Microcapsule formulation and in-vitro characterization of losartan.
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and in-vitro characterisation of microcapsule of losartan for oral delivery
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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Original source:
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A. K. Rath, S. K. Martha and P. K. Sahu
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and in-vitro characterisation of microcapsule of losartan for oral delivery
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20183-10531
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Summary of article contents:
Introduction
This research article focuses on the development of microcapsules formulated with Losartan, an Angiotensin II receptor antagonist used primarily for treating hypertension. The objective was to create a sustained release microencapsulated dosage form aimed at improving the solubility and bioavailability of Losartan, which is classified as having poor solubility and permeability. By using various polymers such as Eudragit, Hydroxypropyl Methylcellulose (HPMC), and Sodium Alginate, the study aims to enhance the stability of the drug and provide sustained release characteristics to improve patient compliance.
Microencapsulation Process
Microencapsulation is the technique used to enclose a specific core material (in this case, Losartan) within miniature capsules. This procedure is beneficial as it slows down the release of the core substance, thereby ensuring a controlled release over time. Various methods like air suspension, coacervation, and solvent evaporation techniques were explored, with the results indicating that the ionic gelation method successfully produced microcapsules with uniform size and good flow properties. The microcapsules exhibited a sustained release profile, ensuring that patients receive the dosage over an extended period, which translates to better therapeutic efficacy.
Properties and Formulation Evaluation
The study presents a detailed evaluation of the characteristics of the microcapsules, including their particle size, density, and flow properties. The average diameter of the microcapsules ranged from 370 µm to 650 µm, with excellent flowability evidenced by Carr’s index and Hausner ratio values below 15%. These properties are critical as they impact the ease of manufacturing and patient adherence to dosing regimens. Furthermore, the encapsulation efficiency of Losartan within the microcapsules varied, demonstrating the effectiveness of different polymer compositions in trapping the drug.
In Vitro Drug Release Studies
The in vitro drug release profiles of the formulated microcapsules demonstrated a variable rate of drug release, linked to the proportions of the polymer used. Formulation MC8, which contained a higher proportion of Eudragit RS, was noted to exhibit a remarkable sustained release, with only 26.35% of the drug released after three hours, compared to other formulations that released the drug at a faster rate. These results indicate the potential for tailored release profiles through manipulation of polymer types and ratios, supporting the notion of developing personalized medications that ensure optimal therapeutic outcomes.
Conclusion
In conclusion, the formulation of Losartan microcapsules utilizing various biocompatible polymers such as HPMC, Eudragit RL, and Eudragit RS presents a promising strategy for drug delivery systems. The findings suggest that microencapsulation can significantly improve the stability and bioavailability of drugs with poor solubility. The optimized microcapsules display favorable characteristics that support sustained release, thereby enhancing patient compliance and therapeutic efficacy. However, further studies focusing on in vivo testing, long-term stability, and drug-polymer interactions are necessary to substantiate the results and establish a solid foundation for clinical applications.
FAQ section (important questions/answers):
What is the purpose of formulating microcapsules for Losartan?
Microcapsules are designed to enhance the bioavailability and sustain the release of Losartan, an Angiotensin II antagonist used to treat hypertension, thereby improving patient compliance and reducing side effects.
What are the key polymers used in Losartan microcapsule formulation?
The formulation includes polymers such as Eudragit RL, Eudragit RS, HPMC, and sodium alginate, which aid in creating the microcapsules with sustained release properties.
How were the Losartan microcapsules prepared?
Losartan microcapsules were prepared using the ionic gelation method, where drug and polymers were dissolved in water, then dropped into a calcium chloride solution for curing.
What characteristics were evaluated for the prepared microcapsules?
Characteristics evaluated include particle size, yield, drug content, encapsulation efficiency, flow properties, swelling index, moisture loss, and in-vitro drug release.
What results were observed regarding the drug release from microcapsules?
The microcapsules exhibited a sustained drug release profile, with formulation MC8 releasing only 26.35% of Losartan over a three-hour period, indicating effective sustained release.
What are the advantages of using microencapsulation for drug delivery?
Microencapsulation allows for sustained release of drugs, better stability, enhanced patient compliance, reduced dosing frequency, and protection of drugs from environmental factors.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Microcapsule formulation and in-vitro characterization of losartan.”. 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 term 'drugs' encompasses a broader category, including Losartan and other medications within pharmacology. The study of drugs like Losartan helps to understand pharmacotherapeutic advancements aimed at controlling conditions like hypertension through innovative delivery systems such as microcapsules.
2) Table:
The word 'Table' refers to organized data representations throughout the article. For instance, several tables present formulation designs, yields, and moisture loss properties for losartan microcapsules. Such tables facilitate comparison and analysis, crucial for interpreting experimental results of drug formulations and aiding further research.
3) Study (Studying):
In the context of the article, 'study' denotes the methodological approach taken to investigate the formulation of losartan microcapsules. It involves various scientific methods such as preparation techniques, in vitro characterization, and dissolution tests to evaluate the efficiency and effectiveness of the formulated microcapsules in achieving sustained drug release.
4) Science (Scientific):
The plural term 'sciences' within the article indicates the multidisciplinary approach taken in drug formulation studies, combining principles of chemistry, biology, and pharmaceutical sciences to understand drug delivery systems and optimize them for better patient outcomes.
5) Swelling:
The term 'swelling' refers to the increase in volume or size of the microcapsules when placed in water. The swelling index indicates the mucoadhesive properties and water absorption capacity of the microcapsules, which are vital for their effectiveness in sustaining drug release and ensuring better interaction within the gastrointestinal tract.
6) Powder:
'Powder' relates to the physical state of the polymers and excipients utilized in the formulation of losartan microcapsules. Various powders, such as sodium alginate and Eudragit, are combined to create the microcapsules, affecting their physical properties, bioavailability, and overall performance in drug delivery.
7) Water:
In the article, 'water' is essential for the dissolution processes and as a medium used in preparation techniques, particularly in the ionic gelation method. It serves as a solvent to create microcapsules, and its interaction with polymers directly impacts the swelling and release characteristics of the formulation.
8) Calcutta:
Calcutta refers to a location in India that is significant as it represents the source of certain chemicals and instruments mentioned in the study. It emphasizes the location of pharmaceutical companies or research institutions involved in producing materials necessary for conducting the drug formulation studies.
9) Pur:
'Poor' describes the solubility and permeability characteristics of Losartan, highlighting one of the critical challenges addressed in the study. The formulation of microcapsules aims to improve these properties significantly, seeking to enhance the bioavailability and therapeutic effectiveness of the drug.
10) Substance:
'Substances' denote the various materials and compounds, including active drugs, excipients, and polymers used in the formulation of microcapsules. Analyzing substances and their interactions is crucial in determining the efficacy and stability of drug delivery systems.
11) Medium:
'Medium' in the context of the article usually denotes dissolution media, such as 0.1N HCl, utilized during in vitro drug release studies. The choice of medium is critical in simulating physiological conditions to evaluate the behavior and efficacy of the drug upon release from microcapsules.
12) Blood:
Blood is relevant due to its role in drug distribution and pharmacokinetics once the microcapsules are ingested and release their component drugs. The physiological interactions between the drug and the circulatory system impact how effectively the drug exerts its therapeutic effects.
13) Life:
'Life' in this context refers to pharmacokinetic aspects, particularly the drug's half-life and duration of action. Understanding drug life is crucial to develop sustained release formulations that maintain therapeutic levels over extended periods, contributing to better patient adherence and treatment outcomes.
14) New Delhi:
New Delhi serves as a reference point for pharmaceutical research and development in India. The mention indicates the geographical relevance where studies and innovations concerning drug delivery systems occur, promoting collaboration among various research institutions and pharmaceutical companies engaged in such work.
15) Container:
'Container' relates to the storage and stability of the formulated microcapsules. Keeping the encapsulated drugs appropriately protected helps maintain their integrity and efficacy. Containers play a vital role in ensuring microcapsules avoid environmental factors that may degrade the active ingredients.
16) Relative:
The term 'relative' is used to describe the relationships and proportions between the polymer types, drug, and other formulation components affecting the microcapsule's release characteristics. It emphasizes the importance of balancing these variables to achieve optimal performance in drug delivery systems.
17) Surface:
'Surfaces' highlight the interactions between microcapsules and biological environments, such as epithelial tissues in the gastrointestinal tract. Understanding surface properties of microcapsules is vital for ensuring optimal drug release rates and enhancing patient compliance and therapeutic effectiveness.
18) Delhi:
Delhi, similar to New Delhi, represents a significant region in India that contributes to pharmaceutical education and healthcare. It serves as a hub for research institutions and industries, acting as a potential area for sourcing materials and talent in developing innovative drug delivery solutions.
19) Kumar:
'Kumar' appears as a reference to researchers or authors in the context of pharmacological advancements. It underscores the collaborative nature of research, where multiple scientists contribute to studies aimed at improving drug delivery systems and enhancing treatment strategies for patients.
20) Salt (Salty):
The term 'salt' is relevant in the context of drug formulations, especially as it pertains to the characteristics of drug compounds. Understanding the salt forms of drugs helps in predicting solubility, permeability, and overall bioavailability, which can significantly influence the microencapsulation process.
21) Discussion:
'Discussion' generally contains interpretations of results obtained from the experimental studies. It delves into analyzing the outcomes, understanding implications of findings, and suggesting future research directions based on data, diagnostics, and formulated hypotheses derived from microencapsulation of Losartan.
22) Jeypore:
Jeypore is the location of the institution where the research was conducted. This reference also emphasizes the regional context of the study, showcasing the diverse geographical areas contributing to pharmaceutical innovation and the educational landscape in India.
23) Rasala:
'Rasala' refers to an author whose works might be influential within the context of the article's framework. This highlights the collaborative nature of scientific research, where numerous contributors provide insights and data that enhance understanding in areas such as drug delivery systems.
24) India:
India is significant as it represents a growing hub of pharmaceutical research and development, contributing to global healthcare solutions. The research conducted in this country may showcase innovations reflecting local health issues and promote novel drug delivery systems like the microencapsulation of drugs.
25) Glass:
'Glass' pertains to laboratory equipment, such as beakers, vials, or containers used during experiments. Glassware is essential in maintaining the integrity of the substances being studied and ensures accurate measurements and safe handling during the drug formulation and testing processes.
26) Food:
'Food' indicates the relevance of excipients and polymers used in the formulations, many of which are derived from edible substances. The interplay between pharmaceutical applications and food science emphasizes safety, efficacy, and biocompatibility in developing drug delivery systems.
27) Pain:
The term 'pain' can relate to the pharmacological impact of Losartan in alleviating symptoms associated with hypertension. Understanding the therapeutic applications aids in emphasizing the significance of sustained release formulations in effectively managing health conditions related to pain and discomfort.
28) Transformation (Transform, Transforming):
'Transformation' in the article refers to changes undergone by the drug or polymers in the microencapsulation process. The modifications are critical in enhancing drug solubility, permeability, and overall bioavailability, showcasing the dynamic nature of pharmaceutical formulations in drug delivery science.
29) Biodegradable:
'Biodegradable' signifies the environmental aspects of excipients and polymers developed for drug delivery. Utilizing biodegradable materials helps reduce ecological impacts, promote safety in pharmaceutical practices, and align with the growing demand for sustainable and eco-friendly drug formulation technologies.
30) Pharmacology:
The term 'pharmacology' encompasses the study of drugs, their effects on biological systems, and mechanisms of action. This field of science is critical in understanding how drugs like Losartan interact within the body and informs practices surrounding drug formulation and patient care.
31) Performance:
'Performance' relates to how well the formulated microcapsules deliver the drug in a sustained and controlled manner. The efficacy of the drug release profiles observed during testing will determine the success of the microencapsulation process in meeting therapeutic objectives.
32) Surrounding:
'Surrounding' addresses the environmental factors that can affect the stability and release characteristics of the microcapsules. Understanding how external conditions, such as humidity and temperature, influence drug formulations is vital for optimizing storage and usage protocols for better patient outcomes.
33) Measurement:
'Measurement' is critical in experimental research, particularly regarding the quantification of drug content, encapsulation efficiency, and release rates. Accurate measurements ensure reliable data that can be analyzed to assess the formulation's effectiveness and offer insights for further improvements.
34) Toxicity:
'Toxicity' addresses the safety aspects associated with drug formulations, particularly the potential adverse effects of the constituents. Evaluating toxicity ensures that microcapsules and their materials are safe for use, aligning with regulatory standards for pharmaceutical products and patient safety.
35) Dressing:
'Dressing' may refer to the use of microcapsules in topical formulations or drug delivery systems that can aid wound healing. Its relevance in the article showcases potential applications beyond oral delivery, indicating the versatility of microencapsulation technology in various therapeutic contexts.
36) Pursuing:
'Pursuing' indicates the ongoing nature of research and development in the field of drug delivery. It emphasizes the effort and dedication in improving formulations and finding solutions to complex pharmaceutical challenges, such as those faced with drugs like Losartan.
37) Sandhya (Samdhya, Shandhya):
'Sandhya' may refer to a researcher or author contributing insights within the study context. Acknowledging contributors enhances the credibility of the research, promotes collaboration within the scientific community, and highlights the diverse expertise involved in the formulation development process.
38) Quality:
'Quality' emphasizes the standards of drug formulations in terms of efficacy, safety, and stability. Maintaining high-quality benchmarks is crucial in pharmaceutical research to ensure that microcapsules meet therapeutic goals and comply with regulatory requirements for patient treatment.
39) Heating:
'Heating' pertains to processes used within the formulation, including drying and melting requirements of certain polymers. Understanding these temperature effects is essential as it impacts the physical attributes and reactivity of microcapsules, ultimately influencing drug release performance.
40) Filling (Filled):
'Filling' indicates the process associated with encapsulating the drug within the microcapsule matrix. Proper filling techniques are essential to ensure consistent distribution of the drug, achieving uniform dosages and optimizing the overall performance of the microencapsulated products.
41) Allergy:
'Allergy' refers to the potential adverse reactions that certain excipients or drugs may cause. In pharmaceutical formulations, assessing allergic properties is crucial to ensure patient safety and avoid hypersensitivity reactions, which can compromise the efficacy and acceptance of the microencapsulated product.
42) Gelatin:
'Gelatin' may relate to a type of excipient or polymer material used in microencapsulation processes. Understanding various excipients, including gelatin, is essential, as they impact the drug's release characteristics, stability, and overall performance in therapeutic applications.
43) Company:
'Company' represents the pharmaceutical industry entities involved in the procurement of materials, formulation processes, or research studies. The quality of companies selected for sourcing materials can impact the overall success and reliability of the formulated microcapsules.
44) Dahiya:
'Dahiya' appears as a contributor within pharmaceutical research, highlighting collaborative efforts in the study. Acknowledging such individuals emphasizes the importance of diverse expertise in advancing drug delivery systems and enhancing therapeutic solutions in practice.
45) Thomas:
'Thomas' refers to a scholar or researcher involved in previous works related to drug formulation or pharmacology, underscoring the collaborative nature of scientific research. Referencing prior studies strengthens the support and background for the current investigation into losartan microcapsules.
46) Martha:
'Martha' signifies one of the authors involved in the study or project, reflecting collaborative research efforts in advancing the field of drug delivery systems. Collaborative work aids in pooling expertise to achieve comprehensive findings and insights into the formulation and characterization of microcapsules.
47) Bitter:
'Bitter' commonly describes the unpleasant taste associated with certain medications, including Losartan. Microencapsulation techniques can effectively mask these flavors, resulting in improved patient compliance, particularly in administering critical medications that may have unpalatable tastes.
48) Cotton:
In pharmaceutical terms, 'cotton' often relates to its source material for cellulose used in various formulations. The derivation of cellulose from cotton underlies several polymers, such as HPMC, highlighting the importance of natural resources in excipient development for drug delivery systems.
49) Indian:
The term 'Indian' denotes the geographical and cultural context of the research conducted in India. It emphasizes the country's involvement in pharmaceutical advancements and the importance of local studies in addressing public health concerns through innovative drug delivery approaches.
50) Gupta:
Gupta signifies a researcher connected to the study, representing the collaboration essential in scientific endeavors. Collaborators like Gupta contribute insights and expertise to advance the goal of optimizing drug delivery systems and enhancing therapeutic effectiveness in patient care.
51) Patil:
Patil indicates a contributor within the pharmaceutical research community, adding diverse perspectives and expertise to the study. The inclusion of various collaborators underscores the multifaceted approach taken to innovate and refine microencapsulation processes for effective drug formulation.
52) Nayak:
'Nayak' references a researcher involved in related pharmaceutical studies, enhancing the collaborative effort in the field. Acknowledging contributors like Nayak reinforces the collective endeavors to improve drug therapies, focusing on advanced delivery systems and maximizing patient outcomes.
53) Beta:
'Beta' relates to the therapeutic or pharmacological context of drug classifications. Understanding beta blockers or beta receptors may be essential in studies related to hypertension and the pharmacodynamics of drugs like Losartan, showcasing the significance in addressing cardiovascular health.
54) Rani:
'Rani' indicates collaboration in the research context, contributing to the work presented in the article. The mention emphasizes the need for collective scientific efforts aimed at formulating effective drug delivery systems and advancing treatment methodologies in pharmacy.
55) Bile:
Bile, being a digestive fluid produced by the liver, highlights its relevance in pharmacokinetics and drug absorption. Understanding how drugs like Losartan are metabolized and excreted can provide essential insights into optimizing the formulation for effective therapeutic strategies.
56) Sahu:
'Sahu' refers to one of the authors or researchers involved in the development of the study. It reflects collective involvement in conducting research aimed at advancing drug formulation techniques and improving therapeutic interventions through collaboration and shared expertise.
57) Wall:
In the context of microencapsulation, 'wall' pertains to the protective coating surrounding the drug core. The encapsulation wall plays a crucial role in controlling the drug's release properties, stability, and ensuring protection against environmental factors, thereby influencing overall drug efficacy.
58) Line:
'Line' may refer to a set of research studies or methodologies explored in the article. It indicates continuity in scientific exploration, encompassing a spectrum of approaches designed to improve drug delivery and pharmacological outcomes through innovative formulations.