Bioadhesive Microspheres: Preparation, Characterization, and Applications

a review on preparation and in-vitro characterization

| Posted in: Science

Journal name: World Journal of Pharmaceutical Research
Original article title: Bioadhesive microspheres
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: a review on preparation and in-vitro characterization

Original source:

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Author:

Pawan Chaware, Sanjay Sharma, Anil Bhandari, Akanksha Garud, Navneet Garud


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Bioadhesive microspheres

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research

Copyright (license): WJPR: All rights reserved


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Summary of article contents:

Introduction

Microspheres have emerged as significant tools in drug delivery systems, enhancing both oral and parenteral controlled release mechanisms. The integration of mucoadhesion into these systems has garnered particular attention due to its capability to prolong the residence time of microspheres at targeted absorption sites, thereby improving drug bioavailability. This review article discusses various preparation methods of microspheres, their in-vitro characterization, and their applications in the pharmaceutical field.

The Importance of Mucoadhesion in Drug Delivery

Mucoadhesion refers to the ability of certain polymers to adhere to mucosal surfaces when hydrated. This property is critical in drug delivery systems, as it enables the targeted application of drugs to specific regions within the body for extended periods. By increasing the contact time of the drug at absorption sites, mucoadhesive microspheres facilitate enhanced drug uptake and bioavailability, which, in turn, leads to improved patient compliance by reducing dosing frequency. This aspect of mucoadhesion highlights its importance in designing effective drug delivery systems.

Methods of Preparation of Microspheres

Various methods are employed to prepare microspheres, including thermal cross-linking, glutaraldehyde cross-linking, and ionic gelation techniques. For instance, in the thermal cross-linking method, chitosan is used alongside citric acid as a cross-linker, while glutaraldehyde can also effectively cross-link chitosan in an emulsion system. Each preparation method influences the properties of the microspheres, such as their morphology and drug release profiles, making the choice of method critical to achieving desired characteristics.

In-Vitro Evaluation Techniques

Characterizing microspheres is essential to understanding their functionality. Techniques such as Fourier Transform Infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and tests for entrapment efficiency, drug loading, and swelling index provide insight into microsphere properties. Additionally, in-vitro mucoadhesion tests and dissolution studies evaluate the performance of microspheres in simulated physiological conditions, ensuring they meet necessary therapeutic requirements.

Conclusion

Bioadhesive microspheres represent a promising advancement in drug delivery systems, effectively enhancing the bioavailability of therapeutic agents. Through various preparation techniques and thorough in-vitro evaluations, these systems can be optimized for specific applications, providing significant benefits in controlled and sustained release formulations. The ability to tailor microsphere properties through different methods and evaluations emphasizes their versatility and potential impact in pharmaceutical applications.

FAQ section (important questions/answers):

What are bioadhesive microspheres used for in drug delivery?

Bioadhesive microspheres enhance drug delivery by prolonging the residence time at absorption sites, improving drug bioavailability, and targeting specific body regions for extended periods.

What methods are commonly used to prepare microspheres?

Microspheres can be prepared using various methods, including thermal cross-linking, solvent evaporation, ionic gelation, emulsification phase separation, spray drying, and hot melt microencapsulation, among others.

What is the significance of mucoadhesion in drug delivery systems?

Mucoadhesion is crucial as it allows dosage forms to adhere to mucosal surfaces, enhancing the contact between drug delivery systems and absorption sites, which can improve therapeutic effectiveness.

How are the physicochemical properties of microspheres evaluated?

The physicochemical properties of microspheres are evaluated through techniques like scanning electron microscopy (SEM) for morphology, Fourier-transform infrared (FTIR) spectroscopy for drug-polymer interactions, and dissolution studies.

What applications do microspheres have in pharmaceuticals?

Microspheres are used in controlled release formulations, enteric-coated dosage forms, protecting drugs from environmental factors, and reducing the volatility or toxicity of substances.

How is the drug entrapment efficiency of microspheres determined?

Entrapment efficiency is calculated by comparing the amount of drug actually loaded in the microspheres to the theoretical drug content, expressed as a percentage.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Bioadhesive Microspheres: Preparation, Characterization, and Applications”. 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 'drug' refers to any substance that can alter physiological processes in the body. In the context of microspheres, drugs are often encapsulated within these systems to achieve controlled or targeted delivery, enhancing therapeutic effectiveness while potentially reducing side effects associated with conventional drug administration methods.

2) Water:
Water is a fundamental solvent in pharmaceutical formulations, particularly relevant in the context of microspheres preparation. Many microsphere formulations involve aqueous dispersions where water acts as a medium to dissolve or disperse ingredients, facilitate emulsion formation, and influence the properties of resulting microspheres.

3) Surface:
The 'surface' of microspheres is critical in determining their interactions with biological membranes and other materials. Surface characteristics such as roughness, charge, and chemical functional groups affect mucoadhesion, release patterns of encapsulated drugs, and overall performance of the microencapsulation system in drug delivery applications.

4) Swelling:
Swelling refers to the increase in volume or size of microspheres upon contact with fluids. This property is essential in understanding drug release kinetics. A higher swelling index can indicate better hydration and hence, a potential for enhanced drug release in response to physiological conditions.

5) Substance:
In pharmaceutical sciences, a 'substance' denotes any matter or material used in formulations, which may include active pharmaceutical ingredients (APIs), excipients, and polymers. The characteristics of these substances directly influence the stability, efficacy, and safety of drug delivery systems such as microspheres.

6) India:
India is a significant hub for pharmaceutical research and development, particularly in areas such as drug delivery systems. The research outlined in the article highlights contributions from Indian institutions, emphasizing the country’s role in advancing systems like bioadhesive microspheres for various pharmaceutical applications.

7) Science (Scientific):
The term 'science' encompasses a systematic enterprise that builds and organizes knowledge in the form of testable explanations and predictions about the universe. In this context, the study of bioadhesive microspheres integrates fields like chemistry, biology, and material science to improve drug delivery systems.

8) Glass:
Glass is often used in laboratory settings to create containers and apparatus for formulating and testing microspheres. For instance, glass slides are used for mounting samples during analysis, and glass beakers are common for mixing and reacting components in microsphere preparation processes.

9) Study (Studying):
The term 'study' indicates a systematic investigation aimed at discovering or interpreting facts. In scientific literature, including the review on bioadhesive microspheres, studies elucidate methods, characterizations, and applications of various formulations, contributing to the advancement of knowledge in drug delivery technologies.

10) Pur:
The term 'poor' can imply inadequate or suboptimal performance of a microsphere formulation. This context is important as it highlights challenges in drug delivery systems, where certain formulations may not meet therapeutic goals due to low drug encapsulation, ineffective release profiles, or insufficient bioadhesion.

11) Developing:
The term 'developing' relates to the process of creating and optimizing new formulations or systems. In pharmaceutical contexts, developing new bioadhesive microspheres involves research, experimentation, and refinement to enhance drug delivery capabilities, targeting efficiencies, and overall therapeutic outcomes.

12) Medium:
The term 'medium' refers to a surrounding environment in which biological or chemical processes occur. In microsphere formulation, various media such as aqueous solutions, oils, or gels are critical in determining the properties and behavior of microspheres during preparation and testing.

13) Road:
The term 'road' may refer to both literal and metaphorical pathways. In the context of pharmaceutical development in India, it can symbolize the journey of research and innovation undertaken by scientists and institutions in advancing drug delivery systems like bioadhesive microspheres along a path of scientific progress.

14) Biodegradable:
Biodegradable materials are those that can be broken down naturally by microorganisms. In the context of microspheres, biodegradable polymers are important for developing drug delivery systems that minimize environmental impact and ensure safe degradation in the body, aligning with sustainable pharmaceutical practices.

15) Performance:
Performance in relevant studies indicates how well microspheres function as drug delivery systems. This encompasses aspects such as drug release rates, bioadhesion properties, stability, and efficiency of targeted delivery, influencing the overall therapeutic effectiveness of the encapsulated drugs.

16) Transformation (Transform, Transforming):
To 'transform' relates to the process of changing a substance into a different form, often in order to improve its properties. In drug delivery formulations, transforming conventional drugs into microspheric forms enhances their bioavailability and therapeutic effects by providing controlled release mechanisms.

17) Detachment:
Detachment in this context refers to the process of microspheres releasing from biological surfaces after applying a detachment force. Understanding detachment mechanisms is crucial for evaluating the mucoadhesive properties of microspheres, which directly impact their efficacy in localized drug delivery.

18) Irritation:
Irritation is a common concern in drug formulations, especially for those administered via mucosal routes. Some formulations may cause irritation to tissues, which can be mitigated through the use of microspheres, as they can control and reduce localized drug concentration, minimizing side effects.

19) Container:
A 'container' is a vessel used to hold the materials for microsphere preparation and storage. The choice of container materials is crucial in preventing interactions that could affect the stability or integrity of the encapsulated drugs and the performance of the microspheres.

20) Pesticide:
Pesticides are substances used for preventing, destroying, or controlling pests. The encapsulation of pesticides in microspheres can enhance their controlled release, reduce environmental contamination, and minimize exposure risks, illustrating the utility of microspheres beyond pharmaceuticals into agricultural applications.

21) Toxicity:
Toxicity refers to the degree to which a substance can harm living organisms. In the context of drug delivery systems, especially those involving microspheres, understanding and minimizing toxicity is critical for ensuring patient safety and maximizing therapeutic efficacy.

22) Akanksha (Akanksa, Akamksa, Akamksha, A-kamksha):
Akanksha is a co-author of the reviewed work, highlighting the collaborative nature of scientific research. The contributions of researchers like Akanksha are significant in advancing the understanding and development of novel drug delivery systems, including bioadhesive microspheres.

23) Activity:
Activity in the context of pharmaceuticals generally refers to the effectiveness or potency of a drug. In the formulation of microspheres, activity is influenced by encapsulation efficiency, release patterns, and interaction with biological membranes, all crucial for achieving the desired therapeutic outcome.

24) Gwalior:
Gwalior is the location of one of the contributing institutions in the research on bioadhesive microspheres. The mention of Gwalior emphasizes the geographical diversity and collaborative efforts within India’s scientific community aimed at advancing pharmaceutical technology and drug delivery systems.

25) Quality:
Quality refers to the degree of excellence of a product, including pharmaceuticals. In microsphere formulations, quality is assessed based on parameters such as drug entrapment efficiency, release profiles, stability, and overall performance in targeted drug delivery applications.

26) Heating:
Heating is a crucial step in certain methods of microsphere preparation, influencing properties such as polymer melting, cross-linking, and drug release profiles. Controlled heating techniques can enhance the formation and characteristics of microspheres, aligning them with desired therapeutic functions.

27) Gelatin:
Gelatin is a biopolymer commonly used in the preparation of microspheres due to its biodegradable and biocompatible properties. Utilizing gelatin in drug delivery systems facilitates controlled release mechanisms and enhances the bioavailability of encapsulated drugs in various routes of administration.

28) Sharman (Sarma, Sharma, Sarman):
Sanjay Sharma is a co-author mentioned in the review, representing the collaborative research efforts in developing bioadhesive microspheres. Each contributor’s expertise plays a vital role in advancing the research, development, and understanding of innovative drug delivery systems.

29) Powder:
The term 'powder' refers to a form of a solid substance composed of finely divided particles. In microsphere formulations, the drug can be in powder form, which is formulated with polymers to create microspheres, influencing characteristics such as release rates and stability.

30) Table:
A 'table' may denote a structured representation of data, often used to summarize results related to the properties of microspheres. Tables in scientific literature provide clear, organized information that aids in the comparison and understanding of various formulation parameters and their effects.

31) Gold (Golden):
Gold is sometimes utilized as a coating agent to improve the conductivity and imaging capabilities during electron microscopy analysis. In the context of microspheres, gold-palladium coatings enhance the visualization and assessment of the morphological characteristics of microspheres using Scanning Electron Microscopy (SEM).

32) Inci (Imci):
Inches are a unit of measurement commonly used in the context of physical dimensions. In the scientific literature, precise measurements of microspheres, including their diameter, are critical for assessing their suitability for specific applications in drug delivery systems.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Bioadhesive Microspheres: Preparation, Characterization, and Applications’. Further sources in the context of Science might help you critically compare this page with similair documents:

Methods of preparation, Drug delivery system, Gastric irritation, Stability study, Hygroscopic properties, Scanning Electron Microscopy, Fourier transform infrared spectroscopy, Scanning electron microscope, Hausner's ratio, Differential scanning calorimetry, Mucosal Layer, Pharmaceutical formulation, Delivery system, Carr's Index, Swelling Index, Bioadhesion, Angle of repose, UV Spectrophotometer, Biocompatible polymer, Solvent evaporation, Microsphere, Environmental hazard, Storage condition.

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