Polymer-Drug Conjugates

Linker Chemistry, Protocols and Applications

1st Edition - July 5, 2023
Editors: Jitender Madan, Ashish Baldi, Monika Chaudhary, Neetu Chopra
Language: English
Paperback ISBN:
9 7 8 - 0 - 3 2 3 - 9 1 6 6 3 - 9
eBook ISBN:
9 7 8 - 0 - 3 2 3 - 9 1 6 9 0 - 5

Polymer-Drug Conjugates: Linker Chemistry, Protocols and Applications discusses important concepts, fundamentals and prospective applications of ‘Linker Chemistry’ in a clear-and… Read more

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Polymer-Drug Conjugates: Linker Chemistry, Protocols and Applications discusses important concepts, fundamentals and prospective applications of ‘Linker Chemistry’ in a clear-and-concise manner. The book provides vital information on chemical entities binding with the drug-polymer complex for targeted drug delivery systems. It highlights roles and significance, different classes and synthetic protocols as well as mechanisms of chemical bond formation in drug-polymer conjugation in drug delivery, also offering insights into the mechanism of polymer interaction with linker and drug molecules by biodegradable chemical bonding.

The protocol of binding with drug molecules is clearly explained and justified with case studies, helping researchers and advanced students in the pharmaceutical sciences understand fundamentals involved and related aspects in molecule designing for effective therapeutic benefits.

Cover image
Title page
Table of Contents
Copyright
Dedication
Contributors
Editors
Preface
Acknowledgment
Chapter 1. Drug delivery: The conceptual perspectives and therapeutic applications
1. Introduction
2. Basic fundamentals of targeted drug delivery systems
3. Passive targeting
4. Active targeting
5. Ligands for targeting
6. Endocytosis
7. Need of targeted drug delivery system
8. Targeted drug delivery system by oral and parenteral routes
9. Regulatory challenges of novel drug delivery system
10. Scale-up challenges of targeted drug delivery systems
11. Marketed formulation based on targeted drug delivery systems
12. Conclusion and summary
Chapter 2. Rational design of linkers in polymer–drug conjugates
1. Introduction
2. Polymer–drug conjugate
3. Linkers/spacers
4. Conclusion
Chapter 3. Exploration of polymers in drug delivery: The structural and functional considerations
1. Introduction
2. Different polymers used in linker chemistry for bioconjugation of drugs
3. Classification of polymers on the basis of their structural and physicochemical behavior
4. Role and function of different polymers used in linker chemistry
5. Selection of polymeric drug delivery system and drug release
6. Some recent developments
7. Conclusion
Chapter 4. Chemistry of conjugation in drug delivery: The prospects of biodegradable bonds in polymer–drug conjugates
1. Introduction
2. Characteristics of an ideal polymer
3. Polymer-based drug delivery system
4. Polymers used in preparation of polymer–drug conjugates
5. Drug release from polymer–drug conjugates is pH sensitive
6. Different linkages involved in polymer–drug conjugation
7. Conclusion
Chapter 5. Polymer–drug conjugation using ester and ortho-ester bond: Mechanism, protocols, and applications
1. Introduction
2. Discovery tale of polymer–drug conjugates
3. Insights into ester and orthoester bond as drug–polymer conjugate strategy
4. Ester and orthoester bond: Chemistry and cleavage
5. End group functionalities of ester and orthoester conjugation: Synthetic procedures and applications
6. Conclusion
Chapter 6. Polymer–drug linking through amide bonds: the chemistry and applications in drug delivery
List of abbreviations
1. Introduction about polymer
2. Polymer–drug conjugates
3. Various polymer–drug linking through amide bond: its chemistry
4. Application of polymer–drug linking through amide bond in drug delivery
5. Conclusion and future aspects with polymer–drug conjugate
Chapter 7. Drug–polymer conjugate tailoring by disulfide linkage for controlled and targeted drug delivery
1. Introduction
2. Basic chemistry of disulfide linkage
3. Binding with disulfide linkage
4. Drug delivery by drug–polymer sulfide linkage conjugates
5. Synthetic strategies of polymer–drug conjugates
6. New facile strategy
7. Polymer therapeutics for drug delivery
8. Applications of tailored drug–polymer conjugates by sulfide linkage
9. Failures of disulfide linkage
10. Successful disulfide linkages
11. Challenges and future projections
Chapter 8. Thioether linkage chemistry: perspectives and prospects in therapeutic designing
List of abbreviations
1. Introduction
2. Paclitaxel/gemcitabine
3. Cyclodextrin hyaluronic acid conjugates
4. Camptothecin–PEG–LHRH drug conjugate
5. BIM-23A760
6. Conclusion
Chapter 9. Drug targeting to cancer cells through stimuli-responsive imine bonds: fascinating aspects of site specificity
1. Introduction
2. Polymeric drug delivery system
3. Shell-sheddable nanoassemblies
4. Core-degradable backbone-multicleavable nanoassemblies
5. Core-degradable pendant-multicleavable nanoassemblies
6. Stimuli-responsive/pH-responsive drug–polymer conjugates for cancer chemotherapy
7. Mechanism of formation of imine bond
8. In vivo fate of pH-responsive drug–polymer conjugates with imine and hydrazone linker
9. Drawbacks of imine and hydrazone linker bond in development of drug–polymer conjugate
10. Applications
11. Polymeric nanoparticles
12. Hydrogels
13. Drug–polymer conjugate (polymeric prodrugs)
14. Polymeric micelles
Chapter 10. Carbamate–drug conjugates in drug delivery: structural and mechanistic considerations
1. Introduction
2. Chemistry
3. Methodologies for carbamate bond formation
4. Applications of carbamates in pharmaceutical field
Chapter 11. Bonding through phosphodiester moiety: Its implications in pharmaceutical modifications
1. Introduction
2. Phosphodiester-containing biomolecules
3. Chemistry of phosphodiester bond
4. Role of phospholipids in drug delivery
5. Oligonucleotide–phosphodiester conjugates
6. siRNA oligonucleotide conjugates
7. Conclusion
Chapter 12. Enzymatically degradable linkers
1. Introduction
2. Chemotherapeutic agents and their therapeutic limitations
3. Concept of cancer targeted polymer–drug conjugates
4. Components of polymer–drug conjugates
5. Design and development of enzyme sensitive nanocarrier–mediated anticancer drug delivery system
6. Conclusion
Chapter 13. Dendrimer–drug conjugates
List of abbreviations
1. Dendrimers-based drug delivery systems
2. Advantages of dendrimer–drug conjugates
3. Prerequisites for dendrimer–drug conjugates
4. Synthesis strategies of dendrimer–drug conjugates
5. Dendrimer prodrugs with spacers
6. Applications of dendrimer–drug conjugates
7. Dendrimer–drug conjugates in cancer therapeutics
8. Dendrimer–drug conjugates in inflammatory diseases
9. Conclusion and perspective of developing dendrimer–drug conjugates
Chapter 14. Antibody–drug conjugate: Emerging trend for targeted treatment
1. Introduction
2. Antibody–drug conjugates design and its chemistry
3. Conjugation mechanism
4. Mechanism of action
5. Antibody–drug conjugate strategies for treatment of diseases
6. Limitation and potency enhancement of antibody–drug conjugates
7. Clinical implication of ADC
8. Conclusion and future perspective
Chapter 15. Drug–polymer conjugates: Challenges, opportunities, and future prospects in clinical trials
1. Introduction
2. Types of polymer–drug conjugates
3. Polymers used in PDC
4. Polymer protein conjugates
5. Preparation of PDCs
6. Analytical methodology
7. Advantages of PDC
8. Applications of PDC
9. Polymer–drug conjugates as a concept for combination therapy
10. Polymer conjugates for new molecular targets are being developed
11. Drug distribution
12. PDC in clinical trials
13. Conclusion and future prospects
Index

Jitender Madan

Dr. Madan’s major areas of research include Self-assembled Supramolecular systems viz. liposomes, niosomes, cyclodextrin, nano- & micro-particles and solid-lipid nanoparticles. The focus is centered onto the exploitation of US FDA approved biomaterials in combination with other potential lipids and polymers to develop the innovative dosage forms and drug delivery systems in order to improve the bioavailability, stability, safety (tolerance) and patient-compliance. Whilst a wide range of applications are being taken up, the special emphasis is given to augment the aqueous solubility and bioavailability of lipophilic drugs.

Affiliations and expertise

Associate Professor, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, India

Ashish Baldi

Dr. Ashish Baldi PhD, alumni of Sagar University and Indian Institute of Technology Delhi, is presently working as Professor and Dean, Faculty of Pharmacy MRSPTU, Bathinda. With over 17 years of experience, 3 Patents, 2 Design applications, 8 books, 4 special issues, over 100 national and international publications, 14 book chapters, 35 Invited lectures, several popular articles, more than 160 papers at conferences/ seminars in India and abroad, and several best paper awards to his credit, he is an active researcher in various facets of pharmaceutical sciences and biotechnology. Presently he is supervising 6 research projects granted by various Government agencies like Ministry of AYUSH, DST, ICSSR, ICMR, FITM. He completed 13 major and minor research projects and transferred 2 technologies to leading pharmaceutical industries.

Affiliations and expertise

Professor, Department of Pharmaceutical Sciences and Technology, Maharaja Ranjit Singh Punjab Technical University, Bathinda, Punjab, India

Monika Chaudhary

Dr. Monika Chaudhary PhD primary areas of research are drug discovery, design and prodrug formulations in the field of medicinal chemistry. Worked in bio conjugation of anti-cancer drugs and published several research as well review papers in the journals of international repute.

Affiliations and expertise

Associate Professor, GVM College of Pharmacy, Sonepat, Haryana, India

Neetu Chopra

Dr. Neetu Chopra received his PhD in Pharmaceutical Chemistry in 2020. His core area of research covers Design of drug molecules by using Drug designing software’s like Auto dock, V-life sciences, Schrodinger, Computational chemistry, Synthesis of drug molecules, Purification of drug molecules by using Column Chromatography, Chemical libraries, Computational chemistry, Drug discovery and development, Lead optimization, Screening of drug molecules Identification of drug molecules by using different spectral analysis techniques.

Affiliations and expertise

Safety and Pharmacovigilance Specialist, Syneos Health, Gurgaon, Haryana, India

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Polymer-Drug Conjugates

Linker Chemistry, Protocols and Applications

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Institutional subscription on ScienceDirect

Jitender Madan

Ashish Baldi

Monika Chaudhary

Neetu Chopra