Drug Delivery: Principles and Applications

Following its successful predecessor, this book covers the fundamentals, delivery routes and vehicles, and practical applications of drug delivery. In the 2nd edition, almost all chapters from the previous are retained and updated and several new chapters added to make a more complete resource and reference.  Helps readers understand progress in drug delivery research and applications  Updates and expands coverage to reflect advances in materials for delivery vehicles, drug delivery approaches, and therapeutics  Covers recent developments including transdermal and mucosal delivery, lymphatic system delivery, theranostics  Adds new chapters on nanoparticles, controlled drug release systems, theranostics, protein and peptide drugs, and biologics delivery INDICE: List of Contributors .Preface .1 Factors that impact the developability of drug candidates Chao Han and Binghe Wang .1.1. Challenges facing the pharmaceutical industry .1.2. Factors that Impact Developability .1.3. Commercial goal .1.3.1. The Chemistry Efforts .1.3.2. Biotechnology in the Discovery of Medicine .1.3.3. Target Validation in Animal Models .1.3.4. Pharmacokinetics and Drug Metabolism .1.3.5. Preparation for Pharmaceutical Products .1.3.6. Remarks on Developability .1.4. Drug Delivery Factors that Impact Developability .References .2. Physiological, Biochemical, and Chemical Barriers to Oral Drug Delivery Paul Kiptoo, Anna M. Calcagno, and Teruna J. Siahaan .2.1. Introduction .2.2. Physiological Barriers to Drug Delivery .2.2.1. Paracellular Pathway .2.2.2. Transcellular Pathway .2.3. Biochemical Barriers to Drug Delivery .2.3.1. Metabolizing Enzymes .2.3.2. Transporters and Efflux Pumps .2.4. Chemical Barriers to Drug Delivery .2.4.1. Hydrogen–Bonding Potential .2.4.2. Other Properties .2.5. Drug Modifications to Enhance Transport Across Biological Barriers .2.5.1. Prodrugs and Structural Modifications .2.5.2. Formulations .2.6. Conclusions .References .3 Physicochemical Properties, Formulation, and Drug Delivery Dewey H. Barich, Mark T. Zell, and Eric J. Munson .3.1. Introduction .3.2. Physicochemical Properties .3.2.1. Solubility .3.2.2. Stability .3.3. Formulations .3.3.1. Processing steps .3.3.2. Influence of physicochemical properties on drugs in formulations .3.3.3. Other issues .3.4. Drug Delivery .3.4.1. Duration of Release .3.4.2. Site of Administration .3.4.3. Methods of Administration .3.5. Conclusion .References .4 Targeted Bioavailability: A Fresh Look at Pharmacokinetics and Pharmacodynamics Issues in Drug Discovery and Development Christine Xu .4.1. Introduction .4.2. Target bioavailability .4.3. Drug delivery trends and targets related to pharmacokinetics and pharmacodynamics .4.4. Pharmacokinetics (PK) – pharmacodynamics (PD) in drug discovery and development .4.5. Source of variability of drug response .4.6. Recent development and issues of bio–analytical methodology .4.7. Mechanistic PK–PD models .4.8. Summary .References .5 The Role of Transporters in Drug Delivery and Excretion Marilyn E. Morris and Xiaowen Guan .5.1. Introduction .5.2. Drug Transport in absorption and excretion. .5.2.1. Intestinal transport .5.2.2. Hepatic Transport .5.2.3. Renal Transport .5.2.4. Blood–brain barrier transport .5.3. ABC (ATP–binding cassette) transporter family .5.3.1. P–glycoprotein (ABCB1) .5.3.2. Multidrug Resistance–associated Proteins (ABCC) .5.3.3. Breast Cancer Resistance Protein (ABCG2) .5.3.4. Other ABC transporters .5.4. SLC (solute carrier) transporter family .5.4.1. Organic Anion Transporting Polypeptides (SLCO) .5.4.2. Organic Anion Transporters (SLC22A) .5.4.3. Organic Cation Transporters (SLC22) .5.4.4. Multidrug and Toxin Extrusion Transporters (SLC47A) .5.4.5. Monocarboxylate Transporters (SLC16 and SLC5) .5.4.6. Peptide Transporters (SLC15A) .5.4.7. Other SLC transporters .5.5. Conclusions .References .6 Intracellular delivery and disposition of small molecular weight drugs Jeffrey Krise .6.1 Introduction .6.2. The relationship between the intracellular distribution of a drug and its activity .6.3. The relationship between the intracellular distribution of a drug and its pharmacokinetic properties .6.4 Overview of approaches to study intracellular drug disposition .6.4.1 Fluorescence microscopy .6.4.2 Organelle isolation .6.4.3 Indirect methods .6.5 The accumulation of drugs in mitochondria, lysosomes and nuclei .6.5.1 Mitochondrial accumulation of drugs .6.5.2 Lysosomal accumulation of drugs .6.5.3 Nuclear accumulation of drugs .6.6 Summary and future directions .References .7 Cell Culture Models for Drug Transport Studies Irina Kalashnikova, Norah Albekairi, Shariq Ali, Sanaalarab Al Enazy, and Erik Rytting .7.1. Introduction .7.2. General Considerations .7.3. Intestinal Epithelium .7.3.1. The Intestinal Epithelial Barrier .7.3.2. Intestinal Epithelial Cell Culture Models .7.4. The Blood–Brain Barrier .7.4.1. The Blood–Brain Endothelial Barrier .7.4.2. Blood–Brain Barrier Cell Culture Models .7.5. Nasal and Pulmonary Epithelium .7.5.1. The Respiratory Airway Epithelial Barrier .7.5.2. The Nasal Epithelial Barrier and Cell Culture Models .7.5.3. The Airway Epithelial Barrier and Cell Culture Models .7.5.4. The Alveolar Epithelial Barrier and Cell Culture Models .7.6. The Ocular Epithelial and Endothelial Barriers .7.6.1. The Corneal and Retinal Barriers .7.6.2. Cell Culture Models of Ocular Epithelium and Endothelium .7.7. The Placental Barrier .7.7.1. The Syncytiotrophoblast Barrier .7.7.2. Trophoblast Cell Culture Models .7.8. The Renal Epithelium .7.8.1. The Renal Epithelial Barrier .7.8.2. Renal Epithelial Cell Culture Models .7.9. 3D In Vitro Models .7.10. Conclusions .References .8 Intellectual Property and Regulatory Issues in Drug Delivery Research Wansheng Jerry Liu and Shahnam Sharareh .8.1. Introduction .8.2. Pharmaceutical Patents .8.3. Statutory Requirements for Obtaining a Patent .8.3.1. Patentable Subject Matter .8.3.2. Novelty .8.3.3. Non–Obviousness .8.4. Patent Procurement Strategies .8.5. Regulatory Regime .8.6. FDA Market Exclusivities .8.7. Regulatory and Patent Law Linkage .References .9 Presystemic and First–Pass Metabolism Qingping Wang and Meng Li .9.1. INTRODUCTION .9.2. HEPATIC FIRST–PASS METABOLISM .9.2.1. HEPATIC ENZYMES .9.3. INTESTINAL FIRST–PASS METABOLISM .9.3.1. INTESTINAL ENZYMES .9.3.2. INTERPLAY OF INTESTINAL ENZYMES AND TRANSPORTERS .9.4. PREDICTION OF FIRST–PASS METABOLISM .9.4.1. IN VIVO ASSESSMENT OF FIRST–PASS METABOLISM .9.4.2. IN VITRO ASSESSMENT OF FIRST–PASS METABOLISM .9.4.3. IN VITRO–IN VIVO PREDICTION .9.4.4. IN SILICO APPROACH .9.5. STRATEGIES FOR OPTIMIZATION ORAL BIOAVAILABILITY .9.6. SUMMARY .References .10 Pulmonary Drug Delivery Pharmaceutical Chemistry and Aerosol Technology Anthony J. Hickey .10.1. INTRODUCTION .10.2. AEROSOL TECHNOLOGY .10.2.1. Particle Production .10.2.2. Propellant Driven Metered Dose Inhalers (pMDIs) .10.2.3. Dry Powder Inhalers (DPIs) .10.2.4. Nebulizer .10.3. DISEASE THERAPY .10.3.1. Asthma .10.3.2. Emphysema .10.3.3. Cystic Fibrosis .10.3.4. Other Locally Acting Agents .10.3.5. Systemically Acting Agents .10.4. FORMULATION VARIABLES .10.4.1. Excipients .10.4.2. Interactions .10.4.3. Stability .10.5. Regulatory Considerations .10.6. FUTURE DEVELOPMENTS .10.7. CONCLUSION .References .11 Transdermal Delivery of Drugs Using Patches & Patchless Delivery Systems Tannaz Ramezanli, Krizia Karry, Zheng Zhang, Kishore Shah, Bozena Michniak–Kohn .11.1. Introduction .11.2. Transdermal patch delivery systems .11.2.1. Definition and history of patches .11.2.2. Anatomy and Designs of Patches .11.3. Patchless transdermal drug delivery systems .11.3.1. First–generation systems .11.3.2. Second–generation systems .11.3.3. Third–generation systems .11.4. Recent advances in transdermal drug delivery .11.4.1. Frontier in transdermal drug delivery: Transcutaneous immunization via microneedle techniques .11.4.2. Patchless Transdermal Delivery: The PharmaDur® Virtual Patch .11.5. Summary .References .12 Prodrug Approaches to Drug Delivery Longqin Hu .12.1. Introduction .12.2. Basic Concepts: definition and applications .12.2.1. Increasing lipophilicity to increase systemic bioavailability .12.2.2. Sustained–release prodrug systems .12.2.3. Improving gastrointestinal tolerance .12.2.4. Improving taste .12.2.5. Diminishing gastrointestinal absorption .12.2.6. Increasing water solubility .12.2.7. Tissue targeting and activation at the site of action .12.3. Prodrug design considerations .12.4. Prodrugs of various functional groups .12.4.1. Prodrugs of compounds containing COOH or OH .12.4.2. Prodrugs of compounds containing amides, imides, and other acidic NH .12.4.3. Prodrugs of Amines .12.4.4. Prodrugs for compounds containing carbonyl groups .12.5. Drug release and activation mechanisms .12.5.1. Cascade release facilitated by linear autodegradation reactions .12.5.2. Cascade release facilitated by intramolecular cyclization reactions .12.5.3. Cascade activation through intramolecular cyclization to from cyclic drugs .12.6. Prodrugs and intellectual property rights two court cases .References .13 Liposomes as Drug Delivery Vehicles Guijun Wang .13.1. Introduction .13.2. Currently approved liposomal drugs in clinical applications .13.3. Conventional and stealth liposomes .13.4. Stimuli–responsive liposomes or triggered release liposomes .13.4.1. General mechanism of triggered–release .13.4.2. Thermo–sensitive liposomes .13.4.3. pH–sensitive liposomes .13.4.4. Photo–triggered liposomes .13.4.5. Triggered release controlled by enzymes .13.5. Targeted liposomal delivery .13.6. Hybrid liposome drug delivery system .13.7. Conclusions and future perspectives .References .14 Nanoparticles as Drug Delivery Vehicles Dan Menasco and Qian Wang .14.1. Introduction .14.1.1. General DDV Properties .14.1.2. The DDV Core .14.1.3. DDV Targeting .14.1.4. DDV Size & Surface .14.2. Organic DDV s .14.2.1 Polymer Based Nanocarriers .14.2.2 Polymeric Micelles .14.2.3 Dendrimers .14.3. Inorganic DDV s .14.3.1. Mesoporous Silca Nanoparticles .14.3.2. Gold Nanoparticles .14.4. Conclusion .References .15 Evolution of Controlled Drug Delivery Systems Krishnaveni Janaparedd, Bhaskara R. Jasti, and Xiaoling Li .15.1 Introduction .15.2 Biopharmaceutics and Pharmacokinetics .15.3 Material Science .15.4 Proteins, Peptides and Nucleic acids .15.5 Targeted drug delivery .15.6 Microelectronics and Microfabrication Technologies .15.7 Conclusion .References .16 Pathways for Drug Delivery to the Central Nervous System Ngoc H. On, Vinith Yathindranath, ZhiZhi Sun, and Donald W. Miller .16.1. INTRODUCTION .16.1.1 Cellular Barriers to Drug Delivery in the CNS .16.1.2 General Approaches for Increasing Brain Penetration of Drugs .16.2. CIRCUMVENTING THE CNS BARRIERS .16.2.1 Intracerebraoventricular Injection (ICV) .16.2.2 Intracerebral Administration .16.2.3 Intranasal Delivery Route .16.3 TRANSIENT BBB DISRUPTION .16.3.1 Osmotic BBB Disruption .16.3.2 Pharmacological Disruption of the BBB .16.4 TRANSCELLULAR DELIVERY ROUTES .16.4.1. SLC Transport Systems in the BBB .16.4.2. ABC Transport Systems in the BBB .16.4.3 Vesicular Transport in the BBB .16.5 CONCLUSIONS .References .17 Metabolic Activation and Drug Targeting Xiangming Guan .17.1 Introduction .17.2. Anticancer prodrugs and their biochemical basis .17.2.1. Tumor–activated anticancer prodrugs based on hypoxia .17.2.2. Tumor–activated prodrugs based on elevated peptidases or proteases .17.2.3. Tumor–activated prodrugs based on other enzymes with elevated activities at tumor sites .17.3. Antibody– and gene– directed enzyme prodrug therapy (ADEPT and GDEPT) .17.3.1. ADEPT .17.3.2. GDEPT .17.4. Summary .References .18 Targeted Delivery of Drugs to the Colon Anil K. Philip and Sarah K. Zingales .18.1. Introduction .18.2. Microbially–triggered release .18.2.1. Azo–linked compounds .18.2.2. Amino acid conjugates .18.2.3. Sugar–derived prodrugs .18.3. pH–sensitive polymers for time–dependent release .18.4. Osmotic release .18.5. Pressure–controlled delivery .18.6. Nanoparticle approaches .18.7. Conclusion .References .19 Receptor–mediated Drug Delivery Chris V. Galliford and Philip S. Low .19.1. Introduction .19.2. Selection of a Receptor for Drug Delivery .19.2.1. Specificity .19.2.2. Receptor Internalization/Recycling .19.3. Design of a Ligand–drug Conjugate .19.3.1. Linker Chemistry .19.3.2. Selection of Ligands .19.3.3. Selection of Therapeutic Drug .19.4. Folate–mediated Drug Delivery .19.4.1. Expression of Folate Receptors in Malignant Tissues .19.4.2. Expression of Folate Receptors in Normal Tissues .19.4.3. Applications of Folate–mediated Drug delivery .19.5. Conclusions .References .20 Protein and Peptide Conjugates for Targeting Therapeutics and Diagnostics to Specific Cells Barlas Büyüktimkin, John Stewart Jr., Kayann Tabanor, Paul Kiptoo, and Teruna J. Siahaan .20.1. Introduction .20.2. Radiolabeled Antibodies for Cancer Treatment .20.3. Antibody Drug Conjugate (ADC) .20.3.1. Sites of Conjugation on MABS, Linkers, And Drugs .20.4. Non–Antibody–Based Protein–Drug Conjugates .20.5. Peptibody .20.6. Protein Conjugates for Diagnostics .20.7. Peptide–Drug Conjugates .20.8. Challenges in Analyzing Conjugates .20.9. Conclusions .References .21 Drug delivery to the lymphatic system Qiuhong Yang and Laird Forrest .21.1. Introduction .21.2. Anatomy and physiology of the lymphatic system .21.2.1. Lymph .21.2.2. Lymphatic vessels .21.2.3. Lymph nodes .21.2.4. Lymph organs .21.3. Influence of physicochemical characteristics of drug carriers on lymphatic uptake and transport .21.3.1. Size .21.3.2. Surface charge .21.3.3. Hydrophobicity .21.4. Carriers for lymphatic drug delivery .21.4.1. Liposomes .21.4.2. Lipid–based emulsions and nanoparticles .21.4.3. Polymer–based carriers .21.5. Administration routes for lymphatic delivery .21.5.1. Intestinal .21.5.2. Pulmonary .21.5.3. Subcutaneous .21.5.4. Intraperitoneal .21.6. Lymphatic–targeting Vaccination .21.7. Conclusions .References .22 The Development of Cancer Theranostics: a New Emerging Tool towards Personalized Medicine Hongying Su, Yun Zeng, Gang Liu, and Xiaoyuan Chen .22.1. Introduction .22.2. Imaging–Guided Drug Delivery and Therapy .22.3. Optical Imaging–Based Theranostics .22.3.1. NIR Fluorescence Imaging .22.3.2. Bioluminescence Imaging .22.3.3 Gold Nanoparticle as a Theranostics Platform .22.3. MRI–Based Theranostics .22.4. Nuclear Imaging–Based Theranostics .22.5. Ultrasound–Based Theranositic Platform .22.6. Multimodality Imaging–Based Theranostic Platform .22.6.1. PET/CT .22.6.2. MRI/Optical .22.6.3. MRI/PET .22.7. Conclusion and Future Perspectives .Acknowledgements .References .23 Intracellular delivery of proteins and peptides Can Sarisozen and Vladimir P. Torchilin .23.1. Introduction .23.2. Intracellular Delivery Strategies of Peptides and Proteins .23.3. Concepts in Intracellular Peptide and Protein Delivery .23.3.1. Longevity in the Blood .23.3.2. Cellular Uptake Pathways .23.3.3. Endosomal Escape .23.4. Peptide and Protein Delivery to Lysosomes .23.5. Receptor–mediated intracellular delivery of peptides and proteins .23.5.1. Transferrin receptor–mediated delivery .23.5.2. Folate receptor–mediated delivery .23.6. Transmembrane delivery of peptides and proteins .23.6.1. Well studied classes of CPPs for peptide and protein delivery .23.6.2. Cellular uptake mechanisms of CPPs .23.6.3. CPP–mediated delivery of peptides and proteins .23.6.4. CPP–modified carriers for intracellular delivery of peptides and proteins .23.7. Conclusions .References .24 Vaccine Delivery: Current Routes of Administration and Novel Approaches Neha Sahni, Yuan Cheng, C. Russell Middaugh, David B. Volkin .24.1. Introduction .24.2. Parenteral Administration of Vaccines .24.2.1 Currently available vaccines and devices for intramuscular and subcutaneous delivery .24.2.2 Currently available vaccines and devices for intradermal administration .24.2.3 Novel devices for parenteral injection .24.2.4 Novel formulations and delivery approaches for parenteral injection .24.3. Oral Delivery of Vaccines .24.3.1 Currently available orally administered vaccines .24.3.2 Novel formulations and delivery approaches for oral administration .24.4. Nasal and Aerosol Delivery of Vaccines .24.4.1 Currently available nasally administered vaccines .24.4.2 Novel devices and formulations for nasal administration .24.4.3 Devices and delivery systems for aerosol administration .24.5. Conclusions .References .25. Delivery of Genes and Oligonucleotides Charles M. Roth .25.1. Introduction .25.2. Systemic Delivery Barriers .25.2.1. Viruses: Learning from Nature .25.2.2. Materials for Nucleic Acid Delivery .25.2.3. Characterization of Nanoparticles .25.2.4. Targeted Delivery of Nucleic Acids .25.3. Cellular Delivery Barriers .25.3.1. Endosomal Escape .25.3.2. Vector Unpackaging .25.4. Current and Future Approaches to Nucleic Acid Delivery .25.4.1. Vectors in the Clinic .25.4.2. Combinatorial Chemistry Approaches .25.4.3. Polymer–Lipid Nanocomposites .25.5. Summary and Future Directions .References .Index

• ISBN: 978-1-118-83336-0
• Editorial: Wiley–Blackwell
• Encuadernacion: Rústica
• Páginas: 720
• Fecha Publicación: 13/05/2016
• Nº Volúmenes: 1
• Idioma: Inglés