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Beschreibung

The book provides essential insights into the revolutionary potential of nanotechnology in medicine, exploring innovative approaches that harness natural materials for targeted and effective disease management.

Nanotechnology has emerged as an innovative field with the potential to transform various sectors, including medicine and allied health sciences. Bioactive nanotherapeutics, a specific area within nanotherapeutics, utilizes natural materials or biomimetic designs to offer distinct advantages such as targeted drug delivery, biocompatibility, and improved therapeutic efficacy. These bioactive-based nanotherapeutics are used in the treatment and management of various diseases.

Bioactive-Based Nanotherapeutics explores this rapidly growing field of therapeutics. It presents a broad overview of the fundamentals of bioactive nanomaterials, their design strategies, and their therapeutic applications. Leading experts from different disciplines have contributed chapters that explore a diverse range of topics, including the basics of bioactive nanotherapeutics, isolation methods of different bioactive compounds, and formulation developments. This volume addresses the importance of nanotechnology for the treatment and management of different diseases, including nasal, gastrointestinal, rectal, and transdermal diseases.

Readers will find the book:

  • Provides scientific research and evidence that supports the effectiveness of bioactive-based nanocarriers in treating diseases;
  • Explores actionable steps and real-life scenarios to illustrate the practical benefits;
  • Provides a comprehensive guide that explains the holistic approach, explaining health-related applications of bioactive-based nanoformulations.

Audience

Pharmacists, biologists, chemists, doctors, academics, and industry professionals interested in holistic and bioactive-based methods for disease treatment.

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Veröffentlichungsjahr: 2025

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Table of Contents

Cover

Table of Contents

Series Page

Title Page

Copyright Page

Preface

1 Basics of Nano-Bioactive Compounds and Their Therapeutic Potential

1.1 Introduction

1.2 Therapeutic Potential of Bioactive Compounds

1.3 Extraction Techniques for Obtaining Bioactive Compound

1.4 Novel Delivery Approach for Bioactive Compounds

1.5 Electrospinning

1.6 Micro- and Nanoencapsulation of Bioactive Compounds

1.7 Polymeric Nanoparticles (NPs)

1.8 Solid Lipid Nanoparticles

1.9 Nanoemulsions

1.10 Nanocrystals

1.11 Phytosomes

1.12 Therapeutic Potential of Nano-Bioactive Compounds

1.13 Conclusion

References

2 Recent Techniques for Isolation of Bioactive Components from Plants

2.1 Introduction

2.2 Extraction Methods

2.3 Recent Chromatographic Methods

2.4 Applications of Two-Dimensional Chromatographic Approaches

2.5 Hyphenated Techniques

2.6 Conclusion

References

3 Bioactive-Based Nanocarriers for Inflammatory Diseases

3.1 Inflammation and Diseases

3.2 Nanocarriers as Drug Delivery System

3.3 Nanocarriers and Inflammation

3.4 Inflammation in Central Nervous System

3.5 Ophthalmological Inflammation

3.6 Cardiovascular Inflammation

3.7 Respiratory Inflammation

3.8 Inflammation in Gastric System

3.9 Excretory System Inflammation

3.10 Inflammation of the Reproductive System

3.11 Inflammation Associated with Dermatology

3.12 Muscular Inflammation

3.13 Skeletal Inflammation

3.14 Applications of Nanocarriers in Inflammation

3.15 Conclusion

References

4 Bioactive-Based Nanocarriers for Dermal Diseases

4.1 Introduction

4.2 Skin Anatomy and Physiology: Implications for Drug Delivery

4.3 Barrier Functions of the Skin

4.4 Transdermal Permeation Challenges

4.5 Factors Influencing Dermal Drug Penetration

4.6 Role of Nanocarriers in Enhancing Drug Penetration

4.7 Types of Bioactive-Based Nanocarriers

4.8 Design Principles and Fabrication Techniques

4.9 Characterization of Bioactive-Based Nanocarriers

4.10 Applications in Diverse Dermal Diseases

4.11 Preclinical Studies:

In Vivo

and

In Vitro

4.12 Challenges and Future Directions

4.13 Conclusion

References

5 Nano-Based Nasal Delivery of Biomacromolecules: A Myriad of Opportunities

5.1 Biomacromolecules

5.2 Characteristics of Biomacromolecules and Delivery Challenges

5.3 Opportunities of Nasal Route

5.4 Main Factors in Nasal Cavity Affecting Delivery of Biomacromolecules

5.5 Nano-Based Delivery Systems as an Efficient Strategy to Improve Intranasal Administration of Biomacromolecules

5.6 Proof of Concept: Biomacromolecules Administered by Intranasal Nano-Based Delivery Systems

5.7 Safety Considerations

5.8 Conclusion

References

6 Bioactive-Based Nanocarriers for Ocular Application

6.1 Introduction

6.2 Barriers and Route of Ocular Drug Delivery

6.3 Nanoparticles in Ocular Diseases Therapy

6.4 Organic Nanocarriers

6.5 Inorganic Nanocarriers

6.6 Benefits of Bioactive-Based Nanoparticles for Occular Application

6.7 Challenges and Future Considerations

6.8 Conclusion

Acknowledgment

References

7 Bioactive-Based Nanocarriers for Gastrointestinal System Disease

7.1 Introduction

7.2 Types of Bioactive-Based Nanocarriers

7.3 Design and Fabrication of Bioactive-Based Nanocarriers

7.4 Bioactive Molecules for Targeting Gastrointestinal Diseases

7.5 Preclinical Studies and Clinical Trials

7.6 Therapeutic Applications of Bioactive-Based Nanocarriers

7.7 Safety and Toxicity Considerations

7.8 Challenges and Future Perspectives

7.9 Conclusion

References

8 Bioactive-Based Nanocarriers for Cancer Treatment and Targeting

8.1 Overview of Current Global Epidemiology and Prevalence of Cancer

8.2 Comparison and Contrast Between Bioactive-Based Nanocarriers and Other Cancer Treatment

8.3 Mechanism(s) for Cancer Treatment and Targeting Using Bioactive Compounds

8.4 Bioactive-Based Nanocarriers for Treatment and Targeting of Different Categories of Cancer

8.5 Limitations of Bioactive-Based Nanocarriers for Cancer Treatment and Targeting

8.6 Future prospects

8.7 Conclusion

References

9 Bioactive-Based Nanocarrier for the Management of Infectious Diseases

9.1 Introduction

9.2 Factors Influencing Bioactive Nanocarriers

9.3 Mechanism of Action of Bioactive Nanocarriers in Infection

9.4 Recent Advancements in Bioactive-Based Nanocarrier for Infections

9.5 Beneficial Aspects of Bioactive-Based Nanocarrier Over Conventional Treatment

9.6 Conclusion and Future Prospects

References

10 Bioactive-Based Nanocarriers for Cosmeceuticals

10.1 Introduction

10.2 Nanotechnology in Cosmeceuticals

10.3 Bioactive Ingredients in Cosmeceuticals

10.4 Nanocarriers for Bioactive Delivery

10.5 Applications of Bioactive-Based Nanocarriers in Cosmeceuticals

10.6 Challenges and Future Perspectives

References

11 Bioactive-Based Nanocarriers for CVD

11.1 Introduction

11.2 The Ongoing CVD Crisis

11.3 Bioactive Compounds and Their Role in Cardiovascular Disease (CVD) Prevention and Treatment

11.4 Role of Bioactive Compounds in CVD Prevention

11.5 Bioactive-Based Nanocarriers for Enhanced Drug Delivery

11.6 Challenges and Future Directions

11.7 Conclusion

References

12 Bioactive-Based Nanocarriers for Diabetes

Abbreviations

12.1 Introduction

12.2 Bioactive-Based Nanocarriers in Medicine and Healthcare Including Diabetes

12.3 Significance of Material Selection in Bioactive-Based Nanocarriers

12.4 Targeting Strategies for Diabetes Therapy

12.5 Benefits of Targeted Drug Delivery in Diabetes

12.6 Factors Affecting Drug Loading Efficiency and Stability in Encapsulation Systems

12.7 Opportunities for Improving Nanocarrier Performance and Targeting Specificity

12.8 Ethical and Regulatory Considerations

12.9 Challenges and Future Perspectives

12.10 Conclusion

Acknowledgments

References

13 Bioactive-Based Nanocarriers in Management of CNS Diseases

13.1 Introduction

13.2 Principles of Bioactive-Based Nanocarriers

13.3 Overcoming the Blood–Brain Barrier

13.4 Nanocarriers of Hope: Revolutionizing Neurodegenerative Disease Management

13.5 Applications in Neurodegenerative Diseases

13.6 Bioactive-Based Nanocarriers for Brain Tumor Therapy

13.7 Bioactive-Based Nanocarriers in Stroke Management

13.8 Traumatic Brain Injury and Nanocarrier Interventions

13.9 Imaging and Diagnostic Capabilities

13.10 Current Preclinical and Clinical Advancements

13.11 Future Prospects and Challenges

13.12 Conclusion

References

14 Nanocarrier Applications for the Delivery of Bioactives for Topical Wound Healing

14.1 Introduction

14.2 Physiology of Wound Healing

14.3 Skin Drug Delivery for Wound-Healing Applications

14.4 Research on Wound Healing Using Nanocarriers Loaded with Bioactive Materials

14.5 Prospects and Challenges of Nanocarriers in Future Wound Healing

References

15 Bioactive-Based Nanocarriers for Targeting Antimicrobial Resistance

15.1 Introduction

15.2 Development of Antibiotic Resistance

15.3 Mechanism of Antibiotic Resistance

15.4 Current Treatment Approaches to Management Antibiotic Resistance and Challenges

15.5 Phytochemicals in the Management of Antibiotic Resistance

15.6 Phytochemical-Based Nanocarriers for the Management of Antibiotic Resistance

15.7 Mechanism of Phytochemical-Based Nanocarriers in Combating Antibiotic Resistance

15.8 Conclusion and Future Perspectives

References

16 Bioactive Phytochemical–Based Nanocarriers for Targeting Non-Alcoholic Fatty Liver Disease (NAFLD)

16.1 Introduction

16.2 Etiology and Pathophysiology

16.3 Current Treatment Options Available for NAFLD

16.4 Bioactive-Based Nanocarriers: A Treatment Option for NAFLD as Smart Drug Carriers

16.5 Toxicological Concerns of Nanocarriers for NAFLD Therapy

16.6 Merits and Demerits of Bioactive-Based Nanocarriers for NAFLD Treatment

16.7 Conclusion and Future Perspectives

References

17 Bioactive Peptide–Based Nanocarrier and Its Application

17.1 Introduction

17.2 Brief Attention on Peptides

17.3 Bioactive Peptide as Nanocarriers

17.4 Conclusion and Future Outlook

References

18 Bioactive-Based Nanocarriers for the Treatment of Lung Disorders

18.1 Introduction

18.2 Advantages and Challenges of Nanocarriers in Lung Disease Treatment

18.3 Role of Bioactive Nanocarriers in Lung Disease Management

18.4 Bioactive-Based Nanocarriers in Asthma Management

18.5 Bioactive-Based Nanocarriers in COPD Treatment

18.6 Pulmonary Fibrosis and Bioactive Nanocarrier Approaches

18.7 Bioactive Nanocarriers for Cystic Fibrosis Treatment

18.8 Tuberculosis Management with Bioactive-Based Nanocarriers

18.9 Future Perspectives and Conclusion

References

19 Bioactive-Based Nanotherapeutics in Pain Management: A Revolutionary Approach

19.1 Introduction

19.2 Pathophysiology of Pain

19.3 Pain Biomarkers

19.4 Treatment for Pain Management

19.5 Significance of Bioactive Compound–Based Nanotherapeutics in Pain Therapy

19.6 Nanotherapeutics: A New Strategy from the Bioactive Compounds for the Treatment of Pain

19.7 Conclusion

References

20 Bioactive-Based Nanocarriers for Neonatal Drug Delivery System: Enhancing Efficacy and Safety in Neonatal Medicine

20.1 Introduction

20.2 Nanocarrier Design Considerations for Neonatal Use

20.3 Bioactive Components in Nanocarrier Systems

20.4 Enhancing Drug Encapsulation, Stability, and Sustained Release

20.5 Minimizing Toxicity and Immunogenicity

20.6 Exploiting Neonatal Physiology for Targeted Delivery

20.7 Nanocarrier Surface Modification and Ligand Conjugation

20.8 Improving Drug Bioavailability in Neonatal Populations

20.9 Promising Applications of Bioactive-Based Nanocarriers in Neonatal Medicine

20.10 Advancements and Future Perspectives

20.11 Conclusion

References

21 Bioactive-Based Nanocarriers for the Treatments of Obesity: A Novel Approach

21.1 Introduction

21.2 Pathophysiology

21.3 Management of Obesity

21.4 Bioactive Compounds

21.5 Nanotechnology

21.6 Conclusion/Future Perspectives

References

22 Regulatory Aspects of Bioactive-Based Nanocarriers

22.1 Introduction

22.2 The Necessity of Regulating Nanomedicine

22.3 Worldwide Strategies for the Regulation of Nanopharmaceuticals

22.4 Conclusion

References

Index

End User License Agreement

List of Tables

Chapter 1

Table 1.1 Table showing various condition treated by bioactive compound.

Table 1.2 Table showing various types of nanocarriers, its advantages, and dis...

Chapter 3

Table 3.1 Applications of nanocarriers in inflammation.

Chapter 4

Table 4.1 Types of bioactive-based nanocarriers.

Chapter 5

Table 5.1 Comparison of main characteristics of conventional small molecules a...

Table 5.2 Highlights from selected studies evaluating intranasal insulin deliv...

Table 5.3 Highlights from selected studies evaluating intranasal delivery of v...

Table 5.4 Highlights from selected studies evaluating intranasal delivery of n...

Chapter 6

Table 6.1 Organic nanocarrier and its application in the treatment of ocular d...

Table 6.2 Inorganic nanocarrier and its application in the treatment of ocular...

Chapter 7

Table 7.1 Bioactive-based nanocarriers used in GIT disorders.

Chapter 8

Table 8.1 Comparison and contrast between bioactive-based nanocarriers and oth...

Table 8.2 Mechanisms of anti-cancer effects of some bioactive compounds derive...

Chapter 9

Table 9.1 Comparative evaluation of bioactive and nano-entrapped bioactive.

Table 9.2 Compilation of recent research highlights of different nanocarriers ...

Chapter 10

Table 10.1 Advantages and disadvantages of nanoparticles.

Chapter 11

Table 11.1 Bioactive-based nanocarriers and their applications in cardiovascul...

Chapter 12

Table 12.1 Nanocarrier type with bioactive component.

Chapter 14

Table 14.1 Common conventional dosage forms: limitations and advantages in wou...

Table 14.2 Studies of bioactives delivery

via

nanocarriers for topical wound h...

Chapter 16

Table 16.1 List of drugs used in the treatment of NAFLD [25].

Table 16.2 Phytochemical-loaded nanoparticles used in NAFLD models.

Chapter 17

Table 17.1 Characteristics of solid-lipid nanoparticles [30, 31].

Table 17.2 Depiction and implementation of self-emulsifying carrier system [48...

Table 17.3 Properties and application of polymeric nanocarrier.

Table 17.4 Properties and application of polysaccharide nanocarrier.

Chapter 18

Table 18.1 Nanocarriers employed for the treatment of lung disorders.

Chapter 19

Table 19.1 Nature and potential causes of pain.

Table 19.2 Types of biomarkers with examples for pain.

Chapter 21

Table 21.1 Role of nanocarriers in drug delivery.

List of Illustrations

Chapter 1

Figure 1.1 Various types of bioactive compounds.

Figure 1.2 Therapeutic application of bioactive compounds.

Figure 1.3 Flowchart showing various methods of extraction.

Chapter 3

Figure 3.1 Diseases associated with inflammation.

Figure 3.2 Nanocarriers used for the treatment of inflammation.

Figure 3.3 Etiology of CNS inflammation.

Figure 3.4 Causes of ophthalmological inflammation.

Figure 3.5 Types of respiratory inflammation.

Figure 3.6 Diseases associated with respiratory inflammation.

Figure 3.7 Causes of gastric inflammation.

Figure 3.8 Causes of excretory system inflammation.

Chapter 4

Figure 4.1 Factor influencing dermal drug penetration.

Figure 4.2 Role of nanocarriers in enhancing drug penetration.

Figure 4.3 Characterization of bioactive-based nanocarriers.

Chapter 5

Figure 5.1 Possible effects that can be achieved following intranasal administ...

Figure 5.2 Schematic illustration of nano-based nasal delivery systems for bio...

Chapter 6

Figure 6.1 Illustration of various ocular drug deliveries.

Figure 6.2 Organic nanocarriers used in the treatment of ocular disease.

Figure 6.3 Regions of inorganic nanocarriers.

Chapter 7

Figure 7.1 The structure of liposomes and different methods of preparation of ...

Figure 7.2 Methods of preparation of nanocrystal.

Chapter 8

Figure 8.1 Sources of bioactive compounds.

Chapter 9

Figure 9.1 Nanocarrier role in overcoming drug resistance. The figure comes un...

Figure 9.2 Factors influencing the antimicrobial activity of nanocarrier again...

Figure 9.3 Schematic representation of targeted antibiotic-loaded bioactive NP...

Figure 9.4 Metal oxide nanoparticles (NPs) interaction with microbial biofilm ...

Figure 9.5 (I). P. grandiflora tuber extracts loaded silver nanoparticles (bio...

Figure 9.6 Factors influencing the bioactivity of bioactive nanomaterials. The...

Chapter 10

Figure 10.1 Types of nanocarriers for bioactive delivery.

Chapter 13

Figure 13.1 Types of nanocarrier.

Figure 13.2 Methods of penetration enhancement of BBB.

Chapter 14

Figure 14.1 The most common nano drug delivery systems and nanomaterials utili...

Chapter 16

Figure 16.1 Pathophysiology of NAFLD.

Chapter 17

Figure 17.1 Pharmacological uses of peptides obtained from different sources.

Figure 17.2 Structure and application of liposomal formulations.

Chapter 18

Figure 18.1 Various bioactive-based nanocarriers for the treatment of lung dis...

Chapter 19

Figure 19.1 Classification of pain relief drugs.

Figure 19.2 Nanocarrier preparation with bioactive compound from plant source.

Figure 19.3 Classification of liposome.

Figure 19.4 Different technique of preparation of liposome.

Guide

Cover Page

Table of Contents

Series Page

Title Page

Copyright Page

Preface

Begin Reading

Index

WILEY END USER LICENSE AGREEMENT

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Scrivener Publishing100 Cummings Center, Suite 541JBeverly, MA 01915-6106

Publishers at ScrivenerMartin Scrivener ([email protected])Phillip Carmical ([email protected])

Bioactive-Based Nanotherapeutics

Edited by

Rakesh K. Sindhu

Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, Haryana, India

Sumitra Singh

Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, Haryana, India

and

Evren Algin Yapar

Department of Pharmaceutical Technology, Faculty of Pharmacy, Sivas Cumhuriyet University, Sivas, Türkiye

This edition first published 2025 by John Wiley & Sons, Inc., 111 River Street, Hoboken, NJ 07030, USA and Scrivener Publishing LLC, 100 Cummings Center, Suite 541J, Beverly, MA 01915, USA© 2025 Scrivener Publishing LLCFor more information about Scrivener publications please visit www.scrivenerpublishing.com.

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Library of Congress Cataloging-in-Publication Data

ISBN 978-1-394-28731-4

Front cover images courtesy of Adobe FireflyCover design by Russell Richardson

Preface

Nanotechnology has emerged as an innovative field with the potential to transform various sectors, including medicine and allied health sciences. Bioactive nanotherapeutics, a specific area within nanotherapeutics, utilizes natural materials or biomimetic designs to offer distinct advantages such as targeted drug delivery, biocompatible, and improved therapeutic efficacy. Bioactive-based nanotherapeutics are used in the treatment and management of various diseases.

This book, “Bioactive-Based Nanotherapeutics,” explores this rapidly growing field of therapeutics. It presents a broad overview of the fundamentals of bioactive nanomaterials, their design strategies, and their therapeutic applications. Leading experts from different disciplines have contributed chapters that explore a diverse range of topics, including the basics of bioactive in bioactive nanotherapeutics, isolation methods of different bioactive compounds, and formulation developments. Chapters explore strategies for designing and engineering bioactive nanoparticles to achieve desired properties for specific therapeutic applications. The book also explores the application of bioactive nanotherapeutics for the treatment of a variety of diseases, including cancer, GIT, infectious diseases, neurodegenerative disorders, etc. Regulatory requirements for bioactive-based nanotherapeutics are also highlighted.

This book is an important resource for researchers, healthcare professionals, and students interested in bioactive nanotherapeutics. It provides a complete understanding of the field and explores the enormous potential of this approach for revolutionizing disease treatment and management.

We, the editors, are confident that this book will serve as a benchmark for further research and development.

Prof. (Dr.) Rakesh K. SindhuProf. (Dr.) Sumitra SinghProf. (Dr.) Evren Algin YaparApril 2025

1Basics of Nano-Bioactive Compounds and Their Therapeutic Potential

Jannat ul Firdaus1, Sumitra Singh2 and Rakesh K. Sindhu3*

1School of Pharmacy, Sharda University, Gr. Noida, Gautam Buddha Nagar, Uttar Pradesh, India

2Department of Pharmaceutical Sciences, Guru Jambheshawar University of Science and Technology, Hisar, Haryana, India

3Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, Haryana, India

Abstract

In a broad way, bioactive compounds can be classified into two forms, essential and nonessential compounds obtained from nature, and are a part of the food chain. Bioactive compounds carry numerous health benefits for the body that promotes good health. Nowadays, these compounds are studied as they prevent many dreadful diseases such as malignant tumors, and cardiovascular disease. These compounds also show free radical scavenging properties and antiphlogistic properties, immunomodulatory potential, as well as antimicrobial properties. These compounds are chemically unstable, susceptible to oxidation, and insoluble in body fluids; therefore, their delivery is a cause of concern. Plant-based bioactive compounds impart therapeutic effects and adverse effects on humans and animals. There is an extensive range of advantages of bioactive compounds in food technology, plant science, geoscience, plant science, biophysical and computational sciences, agrochemicals, cosmetics, and nanobioscience. Bioactive compounds include terpenoids, polyphenols, alkaloids, and other nitrogen-containing compounds. These are generally secondary metabolites. This chapter includes an introduction, medicinal uses of bioactive compounds, extraction techniques, carrier approach for bioactive compounds, and therapeutic potential of nano-bioactive compounds. Diet provides proper nutrients to cover the metabolic requirements and also improves human health.

Keywords: Bioactive compounds, health, nanotherapeutics, nanobioscience, toxicological effects

1.1 Introduction

Bioactive compounds, rich in nature, are molecules with significant impacts on living organisms across plants, animals, and microorganisms. These compounds, various in structure and function, play pivotal roles in biological processes and good health benefits. Various groups of bioactive compounds are phytochemicals, microbial toxins, nutraceuticals, and secondary products. A wide range of biological roles are played by bioactive compounds such as antioxidant, anti-inflammatory, antimicrobial, and anticancer properties. Phytochemicals, such as flavonoids and alkaloids, contribute to plant characteristics and provide health benefits, whereas nutraceuticals offer health advantages beyond basic nutrition [1]. Microbial and secondary metabolites, including antibiotics and plant-derived compounds, hold therapeutic promise. Ongoing research continues to uncover the multifaceted functionalities of natural biologically active compound, facilitating the production of pharmaceuticals and nutraceuticals to enhance human health and well-being. Various plant sources from which bioactive compounds can be obtained are fruits, vegetables, seaweeds, herbs, broccoli, carrots, and cereals. These compounds possess anti-inflammatory and antioxidant potential. These are the secondary metabolites that have health-promoting effects. Bioactive compounds have a diverse range of pharmacological activity as a remedy to treat various disorders. An extensive range of these compounds is available, which can be mainly obtained from plants, vegetables, and whole grains [2], as shown in Figure 1.1.

Figure 1.1 Various types of bioactive compounds.

1.2 Therapeutic Potential of Bioactive Compounds

Bioactive compounds affect living organisms, tissues, or cells. They are generally sold as dietary supplements [3, 4]. Bioactive compounds may be found in various natural foods. These compounds are used to improve health and chronic disease prevention as mentioned in Figure 1.2. Sources for obtaining bioactive compounds are plant, animal, and synthetic way [5, 6]. There is a wide range of therapeutic potentials of bioactive compounds in the extracts and compounds in the anticancer, antidiuretic, antipyretic, free radical scavengers, treat bacterial infections, anti-convulsant, prevention of blood clots [7].

Figure 1.2 Therapeutic application of bioactive compounds.

1.2.1 Alkaloids

Alkaloids have basic nitrogen atoms in their structure, they are mainly amines. Alkaloids can be obtained from plant families such as Solanaceae, Ranunculaceae, Papaveraceous, and Amaryllidaceae. Lysine, ornithine, terpenoid, and polyketide pathways are different pathways by which alkaloids can be obtained [8]. Natural alkaloids include vincristine, hydroxy camptothecin, and ligustrazine. The molecular weight of alkaloids is less than 1 kDa. Alkaloids can be obtained from the stem, root, rhizome, fruit, and bark of medicinal plants [9].

1.2.1.1 Medicinal Use of Alkaloids as Bioactive Molecule

Strychnine, quinine, and nicotine are some well-known alkaloids that have beneficial effects.

Alkaloids possess many pharmacological consequences such as reducing myocardial damage, reducing inflammation, anaesthetics, and antiviral [10].

1.2.2 Antibiotics

Medicines that are used to treat bacterial infections are antibiotics. Antibiotics hamper bacterial growth. Pathogens including prions, viruses, parasites, bacteria, protozoa, worms and mould cause infectious diseases. Through the cardiovascular system, infectious microorganisms spread throughout the body. Bone marrow plays a crucial role in eliminating these deadly pathogens. In reducing the side effects of drugs, resistance, and cost of treatment antimicrobial nanoparticles play a very important role [11].

1.2.2.1 Medicinal Use of Antibiotics as Bioactive Molecule

Bioactive comopounds are used as antibiotics to treat various diseases like Pneumonia, typhoid fever, or gonorrhea [12].

1.2.3 Mycotoxins

Mycotoxins are naturally producing toxins, found in food and cause kidney damage and DNA damage on exposure, resulting into death. Mycotoxins have some pharmacological properties, which act as antibiotics and growth promotants [13].

1.2.3.1 Medicinal Use of Mycotoxins as Bioactive Molecule

1.2.4 Growth Factors

Growth factors are a large group of bioactive macromolecular drugs used for peripheral nerve injuries. Growth factors play an important role in nerve regeneration, which includes nerve cell growth and survival, regeneration of axon and myelin sheath, cell differentiation, and angiogenesis [14].

1.2.4.1 Medicinal Use of Growth Factors as Bioactive Compounds

Growth factors are macromolecules that promote cell survival and proliferation, and they also treat peripheral nerve injuries [14].

1.2.5 Phenolics

Phenolics also known as phenol carboxylic acids are a plant-based phenolic compound found in many plant source foods such as seeds, fruit peel, and vegetable leaves [15].

1.2.5.1 Medicinal Use of Phenolics as Bioactive Compounds

Phenolics are originated form plants and used to treat conditions like free radical damage. These compounds can be used alone or in combination of vitamins [16]. Diet contributes to meeting daily metabolic requirements as well as improvement of human health. Extracts of plants need to be identified and developed that benefit human health [17]. Many chronic diseases can be treated by consumption of plant-based products. Nutraceutical and pharmaceutical sectors are now focusing on these plant-based products for developing food products and natural medicines, having therapeutic effects with less or no side effects [18]. Fruits, vegetables, and nuts play a crucial role in decreasing the risk of neoplasm and heart diseases. Taking one portion of fruits and vegetables in a meal will decrease hazard of heart disease by up to 7%. There are many roles of having healthy food such as improving immunity, healthy hairs, nails, etc., with a decreased carcinoma risk [19]. Secondary metabolites are formed in plants by primary biosynthetic and metabolic routes. They are regarded as biochemical products. Many plant species tend to produce such compounds [20]. The effects of bioactive compounds are shown in Table 1.1 with their beneficial effect.

Table 1.1 Table showing various condition treated by bioactive compound.

Condition

Bioactive compound

Source

References

Inhibiting cancer cell growth

Vincristine, vinblastine, irinotecan, etoposide, podophyllotoxin, and paclitaxel

-

Catharanthus roseus

-Camptothecacuminata-Rhizomes of podophyllum peltatum

[21]

For treating epilepsy

Alkaloids, flavonoids, terpenoids, saponins, and coumarins

Aconitum speciesPassiflora caerulea L.Cannabis sativaCynanchumotophyllum schneidCoumarona odorata

[22]

Antiviral activity

Betulin

-Euphorbia denticulara Lam.

[23]

Antimicrobial activity

D-mannitol and phytol

Hybanthusenncaspermus extracts

[24]

Anti-inflammatory activity

Peptides, polysaccharides, and fatty acid

Microalgae and cyanobacteria

[25]

Local anaethetic

Cocaine and thymol

-

Erythroxylum coca

-

Thymus vulgaris

[26]

Hepatoprotective agent

Phytosterols, carotenoids, and polyphenols

Vegetables, fruits, and nuts

[27]

1.3 Extraction Techniques for Obtaining Bioactive Compound

Recently, bioactive compounds have been used in many commercial sectors: food industries, medicinal industries, and cosmetic industries. There is a need for most standard protocols for extracting these plant-based active compounds. A proper extraction method is also needed for good yield and better quality of bioactive products. The method of extraction is also named sample preparation techniques [28, 29]. From various parts of plants, these compounds can be obtained and analysed [30]. Non-conventional methods of extraction are mostly preferred over conventional methods due to less utilization of artificial chemicals, less duration of operation, and good product. Various extraction methods for plant-based bioactive compounds are mentioned in Figure 1.3. Conventional methods including decoction, maceration, and Soxhlet extraction are also used for extraction [31].

Figure 1.3 Flowchart showing various methods of extraction.

1.4 Novel Delivery Approach for Bioactive Compounds

Nanotechnological approaches are used for the formation of nano-bioactive compounds that are used for making medicines, food products, and energy technology. Nanocarriers are used for as a transportation tool for bioactive compounds as shown in Table 1.2 [32–41]. Nanotechnology is used, nowadays, in food science. These compounds promote health improvement [42]. Nanotechnology is used in the form of nutraceuticals, and the main active constituents are encapsulated and protected, thereby releasing functional components [43, 44]. This technology is used to design and produce devices, structures, and systems where dimensions of the material will be in the range of 10−9 m [45]. For healthier consumer choices, synthetic food products are changing into herbal (plant-based form) as bioactive compounds [34, 46]. Bioactive compounds have many health benefits for the well-being of humans; however, these compounds are unstable at the time of processing of food and storage. When exposed to the alimentary tract, it becomes chemically unstable and has low bioavailability thus limiting their applications [47].

Table 1.2 Table showing various types of nanocarriers, its advantages, and diseases to be treated.

Nanocarriers

Conditions

Advantages

References

Plant proteins (EPPs)

Free-radical scavenging, cytotoxic, reduces swelling, and reduces aging activities for human health

Enhance the solubility, stability, and bioavailability of bioactive.

[32]

Ferritin-based nanocarrier

Free radical scavenging, cytotoxic, diabetes mellitus, and reduces swelling

Nanosized shell-like structure

[33]

Hydrophilic nanocarriers

Antioxidants

Increase solubility and bioavailability of bioactive

[34]

Lipid nanocarriers with nanostructured lipid carriers (NLCs)

Food products

Protecting from acidic environment and drug release

[35]

Gum-based nanocarriers

Encapsulation of food bioactive ingredients

Flexibility, biocompatibility, biodegradability, and availability of reactive sites for molecular interactions

[36]

Bioactive-loaded nanocarriers

Preparation of safe foods, with good nutritional and sensory characteristics, and having tendency to provide multiple health benefits

Increasing the bioavailability of bioactive compounds

[37]

Alginate-based nanocarriers

Malignant tumors, reduces swelling, anti-diabetic, anti-estrogen, anti-mycotic, antibiotic anti-allergic, and anti-thrombotic activities

Nontoxic, comparatively cheap, creating goods simply, polymeric, and decomposable

[38]

Chitosan-based nanocarriers

Development of food products with standard quality and nutritional value

Enhances bioavailability and stability of bioactive ingredients

[39]

Dendrimers nanocarriers

Antioxidants, anti-inflammatory agents, antivirals, antibiotic, anti-cancer agents, and immunomodulatory

Improve the efficiency of phytochemical bioactive compounds

[

40

,

41

]

1.5 Electrospinning

Electrospinning is a promising method, in which bioactive components are encapsulated as it does not require any severe physical conditions. Nanofibers produced by electrospinning are an important technique that provides adequate delivery and release of bioactive compounds [48]. This technique is an electrokinetic process in which nanofibers are formed by the application of electric force [46].

Advantage: This method is highly efficient, profitable, and elastic and utilizes an electric field that is applied over polymer solution at a high speed for the development of fibers or particles at nanosizes [49].

1.6 Micro- and Nanoencapsulation of Bioactive Compounds

These compounds have wide range of biological potential, but, on the same page, they are not stable chemically, have loss of activity, and have degradation. Pure bioactive compounds have limited uses due to factors such as it released fast, poor solubility, and less bioavailability [50, 51].

Encapsulation is a technique that preserves these natural bioactive compounds: damage from environment, improves physicochemical parameters, and enhances its medicinal values [52]. Encapsulation is a good technique as it prevents the quality of food and nutraceutical formulations [53, 54]. The two major types of encapsulation techniques are micro-encapsulation and nanoencapsulation [55]. In the encapsulation process, the active components are coated by carrier material, thereby forming capsules in micrometer or nanometer size. The active ingredient is also called the core. The membrane is used as carrier material [56]. For the effective protection of bioactive compounds, the nanoencapsulation technique is used. Pectin is used as carrier. Pectin also increases the stability and life span of these compounds. Compounds such as Maltodextrin along with gums or proteins imparts an important production for the encapsulatingthe bioactive compounds [57]. The encapsulation process is also defined as the capture of compounds within an immiscible substance, i.e., solid or liquid. The nanoencapsulation process results in nanocapsules having a size less than 1,000 nm [58]. Natural bioactive compounds are encapsulated with various drug delivery methods, which may improve their drug efficacy, have greater in silico stability and release of drug in blood, reduce side effects, and increase target specificity [59].

1.7 Polymeric Nanoparticles (NPs)

The nanocarrier-based targeted delivery systems of medicine are increasing day by day. For controlled drug delivery, poly (alkyl cyanoacrylates) is a type of biodegradable polymer used to develop nanocarriers. In diseases such as neoplasm, drug-loaded polymericnanoparticles are utilized to convey therapies into tumor cells with high efficacy and less toxicity in healthy cells [60, 61]. Polymeric nanoparticles have a particle size range between 1 nm and 1,000 nm. The nanoparticles carry active compounds entangled within or on the surface of polymeric nanoparticles [56]. Nanoparticles can be both nanocapsules and nanospheres that differ in morphology. Polymeric nanoparticles when used as drug carriers have advantages like the ability to protect the drug against the environment, improving the bioavailability and therapeutic index [62, 63].

1.8 Solid Lipid Nanoparticles

These are used as carrier systems for effectively water-dissolvable medication. The colloidal particles having a size range between 10 nm and 1,000 nm. They are used as a different substitute for liposomes as medical carriers. The advantages of SLNs (solid lipid nanoparticles) are as follows: they prefer small size, huge surface area, and high medication stacking [64, 65]. Problems such as deficient drug concentration due to poor ADME, poor drug solubility, and unpredictable bioavailability can be overcome by using an accurate delivery system [66]. Liposomes are spherical vesicles. These nanoparticles contain either one or more than one phospholipid bilayers. Drugs that are lipid soluble can be assimilated into lipid bilayers, whereas hydrophilic drugsare solvable in the aqueous core [67, 68]. Drug carriers that depend on liposomes will allow the intravenous injection of drugs with very low water solubility [69–71].

1.9 Nanoemulsions

Nanoemulsions are colloidal dispersions with droplet sizes below 100 nm, known for their stability, optical transparency, adjustable rheology, and applications in drug delivery, cosmetics, food, pharmaceuticals, and material synthesis [72]. To prepare nanoemulsions, both high- and low-energy methods are used.

High-energy methods: These include high-pressure homogenization, microfluidization, and ultrasonication.

Low-energy methods: These include phase inversion emulsification method and the self-nanoemulsification method.

Nanoemulsion can be prepared by multiple steps, where a microemulsion is first prepared and then turn into nanoemulsion [42, 73, 74]. For the development of pharmaceutical formulations like topical, oral, and injectables, nanoemulsions are used. They also serve as a model for creating nanocrystals of hydrophobic active pharmaceutical ingredients [75, 76]. Multiphase or multiple emulsions are also developed having internalized phases, enabling chemical compartmentalization, which controls the release of active ingredient and complex particles [77, 78]. Encapsulating the bioactive compounds with nanoemulsions is a powerful technique as it protects food ingredients such as vitamins, antioxidants, lipids, and antimicrobial agents. Over conventional techniques, this method is more convenient [79]. This method has a small droplet size, transparent optical properties, more physically stable, and improved bioavailability. Nanoemulsions can be prepared with different sizes of droplets [80–82].

1.10 Nanocrystals

These are crystalline particles that have a size of 1,000 nm consisting of mainly drug that is balanced by stabilizer and surfactants [83, 84]. Nanocrystals are typically produced using methods like crystallization and supercritical fluid crystallization, with dispersing materials such as water, liquid polyethylene glycol, and oil [85, 86].

1.11 Phytosomes

They are lipid-loving molecular complexes that will enclose the potent bioactive and water-soluble phytochemicals within the phospholipid bilayer, which results in enhanced absorption and bioavailability [87]. Phytosomes are structurally similar to liposomes except for the capture of material [88]. These compounds are used to treat many skin conditions, carcinoma, and anti-aging medication and are hydrophilic. Due to this hydrophilic nature, phytosomes have poor bioavailability through the skin or gut. Thereby, novel formulations of phytosomes are made which help to overcome these problems [89].

1.12 Therapeutic Potential of Nano-Bioactive Compounds

The medicinally active compounds derived from plants and used for development of novel therapeutic formulations utilizing bioactive compounds and plant extracts, including nanocrystals, pyrosomes, injectables, hydrogels, emulsions, microspheres, and nanogels. It is found that these nanoformulations have many advantages: increased solubility, more efficacy, good bioavailability, more stability, better tissue distribution, protection from environmental effects, and targeted delivery [90–92].

Vieira et al. (2023) studied the potential effect of polyphenols against cancerous cells. Polyphenols as bioactive compounds, which are derived from fruits and vegetables, have beneficial effects on healthy organisms. Natural plant–based bioactive compounds such as vincristine, curcumin, and caffeic acid have been used as anticancer agents to treat the deadly disease of cancer. Nanotechnology approaches have been used to engulf these bioactive compounds, due to their limited solubility and less release of drug in blood to encapsulate these compounds for increasing the efficacy of these compounds. The results showed that polymeric nanomaterials, mostly carbon-based and metal, are the mostly used nanocarriers toencapsulate polyphenols. The antitumor activity is enhanced due to these delivery systems against various cancer types [93].

Ansari et al. (2020) developed a nano-based therapeutic intervention of bioactive sesquiterpenes for the treatment of malignant tumors. Sesquiterpenes are the major part of essential oil found in different species of plant. To enhance the biological potential of these bioactive compounds, nanotechnology is used. This approach enhanced the anticancer activity of sesquiterpenes [94].

Alfieri et al. (2021) studied the therapeutic potential of plant-derived nano- and microvesicles. Bioengineering technology has advantages like drug carrier systems, vaccination, and genetically used therapies, which make derived vesicles excellent natural or bioengineered nanotools. These plant-derived nano- and microvesicles may impart immunosuppressant, free-radical scavenging activity, and cytotoxic activity when tested on various in silico models [95].

Clarence et al. (2022) studied the potential benefits of bioactive compounds against chronic inflammation of the respiratory tract, which leads to chronic obstructive pulmonary disease symptoms including frequent respiratory infection, cough, and chest tightness. The conventional therapies for this disease only clear the symptoms and fail to treat the functional damage. Nutraceuticals such as piperidine alkaloids have medical benefits that can ameliorate these symptoms and reverse inflammatory damage. The nanoparticles are used to deliver these compounds [96].

Ganesan et al. (2015) studied the pharmacological benefits of bioactive compounds of ginseng in chronic disease. Due to the wide range of therapeutic value of ginseng medicine such as immunity booster and diabetes and fatigue prevention, it is popular around the world and used for ages. Due to presence of volatile oils like ginsenosides, amino acids, and phytosterol, ginseng imparts potent effect. Ginsenosides and polyphenols shows anti-malignant and immunomodulatory effects. The bioactive compounds in ginseng are structurally modified in nanometer in order to improve its pharmacological effect. These nano-sized particles become effective in treating disease as they have higher quantity in blood, improved oxygen supply in blood stream, and less adverse effects [97].

Wound treatment is a difficult situation all around the world. Kumar et al. (2023) researched the pharmacological effect of nanocarrier-mediated delivery of phytoconstituents for wound healing. The plant-based bioactive compounds were used from ancient times for illness, prevention, and therapy. Due to their high rates and more demand with less adverse effects of modern medicine, plant-based bioactive compounds have high demands nowadays. Nanocarrier obtained from plants will deliver natural wound healing treatments in the form of nanofibers, nanoparticles, nanoemulsion, and nanogels have been discussed [98].

Ashraf et al. (2020) discussed the use of entomopathogenic medicinal fungus Cordyceps having nutraceutical and therapeutic value. Cordyceps is a fungus obtained naturally from Himalayan plateau. In traditional Chinese medicine, it is well-known medicine that contains a wide range of bioactive components. Cordycepin is one of the componentsfound to be most vital due to its utmost therapeutic and nutraceutical properties, making it valuable medicine for various serious disorders [99].

Fuloria et al. (2022) studied about potency of Curcuma longa Linn. In addition, its major active constituent is curcumin. In the ancient system of medicine, C. longa has been used for obstruction in biliary andicterus and topical application over ulcers and inflammation, headache, rashes, yellowish stool, and diarrhea. Curcumin as a bioactive compound has many applications nowadays [100].

Fahimirad et al. (2019) discussed the potential medicinal effect of plant derived extracts of silver nanomaterials. Silver nanoparticles have anti-cancer, antimicrobial, wound repair, and wound healing properties. Silver nanoparticles (AgNPs) are crucial compounds in nanotechnology field. As bioactive compounds, these compounds have the efficiency to treat microbial infection and cancer [101].

Salimikia et al. (2023) studied the therapeutic potentials of reserpine formulations. The bioactive compound Reserpine is an indole alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria used for the management and treatment of hypertension first-generation antipsychotic agent. Reserpine is an antibacterial drug that inhibits gram-positive bacteria and mammalian efflux. It can also act as an anticancer agent. Neurotoxicity caused by reserpine can be treated by encapsulating the drug [102].

Hegde et al. (2022) researched the pharmacology of quercetin in diabetic foot ulcers as diabetic foot ulcers are a complicated condition associated with symptoms such as foul smell, pain, redness, pus/fluid discharge promoting delayed wound healing processes, and foot amputations. Quercetin as a bioactive compound has many therapeutic properties such as anti-diabetic, anti-inflammatory, antioxidant, inhibiting the growth of microorganisms, and reducing inflammation [103].

Goyal et al. (2024) reviewed about therapeutic potential of quercetin for central nervous system degenerative disorder and studied its nanotechnological aspects. With the aging of neurons, the process of neurodegeneration begins in the brain. Quercetin is a plant pigment found in vegetables and fruits, and the formulation of quercetin is important as it helps in the delivery of the compound through this route for the treatment [104].

Ansari et al. (2021) studied the therapeutic potential of Tanshinone IIA, a bioactive lipophilic component of Salvia miltiorrhiza extract. Tanshinone IIA has been utilized in traditional Chinese medicine since ages. Nowadays, this nano-bioactive compound is utilized in treatment of diseases such as heart diseases, brain disorders, cancer, diabetes, and obesity [105].

Tuli et al. (2013) considered the therapeutic potential of the bioactive compound Cordycepin. Cordycepin is a nucleoside analog obtained from insect fungus Cordyceps militaris used as anticancer agent induction of apoptosis, inhibition of angiogenesis, and metastasis. Novel drug targets are developed to elevate the therapeutic effect of anticancer medications and reduce the risk associated with it [106].

Wu et al. (2020) discussed the beneficial effects of phenylethanoid glycosides. They can be obtained from many sources and are soluble in water. Various medicinal properties are possessed by PhGs. Nanotechnology improves the bioavailability of these compounds [107].

Nile et al. (2020) studied the therapeutic potential of interferons. To reduce mortality rates due to COVID-19, recognizing already used drug with good safety profile as how to treat hyperinflammation is a risk. Interferons, nanoparticles, vaccines, short sequenced nucleotides, and monoclonal antibodies are used to control and treat SARS-CoV2 [108].

Xu et al. (2023) described the therapeutic effect of cancer nanomedicine. Cytotoxic agents have certain challenges like killing abnormal cells along with normal healthy cells, drug resistance, and poor drug solubility, specifically limiting their therapeutic efficacy. In cancer treatment, the discovery of nanomedicine improves the specificity, efficacy, and tolerability of cancer treatment. In cancer treatment, nanomedicines show more potential, thereby improving patients’ health [109].

Sivasami et al. (2018) studied Curcumin, a bright yellow product of Curcuma longa, aperennial herb having family, Zingiberaceae. The therapeutic potential of curcumin is in inflammatory, neoplastic, and paraneoplastic diseases. Curcumin has been developed using various techniques, and curcumin can be separated from turmeric by using the technique of solvent extraction followed by column chromatography [110].

Esfanjani et al. (2016) explained that, for nanoencapsulating the phenolic compounds, polymeric nanoparticles along with nanocarriers are used. Phenolic compounds are important bioactive compounds as major micronutrients in our diet, and they prevent degenerative disease. For the delivery and protection of phenol compounds, different types of nanoparticles and nanocarriers are mostly used such as polymeric nanoparticles and natural nanocarriers [111].

Armenta et al. (2021) studied about medicinal applications of honey in treating inflammation and oxidative stress. This treatment delays osteoarthritis progression [112].

1.13 Conclusion

Bioactive compounds have many pharmacological effects on the body. These compounds are present in small quantities in foods, which impart beneficial effects. These compounds possess therapeutic activities such as antioxidant, anticancer, immunomodulatory, reduced swelling, and antimicrobial. The literature review suggests that these compounds have limited therapeutic potential because of factors such as low solubility and less bioavailability. It can be obtained from plants, vegetables, fruits, fish, seaweed, herbs, etc. Despite having numerous advantages of bioactive compounds, they are poorly absorbed by the system. So, there is ancrucial demand to meet the developed nanostructured forms of these bioactive compounds to prevent them from degradation, solubility, and instability and to improve bioavailability. The field of nanotechnology is developing fast to deliver improved nanostructures. In silico studies suggest better activity of nanostructured compounds with good therapeutic efficacy and fewer side effects.

Further studies are performed for novel nanodelivery bioactive compounds to treat various diseases. To develop more improved systems with safety and efficacy, continuous need is required in the research and development program. More knowledge is needed to meet the requirement of nanodelivery systems with improved therapeutic potential against various targets. The present book chapter collates various nano-based therapeutic potentials of bioactive active, along with their method of extraction to treat various diseases. To improve the clinical acceptability of drugs, the nanomedicine field is improving day by day with all the advancements.

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