DENDRIMER-BASED DRUG DELIVERY SYSTEMS: From Theory to Practice -- Contents -- Foreword -- Preface -- Acknowledgments -- Contributors -- About the Editor -- 1 Dendrimer Chemistry: Supramolecular Perspectives and Applications -- 1.1. INTRODUCTION -- 1.1.1. Historical Background -- 1.1.2. Architectural Concepts -- 1.1.3. Initial Reduction to Practice -- 1.2. SUPRAMOLECULAR PERSPECTIVES -- 1.2.1. Unimolecular Micelles-The Advent of the Container -- 1.2.2. Framework Conformational Control -- 1.2.3. Harnessing Electronic Properties -- 1.2.4. Drug Delivery Systems -- 1.2.5. Dendritic Self-Assembly, Sensors, and Devices -- 1.3. CONCLUSIONS -- REFERENCES -- 2 Physicochemical Properties of Dendrimers and Dendrimer Complexes -- 2.1. INTRODUCTION -- 2.2. DENDRIMERS -- 2.2.1. PAMAM Dendrimers -- 2.2.2. Other Dendrimers -- 2.3. PHYSICOCHEMICAL PROPERTIES OF DENDRIMERS -- 2.3.1. Static and Dynamic Structures -- 2.3.2. Doping Property -- 2.3.3. Adsorption and Aggregation Properties -- 2.3.4. Luminescence Property -- 2.4. DENDRIMER COMPLEXES -- 2.4.1. Complexes with Functional Molecules -- 2.4.2. Complexes with Polymers -- 2.4.3. Complexes with Inorganic Materials -- 2.5. CONCLUSIONS -- REFERENCES -- 3 The Use of Dendrimers to Optimize the Physicochemical and Therapeutic Properties of Drugs -- 3.1. INTRODUCTION -- 3.2. NEOPLASTIC DISORDERS -- 3.3. GASTROINTESTINAL TRACT -- 3.4. CARDIOVASCULAR SYSTEM -- 3.5. CENTRAL NERVOUS SYSTEM -- 3.6. PAIN AND CONSCIOUSNESS -- 3.7. EYE -- 3.8. EAR, NOSE, AND OROPHARYNX -- 3.9. RESPIRATORY SYSTEM -- 3.10. SKIN -- 3.11. INFECTIONS AND INFESTATIONS -- 3.12. IMMUNE SYSTEM -- 3.13. CONCLUSIONS -- REFERENCES -- 4 Biological Properties of Phosphorus Dendrimers -- 4.1. INTRODUCTION -- 4.2. SYNTHESIS AND FUNCTIONALIZATION OF PHOSPHOROUS-CONTAINING DENDRIMERS FOR BIOLOGICAL PURPOSES -- 4.3. CYTOTOXICITY ASSAYS OF PHOSPHORUS DENDRIMERS.

4.4. PHOSPHORUS DENDRIMERS FOR BIOLOGICAL IMAGING -- 4.5. PHOSPHORUS DENDRIMERS AS NANO-CARRIERS -- 4.5.1. Electrostatic Interactions with One Drug per Terminal Function -- 4.5.2. Electrostatic Interactions for Transfection Experiments -- 4.6. PHOSPHORUS DENDRIMERS AS DRUGS BY THEMSELVES -- 4.6.1. Antiprion Activity of Phosphorus Dendrimers -- 4.6.2. Stimulation of the Human Immune System -- 4.7. CONCLUSIONS -- REFERENCES -- 5 Dendrimer-Based Prodrugs: Synthesis and Biological Evaluation -- 5.1. INTRODUCTION -- 5.2. DESIGN OF DENDRIMER-BASED PRODRUGS -- 5.2.1. A Theoretical Perspective -- 5.2.2. Factors Affecting Linker Selection and Drug Release -- 5.3. SYNTHESIS AND CHARACTERIZATION OF DENDRIMER-BASED PRODRUGS -- 5.3.1. NSAID Prodrugs -- 5.3.2. Anticancer Prodrugs -- 5.3.3. Prodrugs of P-Glycoprotein Substrates -- 5.3.4. Acetylcysteine Prodrugs -- 5.3.5. Colchicine Prodrugs -- 5.3.6. Drug-Integrated Dendrimers -- 5.4. IN VITRO STABILITY OF DENDRIMER-BASED PRODRUGS -- 5.4.1. Chemical Stability -- 5.4.2. Enzymatic Stability -- 5.5. IN VITRO CYTOTOXICITY OF DENDRIMER-BASED PRODRUGS -- 5.6. IN VITRO PERMEABILITY OF DENDRIMER-BASED PRODRUGS -- 5.7. CONCLUSIONS -- REFERENCES -- 6 Improving the Biocompatibility of Dendrimers in Drug Delivery -- 6.1. INTRODUCTION -- 6.2. SAFETY ISSUES OF DENDRIMERS -- 6.3. DESIGNING OF BIOCOMPATIBLE DENDRIMERS FOR THERAPEUTIC PURPOSES -- 6.3.1. Construction of Novel Biocompatible Dendrimers -- 6.3.1.1. Construction of Dendrimers with Biocompatible Units -- 6.3.1.2. Construction of Long-Circulation Dendrimers -- 6.3.1.3. Construction of Cleavable Dendrimers -- 6.3.2. Modification of Already Established Dendrimers -- 6.3.2.1. PEGylated Dendrimers -- 6.3.2.2. Acetylated Dendrimers -- 6.3.2.3. Glycosylated Dendrimers -- 6.3.2.4. Other Functionalized Dendrimers -- 6.4. CONCLUSIONS -- REFERENCES.

7 Degradable Dendrimers for Drug Delivery -- 7.1. INTRODUCTION -- 7.1.1. Literature Survey and Historical Aspects -- 7.1.2. Content and Objectives -- 7.1.3. Survey of Applications of Degradable Dendrimers in Drug Delivery -- 7.2. DENDRIMER-DRUG CONJUGATES AS PRODRUGS -- 7.2.1. Importance of Dendritic Architectures -- 7.2.2. Biocompatibility and Toxicity of Dendrimers -- 7.2.3. Improving the Therapeutic Index: Targeting, Cellular Uptake, Biodistribution, and Drug Persistence -- 7.3. ANTICANCER DENDRIMER-DRUG CONJUGATES -- 7.3.1. Fluorouracil (5-FU) -- 7.3.2. Methotrexate (MTX) -- 7.3.3. Doxorubicin (DOX) -- 7.3.4. Paclitaxel (PTX) -- 7.3.5. Camptotecin (CPT) -- 7.3.6. Lamellarin D -- 7.3.7. Etoposide -- 7.3.8. Chlorambucil -- 7.3.9. Melphalan and Bendamustine -- 7.3.10. Colchicine -- 7.3.11. Epirubicin -- 7.3.12. Tubulysin -- 7.3.13. Other Drugs Bound to PAMAM Dendrimers -- 7.3.14. Metal-Based Anticancer Drugs -- 7.3.14.1. Platinum -- 7.3.14.2. Ruthenium -- 7.3.14.3. Radioactive Metals -- 7.4. ANTICANCER MULTIFUNCTIONAL DENDRITIC PLATFORMS WITH TARGETING UNITS -- 7.5. ANTICANCER DENDRITIC PLATFORMS FOR POLYTHERAPY -- 7.6. ANTIINFLAMATORY DENDRIMER-DRUG CONJUGATES -- 7.6.1. Nonsteroidal Dendrimer Conjugates -- 7.6.1.1. Aceclofenac -- 7.6.1.2. Ibuprofen -- 7.6.1.3. Naproxen -- 7.6.1.4. N-acetyl-L-cysteine -- 7.6.2. Steroidal Dendrimer Conjugates -- 7.6.2.1. Methylprednisolone -- 7.6.2.2. Cholesterol -- 7.6.2.3. Dexamethasone -- 7.6.3. Antiinflammatory Eye Delivery -- 7.6.3.1. Glucosamine -- 7.6.3.2. Carteolol -- 7.7. ANTIBACTERIAL AND ANTIMICROBIAL DENDRIMER-DRUG CONJUGATES -- 7.7.1. Penicillin V -- 7.7.2. Desferrioxamine B -- 7.7.3. Amphotericin B -- 7.7.4. Other Antileishmanial and Antichagasic Drugs -- 7.7.5. Other Dendrimer-Drug Conjugates -- 7.8. CONCLUDING REMARKS -- ACKNOWLEDGMENTS -- REFERENCES.

8 Design of Stimuli-Responsive Dendrimers for Biomedical Purposes -- 8.1. INTRODUCTION -- 8.2. PEGYLATED DENDRIMERS WITH CONTROLLED RELEASE PROPERTIES -- 8.2.1. PEGylated Dendritic Polymers with pH-Sensitivity -- 8.2.2. PEGylated Dendritic Polymers with Light-Sensitivity -- 8.2.3. PEGylated Dendrimers with Middle-Layered Shells -- 8.3. TEMPERATURE-DEPENDENT DENDRITIC POLYMERS -- 8.3.1. Dendritic Polymers Modified with Thermo-Sensitive Polymers -- 8.3.2. Dendrimers Containing Thermo-Sensitive Moieties -- 8.4. COLLAGEN-MIMIC DENDRIMERS AND DENDRIMER-BASED HYDROGELS -- 8.4.1. Collagen-Mimic Dendrimers -- 8.4.2. Dendrimer-Based Hydrogels -- 8.5. CONCLUSION -- ACKNOWLEDGMENTS -- REFERENCES -- 9 Dendrimer-Based Gene Delivery Systems: Administration Routes and In Vivo Evaluation -- 9.1. INTRODUCTION -- 9.2. DENDRIPLEXES AS VECTORS -- 9.2.1. Dendrimers Used in Gene Therapy -- 9.2.2. Electrostatic Interactions and the Role of Charge Ratios -- 9.2.3. Dendrimer Generation -- 9.2.4. The Role of Dendrimer Architecture -- 9.2.5. The Role of Dendrimer Chemistry and Modification -- 9.2.6. The Bulk Environment -- 9.3. TRANSFECTION OF CELLS -- 9.3.1. Uptake -- 9.3.2. Intracellular Trafficking -- 9.4. GENE DELIVERY IN VIVO -- 9.4.1. The Physiological Environment as Barrier -- 9.4.2. Protein Adsorption and Corona Formation on NPs -- 9.4.3. The Effects of Corona Formation on NP Properties -- 9.4.4. Local and Topical Gene Therapy -- 9.4.5. Systemic Gene Therapy -- 9.5. CONCLUSIONS -- REFERENCES -- 10 Triazine Dendrimers for DNA and siRNA Delivery: Progress, Challenges, and Opportunities -- 10.1. INTRODUCTION -- 10.1.1. Viruses Lead the Way -- 10.1.2. Nonviral Carriers Become More Appealing -- 10.1.2.1. Physical Methods of Gene Delivery -- 10.1.2.2. Liposomes -- 10.1.2.3. Polymers -- 10.1.2.4. Dendrimers -- 10.2. TRIAZINE DENDRIMERS: EARLY SYNTHETIC ACHIEVEMENTS.

10.3. TRIAZINE DENDRIMERS FOR TRANSFECTION: SELECTION CRITERIA FOR STRUCTURES -- 10.3.1. Surface Groups -- 10.3.1.1. Hydroxyl Groups: Reducing Cytotoxicity -- 10.3.1.2. Hydrophobic Groups: Stabilizing Complex Formation or Improving Endosomal Escape -- 10.3.1.3. Guanidines: Improving Binding and Cellular Uptake -- 10.3.2. Core Manipulations -- 10.3.2.1. Higher Generation -- 10.3.2.2. Rigid versus Flexible -- 10.4. DNA TRANSFECTION USING TRIAZINE DENDRIMERS -- 10.4.1. Binding Affinity -- 10.4.1.1. Effect of Peripheral Groups -- 10.4.1.2. Effect of the Core -- 10.4.2. Size and Charge -- 10.4.3. Cytotoxicity -- 10.4.3.1. Cytotoxicity -- 10.4.3.2. Hemolysis -- 10.4.3.3. Aggregation of Erythrocytes -- 10.4.4. Transfection Efficiency -- 10.4.4.1. Effect of the Peripheral Groups -- 10.4.4.2. Effect of the Core: Generation and Flexibility -- 10.5. siRNA TRANSFECTION USING TRIAZINE DENDRIMERS -- 10.5.1. Binding Properties -- 10.5.1.1. Binding Affinity -- 10.5.1.2. Effect of the Peripheral Groups -- 10.5.1.3. Effect of the Core: Generation and Flexibility -- 10.5.1.4. Complex Stability -- 10.5.1.5. Effect of the Peripheral Groups -- 10.5.1.6. Effect of the Core: Generation and Flexibility -- 10.5.2. Size and Charge -- 10.5.2.1. Effect of the Peripheral Groups on the Size -- 10.5.2.2. Effect of the Core on the Size: Generation and Flexibility -- 10.5.2.3. Effect of the Peripheral Groups on the Zeta Potential -- 10.5.2.4. Effect of the Core on the Zeta Potential: Generation and Flexibility -- 10.5.3. Uptake and Subcellular Distribution -- 10.5.3.1. Effect of the Peripheral Groups on Uptake -- 10.5.3.2. Effect of the Core on Uptake: Generation and Flexibility -- 10.5.3.3. Effect of the Peripheral Groups -- 10.5.3.4. Effect of the Core: Generation and Flexibility -- 10.5.4. Transfection Efficiency -- 10.5.4.1. Effect of the Peripheral Groups.

10.5.4.2. Effect of the Core: Generation and Flexibility.