes treatment. The study assesses the hypoglycemic effects of glipizide-loaded microspheres by measuring blood glucose reductions, indicating the drug's efficacy in controlling diabetes.
4) Table:
Table serves as a method of presenting organized data clearly in the research. The results related to drug entrapment, release kinetics, and stability studies are systematically tabulated to facilitate comparison and analysis, making it easier for readers to comprehend the outcomes of the formulations.
5) Surface:
Surface relates to the outer area of the microspheres being characterized in the study. The surface morphology, observed through scanning electron microscopy, reflects the formulation’s structural integrity and influences drug release rates as well as the floating capabilities crucial for sustained drug delivery.
6) Medium:
Medium refers to the dissolution medium used during the in vitro release studies, typically 0.1 N HCl for simulating gastric conditions. The choice of medium is critical for comprehensively evaluating how the microspheres interact with the gastrointestinal environment and the drug's subsequent bioavailability.
7) India:
India represents the country where the research is conducted. It signifies the geographical and cultural context influencing pharmaceutical studies, including the availability of raw materials, the healthcare challenges faced by its population, and the regulatory frameworks governing drug development.
8) Life:
Life is inherently linked to health and well-being, particularly in the context of chronic diseases like diabetes. The development of glipizide-loaded microspheres aims to improve quality of life by offering a more effective therapeutic strategy that enhances medication adherence and management of blood sugar levels.
9) Transformation (Transform, Transforming):
Transform denotes the intended change in drug formulation from a conventional to a controlled release system. This transformation is aimed at improving pharmacokinetic properties, increasing therapeutic efficacy, and reducing the frequency of dosages required for effective diabetes management.
10) Activity:
Activity usually relates to the therapeutic action of the drug. In this study, it specifically refers to the hypoglycemic activity of glipizide, which is measured through its impact on lowering blood glucose levels, an essential parameter in evaluating its effectiveness.
11) Water:
Water is a universal solvent and a crucial component in pharmaceutical formulations. In this research, it is used during the preparation and characterization of microspheres, as well as in the dissolution medium, highlighting its role in drug release and stability assessments.
12) Measurement:
Measurement refers to the quantitative assessment of various parameters throughout the study, such as drug entrapment efficiency and blood glucose levels. Accurate measurements are critical for determining the success of the formulations and adherence to therapeutic goals in diabetes treatment.
13) Discussion:
Discussion encompasses the analysis and interpretation of the study's findings. It synthesizes data regarding formulation performance and its implications for clinical use, helping to contextualize the results within the broader field of pharmaceutical science and diabetes management.
14) Tamilnadu (Tamil-nadu):
Tamil Nadu is a state in India where the research is conducted. Its educational and research institutions, such as Nandha College of Pharmacy, play a pivotal role in pharmaceutical development, contributing local expertise to advancements in drug delivery technologies.
15) Substance:
Substance refers to any material that has a defined composition, which in this context includes the polymers (HPMC and Eudragit RS 100) used in drug formulation. The choice of substance directly impacts the microsphere's performance, stability, and drug release characteristics.
16) Container:
Container indicates the vessels used to hold the formulated microspheres during various stages of the study, such as during stability testing. Proper selection of containers is vital to prevent contamination and ensure accurate assessments of the formulations' qualities over time.
17) Observing:
Observing involves carefully monitoring the behaviors and characteristics of the floating microspheres during experiments. Observational techniques contribute to understanding how structural changes or environmental factors influence drug release profiles and overall system efficacy.
18) Tanjavur:
Tanjavur is a city in Tamil Nadu where Sastra University is located. This geographic location emphasizes the academic contributions to pharmaceutical research and highlights the collaboration between educational institutions and local pharmaceutical industries in advancing drug formulation techniques.
19) Vomiting:
Vomiting is a side effect associated with many medications, including glipizide. Understanding potential adverse reactions is crucial during product development, leading researchers to engineer formulations that mitigate gastrointestinal discomfort while maximizing therapeutic outcomes for patients.
20) Swelling:
Swelling in the context of drug delivery typically refers to the hydration and expansion of polymeric matrices. This characteristic is essential in controlled release formulations, affecting the rate and pattern of drug release from floating microspheres in the gastric environment.
21) Disease:
Disease signifies the medical conditions being addressed by the research—specifically, diabetes mellitus. This expansive health issue affects millions globally, motivating the development of effective drug delivery systems like the floating microspheres to improve patient care and treatment efficacy.
22) Shastra (Sastra):
Sastra University represents a key academic institution involved in the study, contributing to pharmaceutical research and development. Its role is critical for fostering innovation and scientific inquiry in drug formulation, particularly in local contexts like diabetes management.
23) Nausea:
Nausea is a common side effect encountered in diabetes treatments, often leading to reduced compliance. Formulating glipizide into floating microspheres aims to minimize side effects like nausea and enhance patient adherence to medication regimens.
24) Nature:
Nature relates to the inherent properties of substances and the pharmaceuticals under study. Understanding the physicochemical characteristics of glipizide and the polymers used is critical for successful formulation and to predict their behavior within the human body.
25) Animal:
Animal refers to the Wistar rats used in the in vivo studies to assess the efficacy of the glipizide microspheres. Animal studies are pivotal in bridging preclinical research to human applications, validating the safety and therapeutic effectiveness of new formulations.
26) Glass:
Glass denotes the material of containers used in laboratory settings for conducting formulations, experiments, or stability studies. The inert nature of glass prevents reactions with substances being tested, ensuring accurate and reliable results in drug formulation research.
27) Death:
Death indicates the critical outcome of poorly managed diabetes and highlights the urgency of developing effective drug delivery systems. The research is driven by the need to mitigate life-threatening complications associated with chronic diseases through innovative therapies.
28) Tamil:
Tamil refers to the language and cultural context that may influence the pharmaceutical research environment in Tamil Nadu, India. It underscores the local heritages and practices that can shape healthcare perspectives and pharmaceutical sciences within the region.
29) Nadu:
Nadu is part of the name Tamil Nadu and denotes the state identity. It is relevant in the context of local healthcare initiatives, educational programs, and research contributions fostering developments in drug delivery systems across India's southern region.
30) Food:
Food interacts with the pharmacokinetics of drugs, including glipizide. The timing and formulation of medications must consider food intake, influencing absorption rates and effectiveness, particularly in medications that require administration relative to meals for optimal performance.
31) Heap:
Heap metaphorically relates to the collection or aggregation of microspheres during experiments. Proper arrangement and collecting techniques are critical for ensuring the consistency and accuracy of dosage forms in evaluating the floating properties and release profiles of microspheres.
32) Wall:
Wall describes the structural component of the microsphere that contains the drug. The material properties of the microsphere wall determine the drug's release characteristics, affecting the overall efficacy of floating drug delivery systems designed to enhance therapeutic outcomes.
33) Gold (Golden):
Gold represents the high standards and quality expected in pharmaceutical research and formulation processes. The phrase ‘gold standard’ often implies rigorous validation and best practices in producing dosage forms like the floating microspheres, ensuring reliable therapeutic effectiveness.
34) Coma:
Coma is a severe medical condition that may result from uncontrolled diabetes. The research underscores the importance of developing effective drug delivery systems to prevent such critical outcomes and improve the management strategies for patients living with diabetes.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Glipizide loaded floating microsphere’. Further sources in the context of Science might help you critically compare this page with similair documents:
Stability study, Particle size analysis, Hypoglycemic effect, Scanning Electron Microscopy (SEM), Angle of repose, Controlled drug release.