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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5640_Библиотеки_им_академика_М_И_Перельмана.pdf
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- •Preface
- •Contents
- •Contributors
- •1. Introduction
- •2. The Initial Phase of Drug Delivery Systems
- •3. Recent Drug Delivery Systems
- •4. Drug Delivery via Carriers
- •5.4 Polymer-Lipid Hybrid Nanoparticles Drug Delivery System
- •5.5 Self-Micro Emulsifying Drug Delivery System
- •5.6 In Situ Gel Drug Delivery System
- •5.8 Targeted Drug Delivery
- •6. Ceramic-Based Drug Delivery System
- •7. Polysaccharide-Based Drug Delivery System
- •8. Closed Loop Insulin Delivery System
- •9. Liposome-Mediated Drug Delivery
- •5. Recent Drug Delivery Systems
- •5.3 Hexagonal Boron Nitride Nanosheet Drug Delivery System
- •10. Dendrimers
- •11. PEGylated Drug Delivery System
- •12. Antibody-Drug Conjugate System
- •13. Mesoporous Silica-Based Drug Delivery
- •14. Transdermal Drug Delivery System
- •15. Hydrogel-Mediated Ocular Drug Delivery
- •16. Challenges with Current Drug Delivery Systems
- •17. Future Direction and Conclusion
- •References
- •1. Introduction
- •2. Pharmacokinetic Principles
- •2.1 Application of the Pharmacokinetic Principle in the Biomedical Fields
- •3. Cell Membrane/Biological Membrane
- •3.1 Passage of Drugs Across Biological Membranes
- •3.1.1 Simple Transport
- •3.1.2 Specialized Transport
- •4. Routes of Drug Administration
- •4.1 Oral (Enteral) Versus Parenteral Administration
- •4.2 Various Routes of Drug Administration
- •5. Absorption
- •5.1 Factors Affecting Absorption of Drugs
- •5.1.1 Physio-chemical Characteristics
- •5.1.2 Dosage Form
- •5.1.3 Concentration and Volume
- •5.1.4 Blood Flow
- •5.1.5 Surface Area
- •5.1.6 Administration Route
- •5.1.7 Disease States
- •5.2 Gastrointestinal Tract
- •5.3 Parenteral Sites
- •5.4 Pulmonary Sites (Alveoli)
- •5.5 Topical Sites
- •6. Distribution
- •6.1 Factors Affecting Distribution of Drugs
- •6.1.1 Physicochemical Properties of the Drug
- •6.1.2 Binding to Plasma and Tissue Proteins
- •6.1.3 Blood Flow and Organ Size
- •6.1.4 Specialized Compartments and Barriers
- •6.1.5 Specialized Transport Systems
- •6.1.6 Disease States
- •6.1.7 Physiological Factors
- •7. Metabolism/Biotransformation
- •7.1 Functions of Metabolism
- •7.2 Sites of Metabolism
- •7.3.1 Microsomal Enzymes
- •7.3.2 Non-microsomal Enzymes
- •7.4 Pathways of Biotransformation
- •8. Excretion
- •8.1 Routes of Excretion
- •8.1.1 Renal Excretion of Drugs
- •8.1.2 Extra-Renal Excretion of Drugs
- •9.1 Minimum Effective Concentration (MEC)
- •9.2 Maximum Safe Concentration (MSC) or Minimum Toxic Concentration (MTC)
- •9.4 Area Under the Curve (AUC)
- •9.5 Peak Effect
- •9.7 Onset of Action
- •9.8 Onset Time
- •9.9 Duration of Action
- •10. Order of Pharmacokinetic Processes
- •10.1 Zero-Order Kinetics
- •10.2 First-Order Kinetics
- •10.3 Mixed-Order Kinetics
- •11. Pharmacokinetic Models
- •11.1 Compartmental Models
- •11.3 Physiological Models
- •12. Determinants of Pharmacokinetics
- •12.1 Absorption
- •12.1.1 Bioavailability
- •12.1.2 Bioequivalence
- •12.1.3 Area Under Curve (AUC)
- •12.2 Distribution
- •12.2.1 Volume of Distribution
- •12.3 Elimination
- •12.3.2 Clearance (Cl) or Body Clearance
- •13. Conclusion
- •References
- •1. Introduction
- •2. Principles of Targeted Drug Delivery
- •3.1 Changes in pH and Salt Development
- •3.7 Dendrimers
- •4.1 Small-Sized Molecule-Based Targeting Strategies
- •4.2 Nucleic Acid Fragment-Based Targeting Strategies
- •4.3 Peptide- and Antibody-Based Targeting Strategies
- •4.4 Cell-Based Targeting Strategies
- •5. Conclusion
- •References
- •3.4 Liposomes
- •3.5 Solid Lipid Nanoparticles
- •3.6 Co-crystal Preparation
- •1. Introduction
- •2. History
- •3.1 Organic Nanoparticles
- •3.2 Inorganic Nanoparticles
- •4. Nanotechnology-Based Drug Delivery Systems
- •4.1 Smart Drug Delivery Systems
- •4.3 Multifunctional Drug Carriers
- •4.4 Organic/Inorganic Composites
- •5. Nanoparticulate Drug Delivery Systems
- •5.1 Liposomes
- •5.2 Microemulsions
- •5.3 Nanoparticles
- •6. Applications
- •6.1 Enhanced Drug Delivery
- •6.2 Overcoming Biological Barriers
- •6.3 Controlled Drug Release
- •6.4 Combination Therapy
- •6.5 Personalized Medicine
- •7. Limitations
- •7.1 Complexity and Cost
- •7.2 Biocompatibility and Toxicity
- •7.3 Stability and Shelf Life
- •7.4 Drug Loading and Release
- •7.5 Biological Barriers and Clearance
- •8. Conclusions
- •References
- •1. Introduction
- •2. Guidelines for Design of Lipid-Based Formulations
- •3. Formulation Strategies
- •3.1 Lipid Nanoparticles
- •3.1.1 Solid Lipid Nanoparticles (SLNs)
- •3.1.2 Nanostructured Lipid Carriers (NLCs)
- •3.2 Liposomes
- •3.2.1 Conventional Liposomes
- •3.2.2 PEGylated Liposomes
- •3.2.3 Multifunctional Liposomes
- •3.3 Microemulsions and Self-micro Emulsifying Drug Delivery Systems (SMEDDS)
- •3.4 Hybrid Systems
- •3.4.1 Lipid-Polymer Hybrid Nanoparticles
- •3.4.2 Lipid-Protein Hybrid Systems
- •4. Advanced Characterization Methods
- •4.1 In Vitro and In Vivo Assessment
- •4.1.1 Dissolution Studies
- •4.1.2 Permeability Studies
- •4.2 Imaging Techniques
- •4.2.1 Electron Microscopy
- •4.2.2 Fluorescence Imaging
- •Fluorescent Probes
- •Confocal Microscopy
- •4.2.3 Magnetic Resonance Imaging (MRI)
- •4.3 Stability Studies
- •4.3.1 Oxidative Stability
- •4.3.2 Thermal Stability
- •5. Applications of Lipid-Based Drug Delivery Systems
- •5.1 Cancer Therapy
- •5.1.1 Targeted Drug Delivery
- •5.1.2 Combination Therapy
- •5.2 Central Nervous System Disorders
- •5.2.2 Neuroprotective Effects
- •5.3 Antiviral and Antimicrobial Applications
- •5.3.1 Lipid Nanoparticles for Antiviral Drugs
- •5.3.2 Antibiotic Delivery Systems
- •6. Future Perspectives and Challenges
- •7. Conclusion
- •References
- •1. Introduction
- •3. Design and Characterization of Polymeric Drug Delivery Systems
- •4. Responsive Polymers
- •4.1 Polymeric Hydrogels
- •4.1.1 Characterization of Polymeric Hydrogels
- •Structural Analysis
- •Functional Analysis
- •4.2 Polymeric Micelles
- •4.2.1 Characterization of Polymeric Micelle
- •Critical Micelle Concentration Determination (CMC)
- •Morphological Characterization
- •Physicochemical Characterization
- •4.3 Liposomes
- •4.3.1 Ethosome
- •4.3.2 Transferosome
- •4.3.3 Niosome
- •4.4 Polyplexes or Polymer-Drug Conjugates
- •4.4.1 Dendrimers
- •4.4.2 Polymer-Protein Conjugates
- •4.4.3 Polymeric Nanoparticles
- •5. Conclusion
- •6. Future Prospects
- •References
- •1. Introduction
- •2.1 Types of Stimuli
- •3. Mechanism of Stimuli Responsiveness
- •3.1 pH-Responsive Systems
- •4. Materials
- •4.1 pH-Responsive Materials
- •4.4 Synthetic Thermo-Responsive Materials
- •4.7 Magnetic Responsive Materials
- •4.8.1 Intrinsically Conducting Polymers
- •4.8.2 Hydrogels
- •5. Methods
- •5.1 pH-Responsive Drug Delivery Systems
- •6. Conclusion
- •7. Notes
- •References
- •1. Introduction
- •3. Basic Features Required for the Biomaterial
- •4. Characteristics of Biomaterials
- •6. Biocompatibility as the Crucial Item
- •7. Biomaterials in Drug Delivery
- •8. Controlled Drug Delivery
- •9. Clinical Need for Controlled Drug Delivery
- •10. Biomaterials for Controlled Release of Small Molecules
- •11. Bioresponsive Polymers: From Design to Implementation
- •11.3 Hydrolysis and Enzymatically Responsive Polymers
- •11.7 Swelling and Contracting Polymers
- •12. Transdermal Drug Delivery Systems
- •12.1 Barriers to Transdermal Delivery
- •12.2 Development of Transdermal Drug Delivery Patches
- •12.3 Hydrogels Versus Non-hydrogel Polymeric Patches
- •12.4 Patches Based on Biopolymers
- •12.5 Patches Based on Synthetic Polymers
- •12.6 Drug Particles/Carriers
- •12.7 Commercial Patches
- •13. Smart Biomaterials
- •14. Conclusion and Future Perspective
- •References
- •1. Introduction
- •1.1 Historical Evolution
- •2. Skin Anatomy and Physiology
- •2.1 Cutaneous Layer Organization
- •2.2 Cutaneous Barrier Function
- •3. Mechanisms of Transdermal Drug Delivery
- •4. Formulation Strategies for Transdermal Drug Delivery
- •4.1 Drug Selection Criteria
- •4.2 Vehicle and Excipient Considerations
- •4.3 Permeation Enhancers
- •4.4 Transdermal Drug Delivery Technologies
- •5. Evaluation Methods for Transdermal Drug Delivery Systems
- •6. Applications of Transdermal Drug Delivery
- •6.1 Therapeutic Areas
- •6.2 Case Studies of Successful Transdermal Products
- •7. Regulatory Considerations and Approval Process
- •7.1 FDA Guidelines for Transdermal Drug Delivery Systems
- •7.2 Quality Control and Manufacturing Standards
- •7.3 Clinical Trial Requirements
- •8. Challenges and Future Perspectives
- •8.1 Overcoming Cutaneous Barrier Properties
- •8.2 Expanding the Range of Deliverable Drugs
- •8.3 Intelligent and Responsive Transdermal Systems
- •8.4 Integration with Other Drug Delivery Technologies
- •8.5 Conclusion
- •References
- •1. Background
- •2. Importance of the Tumor Microenvironment (TME) in Cancer Progression and Therapy
- •2.1 Components of the TME
- •2.2 Therapeutic Targeting of the TME
- •2.3 Impact of Standard Therapies on the TME
- •3. Tumor-Homing Peptides
- •3.1 Different Strategies for Targeting Peptides to Tumor Microenvironment
- •3.2 Applications and Development
- •3.3 Examples and Discoveries
- •4. Tumor Microenvironment Responsive Drug Delivery Systems (DDSS)
- •5. Nanoparticle-Based Smart Drug Delivery Systems
- •5.1.1 Endogenous Stimulus-Responsive Drug Delivery Systems (DDSs)
- •5.1.2 Exogenous Stimulus-Responsive DDSs
- •5.2.2 Dynamic Strategies for Tumor Targeting
- •6. Challenges and Opportunities for Targeted Delivery to Cancer Cells
- •7. Future Directions
- •8. Conclusions
- •References
- •1. Introduction
- •2. Materials
- •2.1 Types of Biosensors
- •2.1.2 Smart Polymers
- •2.1.3 Microfabricated Devices
- •2.2.1 Enzyme-Based Biosensors
- •2.2.2 Antibody-Based Biosensors
- •2.2.3 Aptamer-Based Biosensors
- •2.2.4 Whole-Cell-Based Biosensors
- •3. Methods
- •3.1 Approach Toward Designing Biosensors
- •3.1.1 Selection of the Analyte and Bioreceptors
- •3.1.2 Immobilization of Biosensors
- •3.1.3 Selection of Transducer
- •3.2 Green Biosensors
- •3.3 Challenges in Development of Biosensors-Based Drug Delivery Systems
- •References
- •1. Introduction
- •3. Ocular Barriers Hindering Absorption of Drugs
- •3.1 Precorneal Barriers
- •3.1.1 Tear Film, Tear Turnover, and Nasolacrimal Duct Drainage
- •3.1.3 Conjunctival and Scleral Barriers
- •3.2 Corneal Barrier
- •3.3 Blood-Ocular Barriers
- •4. Various Routes for Ocular Drug Delivery
- •4.1 Topical Administration
- •4.2 Subconjunctival Administration
- •4.3 Transscleral Administration
- •4.4 Intracameral Administration
- •4.5 Intravitreal Injections/Implants (IVIs)
- •4.6 Retrobulbar Administration
- •4.7 Systemic Administration
- •5. Nanotechnology-Based Ocular Drug Delivery Platforms
- •5.1 Nanoparticles (NPs)
- •5.1.1 Polymeric Nanoparticles (PNPs)
- •5.2 Nanomicelles
- •5.3 Nanoemulsions (NEs)
- •5.4 Nanosuspensions
- •5.5 Nanocrystals (NCs)
- •5.6 Liposomes
- •5.7 Microemulsions
- •5.8 Niosomes
- •5.10 Dendrimers
- •5.11 Nanowafers
- •5.12 Cubosomes
- •5.13 Bilosomes
- •5.14 Olaminosomes
- •5.15 Contact Lenses
- •5.16 Hydrogels
- •5.17 Microneedles (MNs)
- •6. Alternative Ocular Drug Delivery Approaches
- •6.1 Gene Therapy
- •6.1.1 Viral Vectors
- •6.1.2 Non-viral Vectors
- •6.1.3 Antisense Oligonucleotides (ASOs), RNAi, CRISPR-Cas9
- •6.2 Exosomes
- •6.3 Self-nano Emulsifying Drug Delivery Structures (SNEDDS)
- •7. Clinical Status of Nanotechnology-Based Ocular Drug Delivery Systems
- •8. Future Outlooks
- •References
- •1. Introduction
- •2. Anatomy and Physiology of GIT
- •2.1 Mouth and Esophagus
- •2.2 Stomach
- •2.3 Small Intestine
- •2.4 Ruminant Digestive System
- •3. Blood Supply
- •4. Nerve Supply
- •5. Challenges in GIT Drug Delivery
- •5.1 Acidic Environment of the Stomach
- •5.2 Alkaline pH of the Intestine
- •5.3 Variable GI Transit Times
- •6. Future Opportunities in GIT Drug Delivery
- •6.1.1 Targeted Delivery Systems
- •6.1.2 Ligand-Conjugated Nanoparticles
- •6.1.3 Liposomes
- •6.1.4 Solid Lipid Nanoparticles
- •6.2 Controlled Release Systems
- •6.2.1 Osmotic Pumps
- •6.2.2 Matrix Systems
- •6.3 Mucoadhesive Systems
- •6.3.1 Mucoadhesive Polymers
- •6.4 Absorption Enhancers
- •6.5 Tight Junction Modulators
- •6.6 Development of Prodrugs
- •7. Conclusion
- •References
- •1. Introduction
- •2. Anatomy and Physiology of the Respiratory System
- •3. Traditional Methods of Respiratory Drug Delivery
- •3.1 Metered-Dose Inhalers (MDIs)
- •3.2 Dry Powder Inhalers (DPIs)
- •3.3 Nebulizers
- •3.5 Improved Patient Compliance Through User-Friendly Devices
- •3.8 Enhanced Absorption by Overcoming Biological Barriers
- •3.9 Macromolecule Delivery Facilitation
- •3.10 Reduced Side Effects Through Improved Targeting
- •3.11 Formulation Challenges Addressed
- •3.12 Smart Technology Integration for Personalized Treatment
- •3.13 Environmental Sustainability Considerations
- •4. Novel Drug Delivery Approaches
- •4.2 Liposomal Formulations
- •5. Advanced Inhalation Devices
- •6. Targeted Drug Delivery Strategies
- •6.2 pH-Responsive Drug Release
- •7. Emerging Therapeutics for Respiratory Diseases
- •8.2 Combination Therapies
- •8.3 Prodrug Approaches
- •9. Personalized Medicine in Respiratory Drug Delivery
- •10. Future Perspectives and Emerging Technologies
- •10.1 3D-Printed Inhalers
- •11. Conclusion
- •References
- •1. Introduction
- •2. Delivery of Small Molecules
- •3. Drawbacks of Conventional Drug Delivery System
- •4. Factors Affecting Cardiovascular Drug Targeting System
- •4.1 Particle Shape
- •4.2 Particle Size
- •4.3 Particle Density
- •4.4 Flow Characteristics
- •5. Various Targeted Drug Delivery Systems
- •5.1 Application of Exosomes and EVs (Extracellular Vesicles)
- •5.4 Nanomedicines in Cardiovascular Therapy
- •5.5 PLGA-Based Nanoparticles
- •5.6 Liposomal Delivery Systems
- •5.7 Delivery of Biologicals
- •5.8 RNA-Based Delivery
- •5.9 Therapeutic Proteins and Peptides
- •6. Future Perspectives and Challenges
- •7. Conclusion
- •References
- •1. Introduction
- •2. Materials
- •2.1 Equipment
- •2.2 Drugs
- •3. Methods
- •3.1.1 Extrusion-Based 3D Bioprinting
- •3.1.2 Inkjet 3D Bioprinting
- •3.1.3 Light-Based Bioprinting
- •3.1.4 Laser-Assisted Printing
- •3.2 Multiple Drug Delivery
- •3.2.1 Multilayer Films with Capsule-Integrated Polypeptide/Polyelectrolyte
- •3.2.2 Multilayer Shells Using Polypeptides/Polyelectrolytes (PL or PG) and LbL Assembly
- •3.3.1 Physical Stimulation-Responsive Drug Delivery Systems
- •3.3.4 Light-Responsive Drug Delivery Systems (LRDDS)
- •3.4 Small Molecule Delivery System
- •3.4.1 Intraarticular Delivery System
- •3.5 Gene Delivery System
- •3.6 Stem Cell Technology
- •4. Conclusion
- •References
- •1. Introduction
- •2. Importance of Targeted Drug Delivery to the Reproductive System
- •3. Challenges in Drug Delivery to the Reproductive System
- •4. Advances in Drug Delivery Systems
- •4.2 Liposomes
- •4.3 Hydrogels and Biodegradable Polymers
- •4.4 Injectable and Implantable Devices
- •4.5 Micro- and Nano-Needles
- •4.6 Spermbots
- •5.1 Vaginal and Cervical Delivery
- •5.2 Uterine and Intrauterine Delivery
- •5.3 Penile and Testicular Delivery
- •6. Targeted and Precision Medicine Approaches
- •6.1 Hormone Replacement Therapy (HRT)
- •6.2 Gene Therapy and RNA-Based Approaches
- •6.3 Personalized Medicine in Reproductive Disorders
- •7. Therapeutic Applications and Innovations
- •7.1 Infertility and Assisted Reproductive Technologies (ART)
- •7.2 Treatment of Reproductive Cancers
- •7.4 Contraceptive Technologies
- •8. Safety and Regulatory Considerations
- •9. Future Directions and Emerging Trends
- •References
- •1. Introduction
- •2. Liposomes
- •3. Preparation of Liposomes
- •3.1 Reagents
- •3.2 Hydration and Liposome Extrusion
- •3.4 Conjugation
- •3.8 PEGylation
- •3.8.1 Materials Required
- •3.8.2 Procedure
- •3.9 Liposomal Doxorubicin (LD)
- •3.10 Marqibo (Vincristine Sulfate)
- •3.11 DepoCyt (Cytarabine)
- •4. Poly(Lactic-co-Glycolic Acid, PLGA) Nanoparticles
- •4.2 Methods
- •4.2.1 Reagents
- •4.2.2 Procedure
- •5. Polycaprolactone (PCL)
- •5.2 pH Sensitivity and Stability
- •5.3 Methods
- •5.3.1 Materials
- •5.4 Drug Loading
- •6. Chitosan-Based Systems
- •6.1 Encapsulation of Nucleic Acids and Proteins
- •6.3 pH Sensitivity and Stability of Chitosan Nanoparticles
- •6.4 Methodology
- •6.4.1 Reagents
- •6.4.2 Procedure
- •7. Dendrimers
- •7.1 Antisense Oligonucleotides
- •7.2 Small-Interfering RNA (siRNA)
- •7.4.1 Divergent Method
- •7.4.2 Convergent Method
- •8. Challenges in Developing Orphan Drugs
- •References
- •1. Introduction
- •2. Vaccine Delivery Systems
- •3. Polymers
- •4. Non-biodegradable NPs
- •5. Calcium Phosphate NPs
- •6. Colloidally Stable Nanoparticles
- •7. Proteasomes
- •8. Liposomes
- •9. Virus-like Particles (VLPs) and Virosomes
- •10. Immune-Stimulating Complexes ISCOMs
- •11. Emulsion Delivery Systems
- •12. Exosome-Based Vaccine Delivery System
- •13. Immunotherapy Using Nano- and Microparticles
- •14. Properties and Role of Nanoparticles in Drug Delivery
- •15. Biomimicry
- •16. Micellar Systems
- •17. Hydrogels
- •18. Edible Vaccines
- •19. Plant-Derived Viruses
- •20. Melt-in Mouth Strips
- •21. Transdermal Delivery
- •22. Delivery of Nucleic Acids
- •23. mRNA Delivery
- •24. Delivery of Cytokines
- •25. DC Targeting
- •26. Drug Delivery Targeting T Cells
- •27. Conclusions
- •References
- •1. Introduction
- •2. Materials
- •2.1 Equipment
- •2.2 Reagents and Solutions
- •3. Methods
- •3.1 Adenovirus
- •3.3 Retroviral Vectors (RV)
- •3.4 Lentivirus (LV)
- •4. Conclusion
- •References
- •1. Introduction
- •2. Technologies Utilizing Cells in Treating Diseases
- •2.1 Somatic Cell Technologies
- •2.2 Immortalized Cell Lines
- •2.5 Genome Editing Technologies
- •2.6 Cell Plasticity Technologies
- •3. Different Kinds of Cells Are Utilized in the Process of Cell Treatment
- •4. The Practices of Regenerative Medicine and Cell Therapy
- •4.1 Veterinary Medicine Therapeutic Uses
- •5. Advancements and Challenges in Drug Delivery
- •6. Drug Delivery Systems and Applications
- •6.2 Drug Nanocarriers Based on Hyaluronic Acid
- •6.3 Hexagonal Boron Nitride Nanosheet Drug Delivery System
- •6.4 Polymer-Lipid Hybrid Nanoparticles
- •6.6 In Situ Gel Drug Delivery System

Biomaterials in Drug Delivery: Design and Applications 169
diseased tissues and cells [28]. In this approach, ligands that bind to
surface molecules or receptors overexpressed in diseased cells and
tissues are selected for and conjugated to delivery materials
38]. Materials designed for controlled release should ideally also
[
protect drugs from rapid clearance and/or degradation within
the body.
Developing such biomaterials for controlled release is challenging and requires a multidisciplinary approach, incorporating engineers, physical scientists, biologists, and clinicians [
Design parameters include:
1. The incorporation of adequate drug within the host material
for prolonged release profiles that are required to achieve therapeutic efficacy
2. Protection of therapeutics from breakdown in vivo while also
maintaining biological activity
3. Predictable release over the course of the therapeutic regimen,
ranging from days to years.
Additionally, the materials themselves and their degradation
products should be nontoxic and biocompatible within the body,
avoiding patient discomfort prior to and following administration.
The expense of a particular material-drug formulation, due to the
cost of material synthesis and/or fabrication, must also be taken
into account during the design phase.
39].
10 Biomaterials for Controlled Release of Small Molecules
Initial studies describing the incorporation of bioactive molecules
into solid polymeric materials for achieving a sustained release
profile were conducted in the 1950s and 1960s for agricultural
applications [
trolled drug release systems for medical applications were pioneered
in the 1960–70 s [40]. The first reported biomaterial for controlled
molecule release was silicon rubber when it was observed that
hydrophobic, lipophilic, small-molecule (molecular weight
<300 g/mol) dyes diffused through the wall of silicon tubing
Given that medical-grade silicones are biocompatible and
41].
[
used for implantation for a range of medical applications, this
discovery led to the use of silicone rubbers for the controlled release
of drugs, including atropine, histamine, anesthetics, steroids, and
antimalarial and antischistosomal agents [42–44]. Notably,
implanted silicone rubber released drugs over the course of days
to months in dogs, rats, and sheep [
biomaterials induce controlled release of biologically active agents
in the body. These reports suggested that modulating pharmacological actions by controlling drug release from biomaterials could
35]. Soon thereafter, polymeric biomaterials as con-
42, 43, 45], demonstrating that

170 Naveen Kumar
be achieved, ultimately leading to the formation of ALZA in 1968
for the commercialization of some technologies [
further led to the development of an early drug delivery system
approved by the US Food and Drug Administration (FDA) in
1990, Norplant (now Jadelle), a contraceptive composed of silicone
rubber tubes implanted in the forearm that releases levonorgestrel
for up to 5 years with pregnancy rates of less than 1% per year
46]. Research within the field of biomaterials, drug delivery, and
[
controlled release accelerated during this period, giving rise to the
development of osmotic pumps for oral drug delivery in dogs [
dr
ug-loaded
meric and albumin microsphere-based encapsulation for sustained
release of drugs in rats, rabbits, and humans [49], as well as new
mathematical models to quantify drug release from biomaterials
[
50]. Hydrogels, 3D networks of polymer chains cross-linked to
form matrices with high water content, are now widely used in drug
delivery and tissue engineering due to their tunable physical, chemical, and biological properties [
demonstrate application
[
52]. In drug delivery, PEG has been utilized as a “stealth material”
that enhances the circulation half-life of drugs, reduces drug accumulation in clearance organs such as the liver, while also enhancing
the sur face biocompatability of materials [
sive overviews on hydrogels [
biomaterials for drug delivery and controlled release, are detailed
elsewhere [
hydrogels for ophthalmic drug delivery [
51]. Broadly speaking, hydrogels
in areas such as regenerative medicine
53]. More comprehen-
51, 54], as well as the history of
55].
41]. This work
47]
48], poly-
,
11 Bioresponsive Polymers: From Design to Implementation
An ideal therapeutic drug is expected to treat or cure a disease
without resulting in any side effects [
not been achieved so far. Many chemotherapeutics are found to
destroy both cancerous and healthy cells within the vicinity of the
target site [
drug directly to diseased cell populations. Polymers have been
found to permit the creation of “responsive” materials within the
host environment and can be formulated with drugs to control
release [
the molecular weight of polymers that can be controlled via monomer stoichiometry using controlled polymerization strategies like
atom transfer radical polymerization, reversible addition fragmentation chain transfer, nitroxide-mediated polymerization, and living
ring-opening metathesis polymerization. A bioresponsive material
is one that can respond to a specific “trigger” inside or outside of
the body. Because the body have unique pathological parameters
such as pH gradients, temperatures, enzymes, and small molecules,
the creation of materials that will respond to physiological
57]. An efficient chemotherapeutics would administer
58].
This polymer attribute is due to tuning propensity of
56]. However, this goal has

Biomaterials in Drug Delivery: Design and Applications 171
alterations in both space and time is required. Triggers include
chemical, biological, and physical stimuli. The chemical and
biological ones are intrinsic to the body, while the physical stimuli
are extrinsic to the body and can thus be used to quicken sole drug
delivery [
59].
11.1 RedoxSensitive Polymers
The human body consists of compartmentalized regions of differing redox potential. The reducing agent glutathione, for example,
is found at a concentration two to three orders of magnitude larger
within cells than outside of them. Bio-responsive materials are
initiated by redox potential difference in tissue environment and
its surrounding [
60]. Contrastingly, oxidizing agents that include
hydrogen peroxide are associated with tissue inflammation and
injury [61]. These differences in redox potential between a local
tissue/cellular environment and their surroundings present an
opportunity to create bioresponsive materials that are triggered
via oxidation or reduction within the body. In order to respond
to reduction triggers within the body, materials derived from disulfides are commonly employed [
60]. Disulfide-based materials are
frequently used as bioresponsive materials because disulfide bridges
can be reduced under mild conditions to afford dithiol analogues.
Within the cell, this process is most commonly mediated by glutathione, a tripeptide consisting of glycine, cysteine, and glutamic
acid. To date, dilsufide-based materials have been exploited for
applications ranging from protein delivery to gene expression,
among others [
62]. Importantly, disulfide/dithiol interchange is a
reversible chemical reaction which can be important for biomedical
applications. Interestingly, many sulfur-based materials have also
been developed to respond to oxidation triggers. Sulfur is a unique
atom in that it can exist in multiple oxidation states; accordingly,
sulfur-based materials including block copolymers have been
prepared for applications in areas such as gene delivery [
63]. Alter-
natively, materials derived from boronic acids/esters have also been
developed to respond to oxidation triggers [64].
In the presence of
oxidizing agents such as hydrogen peroxide, boronic acids/esters
can be converted into the corresponding alcohol. This chemical
process has been exploited for triggered protein release applications
using dextran as a base material, among others. There are materials
that can respond to both oxidation and reduction triggers, which
are incorporated into responsive polymers. One of the most common functional group motifs used for these dual activation materials are diselenides. Diselenides are similar in chemical structure to
disulfides and have also been incorporated into responsive polymers. Unlike disulfide materials, however, diselenides are sensitive
to both oxidation and reduction, which allows for alternative triggers within nanobiotechnology application [
65].

172 Naveen Kumar
11.2 pH-Responsive Polymers
The constituents of the human body such as tissues, fluids, and
organelles have varied pH values. Areas like stomach, vagina, and
lysosomes display acidic pH (<7.0), ocular surfaces (7.1), blood
(7.4), and bile (7.8) [
58]. Owing to these varied pH of systems and
organs in the body, improvement in the efficacy and precision of
therapeutic molecules will necessitate the design of polymeric drug
delivery systems that are pH specific. pH-responsive materials have
been useful in nucleic acid delivery, doxorubicin delivery, and taste
masking [
66]. The target treatment of tumors has been enhanced
using the pH-responsive materials. Such known target delivery
includes multifunctional acid-sensitive nanocomposites for anticancer drugs and acid-responsive poly ethylene glycol derivatives for
the controlled release of therapeutics in tumor target treatment
67]. As a general strategy to create pH-sensitive materials, it is
[
common to incorporate chemical functional groups that can be
protonated or deprotonated within polymeric matrices [68]. For
example, amine-containing polymers including those derived from
dimethylaminoethylmethacrylate are protonated under acidic conditions to yield reversibly cationic materials [
69]. By contrast,
carboxylate-containing polymers including poly(acrylic acid) are
deprotonated under basic conditions to afford anionic matrices.
Given that the charge of these polymers can be readily altered,
materials derived from these polymers can respond to pH changes
by swelling, degrading, shrinking, or dissociating. In doing so,
these materials can release their drug cargo in a pH-responsive
fashion within target tissues and organs in the body. To date,
pH-responsive materials have been used for a variety of applications
including nucleic acid delivery, doxorubicin delivery, and taste
masking, among others [
One specific area
66].
where pH-responsive materials have improved
therapeutic targeting is in the treatment of tumors. The tumor
microenvironment often exists at a lower pH (≈5.7) than its surroundings (≈6.8–7) due to localized acidosis [
70]. Given this
difference, multifunctional acid-sensitive nano-composites have
been explored for the controlled release of anticancer drugs
71]. Importantly, these materials were also functionalized with
[
folic acid, improving the targeting of these materials to overexpressed folic acid receptors on the cancer cell surface. Moreover, a
similar concept has been employed for materials incorporating acidsensitive diaminoketal cross links, and drug-laden versions of these
materials have demonstrated increased cellular uptake relative to
that observed for the free drug alone [
Finally, acid-responsive
72].
poly(ethylene glycol) derivatives have also been designed for the
controlled release of therapeutics using hydra-zine chemistry, and
tumor targeting with pH-responsive materials continues to be an
area of interest to the drug delivery community [
67].

Biomaterials in Drug Delivery: Design and Applications 173
11.3 Hydrolysis and Enzymatically Responsive Polymers
Hydrolysis-sensitive polymeric materials have also been designed,
synthesized, and implemented in vivo for drug delivery purposes.
Hydrolysis-prone materials by definition can be degraded by water,
a trigger that is ubiquitous in the human body. This degradative
process most commonly occurs through the nucleophilic addition
of water into an electrophilic functional group on a polymer. Commonly employed electrophilic functional groups on polymers
include esters and anhydrides, each of which have been employed
in multiple types of responsive materials [
73]. The Gliadel wafer is
one example product on the market that demonstrates the power of
hydrolysis-sensitive materials for drug delivery [
74]. Consisting of
the chemotherapeutic Carmustine impregnated within a polyanhydride material, the Gliadel wafer can be implanted into brain
tumors for the controlled release of chemotherapeutic to malignant
gliomas. Of note, the Gliadel wafer improves the 6-month survival
rate of patients diagnosed with glioblastoma multiforme
[
74]. Enzyme-responsive polymers have also been developed for
drug delivery. The concentrations of specific enzymes including
matrix metalloproteins, hyaluronidases, phospholipases, and
prostate-specific antigen can deviate from normal values in association with specific disease pathologies. Accordingly, many enzymeresponsive polymer systems have been developed, with applications
ranging from tumor imaging, to doxorubicin delivery, and minimizing inflammation in the colon, among others [
75].
11.4 TemperatureResponsive Polymers
11.5 MagneticResponsive Polymers
Another drug delivery vehicle is the temperature-sensitive polymer
that can operate at both human body temperature of 37 °C and at
ambient temperature such as 25 °C. To take advantage of this
difference, polymer systems that flow at room temperature but
become gel at body temperature have been developed—these materials are predominantly used for local delivery applications, capitalizing on the sol-gel transition of specific polymers [
76]. These
polymers include poloxamers, poly(N-alkyl acryl amides), poly
(N-vinyl caprolactams), cellulose, xyloglucan, and chitosan. These
thermo-responsive polymers can be modified via varying the ratio
of monomers, endgroup modifications, and post-polymerization
modifications to make them suitable for varying applications [
77].
Magnetic-responsive polymers are therapeutic drug-loaded polymers that work under the influence of magnetic resonance imaging
(MRI) to deliver its drug to the target. Magnetic pulsing techniques serve as yet another “trigger” for controlling the release of
drugs from responsive materials. This concept has been extended to
designing systems to release compounds to specific organs by pairing therapeutic treatment with drug-loaded polymers and magnetic
Select examples include
resonance imaging (MRI) techniques [
78].
(i) the systematic release of dopamine from alginates impregnated
with magnetic beads; (ii) targeted plasmid delivery to the lung

174 Naveen Kumar
using chitosan nanopar ticles; and (iii) insulin delivery, among
others [
pH-responsive materials
79]. Magnetic “triggers” have also been combined with
to afford dual responsive drug delivery
systems. The combination of two or more environmental responses
in a single material can be highly advantageous. For example, if one
were to include magnetic particles within a polymer that was
designed to degrade in highly acidic conditions, then one could
use MRI imaging to pinpoint the exact location that the drug was
delivered upon dispersion of the pa
stomach. An
added benefit to incorporating magnetic material
rticles within, for instance, the
within a delivery nanoparticle is that it can double as a retrieval
method. When designing any material or drug that will be
implanted in a patient, it is important to establish a contingency
plan. In case of an undesired immune response or rejection, for
both molecular chemicals and living tissue alike, being able to
remove the injected or implanted material is crucial. Having a
magnetic system allows for the material to be more easily removed,
especially in
a self-circulating system (e.g., the blood stream or
intraperitoneal spaces). Accounting for these factors into a drug–
polymer design broadens the project scope and challenges interdisciplinary research in order to achieve a unified engineered material.
It is also important to note that some magnetic responsive systems
have been approved by the FDA [
80].
11.6 LightResponsive Polymers
Light-responsive polymers are used as external drug delivery systems that use noninvasive and painless techniques as drugs are
delivered by light UV- and visible-wavelength irradiation stimulation. The ease by which drugs can be delivered by light stimulation
has been a major motivation for the design of systems to respond to
this style of noninvasive trigger. Light stimulation drug delivery has
been desirable due to the controlled spatial and temporal release of
a therapeutic payload with both UV- and visible-wavelength irradiation. This technique provides a remote-activated approach that
does not require direct patient contact [
Current challenges
81].
associated with light-activated controlled drug release include the
distance of the polymer vehicle from the light source, the density of
native host tissue that the light has to penetrate to reach the
delivery vehicle, and the potential for drug molecule degradation
upon exposure to light. One underlying mechanism of lightinduced drug delivery involves a shift in molecular conformation
including cis-trans isomerization and ring-opening reactions
82].
This technology has been used to target melanoma cells
[
through the release of drugs from a light-responsive azobenzenemodified amphiphilic block copolymer [
83]. Upon irradiation, the
conformation of the azobenzene switches, thereby altering the selfassembling structures and releasing the payload.

Biomaterials in Drug Delivery: Design and Applications 175
11.7 Swelling and Contracting Polymers
There are polymers that can swell or shrink in response to external
stimuli. Changes in porosity can result from leaching of ionic crosslinking molecules, which in turn alters the diffusion pathways for
sensing molecules [
changes in porosity occasioned as ionic cross-linking molecules are
leached, resulting in alteration of the diffusion pathways for sensing
molecules. Alginate, a commonly employed polymer that is isolated
from seaweed, is relatively biocompatible. Tuning the spatial and
temporal release of encapsulated materials is rather challenging, but
has been successfully applied for a variety of applications using
alginates. A recent example includes the sustained delivery of vascular endothelial growth factor (VEGF) and subsequent analogues
from alginate to a localized region within the body. Using an
injectable alginate design, the controlled release of VEGF was
utilized to promote lymphatic vessel development through
improved vascularization [
have the potential to create future generations of materials for the
paralleled delivery of therapeutics, regional specific sensing, and
secondary responses for noninvasive detection.
12 Transdermal Drug Delivery Systems
Conventional (“free”) drugs exhibit limitations that can be
improved through their incorporation in drug delivery system.
The chemical nature of the drug molecule can be responsible for
its poor solubility resulting in drug precipitation when in aqueous
media. The use of drug carriers such as lipid micelles or liposomes,
among others, can surpass this major limitation improving drug
solubility (Lukyanov and Torchilin 2004). Although many efforts
have been developed to promote topic/transderm al drug delivery,
the systemic route is still the major strategy used for drug administration. A drug administered by this method reaches the systemic
circulation (blood) inducing, therefore, a systemic action. On the
other hand, drugs given by the topical route are mainly applied on
skin or mucous membrane, being able to promote both of systemic
and localized action.
84]. This phenomenon can have stemmed from
85]. In general, these hybrid designs
12.1 Barriers to Transdermal Delivery
Skin is a highly efficient barrier that limits molecular transport both
from and into the body, preventing molecular permeation. This
natural barrier avoids the penetration of foreign molecules such as
the flux of toxins, while minimizing the water loss. Skin is composed by multi-layers. On skin’s outer surface, there is a non-living
layer of keratin-filled cells surrounded by a lipid-rich extracellular
matrix named stratum corneum (SC), an extremely thin
biomembrane
.

176 Naveen Kumar
12.2 Development of Transdermal Drug Delivery Patches
12.3 Hydrogels Versus Non-hydrogel Polymeric Patches
12.4 Patches Based on Biopolymers
12.5 Patches Based on Synthetic Polymers
Transdermal delivery systems can be divided into three generations
of development. As stated in European Pharmacopoeia, transdermal patches are designed to provide the controlled and sustained
release of active substances to the systemic circulation after crossing
the skin barrier, mostly by diffusion and resulting in a prolonged
and adequately constant absorption rate. The majority of the actual
patches are within the first generation.
Matrix- and reservoir-type patches can be divided into hydrogel and
non-hydrogel polymeric patches. Hydrogel is a water-swollen and
cross-linked polymeric network produced by the simple reaction of
one or more monomers. Hydrogels have received high attention in
the past 50 years, due to their exceptional promise in wide range of
biomedical applications [
48].
Biopolymers, mostly natural ones, have been receiving careful
attention due to their biocompatibility, being editable, low toxicity,
and susceptibility to degradation by human enzymes or by hydrolysis, as well as renewable and sustainable giving rise to a broader
use especially in fields such as biomedical sciences, pharmaceuticals,
cosmetics, and other related fields.
The commercially available patches are based on synthetic materials
that display greater mechanical resistance and non-degradation
over time. These materials can be widely used in different patches
design such as drug-in adhesive (DIA) and microneedles patches.
The DIA patches consist in the incorporation of a drug and possible
additives in pressure sensitive adhesives (PSA) that is limited by a
backing film and release liner.
12.6 Drug Particles/ Carriers
12.7 Commercial Patches
Drug release is greatly conditioned by the physical and chemical
properties of the drug. Carrier systems ranging from micro- to
nanoscale are able to transport a wide variety of therapeutic molecules with enhanced solubility and targeting. Such systems can be
incorporated during patch production in order improve drug
release, enhancing its permeation through skin layers. Nanovesicles, for instance, allow the delivery of the entrapped molecules into
or across the skin.
New and desired products are commercialized to fulfil the unmet
medical needs at a reasonable cost. Approximately two dozen
molecules have been approved for transdermal administration by
the regulatory authorities to reach the market. Most of these drugs
are for prescription use only, with many being available as generic
patches following patent expirations.
The development
of new and effective DDS has been greatly
improving treatments efficacy, solving the common problems associated with the use of conventional “free” drugs. Their

13 Smart Biomaterials
Biomaterials in Drug Delivery: Design and Applications 177
administration through transdermal route has been attracting considerable attention due to its numerous advantages, such as less
frequent, painless, and flexible dosing, as it also generates less
amount of dangerous waste. These factors have been stimulating
the research and development of transdermal DDS to be effective.
Another class of innovative biomaterials that are pushing forward
pioneering medical approaches are the ones taking the name of
smart biomaterials, due to their ability to respond to changes in
physiological parameters or external stimuli [
materials are able to modify their physicochemical and mechanical
properties as a reaction to biological, chemical, and physical signals,
i.e., temperature, humidity, pH, redox potential, enzymatic activity,
light, and mechanical stimuli. Among these biomaterials, smart
hydrogels are frequently exploited for tissue engineering and drug
delivery applications [
be cross-linked also using reversible methods, such as physical
cross-linking, thermally induced entanglement, and self-assembly,
which may allow for controlling drug release and biodegradation
92, 93]. Biodegradable hydrogels are often obtained by means
rate [
of cleavable cross-linkers, which can be dissolved through hydrolysis, proteolysis, or disentanglement following a specific stimulus
94]. Other biomaterials such as shape memory (SM) alloys and
[
polymers own the unique ability to recover to their original geometry and structure after exposure to an external stimulus, such as
temperature, magnetic field, electric field, light, or relative
humidity [
smart materials that have attracted attention as actuators for the
development of artificial muscles. These polymers present some
similarities with the functional response of biological muscles in
terms of resilience, resistance, and large actuation stretching or
bending [
have also been adopted in bioinspired robotics to simulate specific
actuation and sensing properties, such as, by way of example, the
tactile features of human skin or the ability of some animals to sense
subtle vibrations in the environment [
applications of biomaterials to regenerative medicine is represented
by their use as systems to release extracellular vesicles (EVs) and
soluble factors [
tent progenitor cells that are able to self-renew, differentiate into
multiple lineages, and also accomplish trophic effects [100]. These
effects are due to the secretion of EVs, which transport a variety of
intracellular molecules (lipids, proteins, RNA, and DNA) suitable
for guiding the regenerative process during tissue repair. These
95].
Electroactive polymers
96, 97]. Nanomaterials and nanostructured biomaterials
89–91]. I
99]. Mesenchymal stem cells (MSCs) are pluripo-
ndeed, the hydrogel structure can
(EAPs) are another emerging class of
98].
86–88]. These bio-
One of the most recent

178 Naveen Kumar
molecules control different cellular functions (e.g., migration, proliferation, differentiation, and synthesis of extracellular matrix components); furthermore, they suppress the local immune system,
inhibit fibrosis and apoptosis, enhance angiogenesis, and stimulate
mitosis and differentiation of reparative cells.
14 Conclusion and Future Perspective
Significant progress has been made in improving the biomaterialbased drug delivery systems. However, only a limited number of
affinity-based delivery systems have been developed for the delivery
of neurotrophic factors. Therefore, there is a need for the development of broad-spectrum reservoir-based delivery systems, including microspheres, electrospun nanofibers, hydrogels, and
combinations of these systems. Drug delivery systems transport
biologically active agents, such as growth factors and genetic material, into the desired location to promote beneficial effects for the
treatment of diseases and disorders, osmotic pumps for the delivery
of neurotrophic factors to target site, affinity-based delivery systems
(ABDS) in which drug loading and controlled release are achieved
through the interactions of therapeutic drug and the delivery system, and reservoir-based delivery systems, where a polymer structure encapsulates the drug while its release is controlled via the
material properties.
Skin p
rovides a l
application and absorption of a patch-like device to its surface,
constituting a noninvasive procedure that will promote a continuous intervention. Transdermal DDS have been exploited as a successful controlled drug release platform that have received
regulatory approval for a series of products. Transdermal DDS
can be applied when a drug has a significant first-pass effect in the
liver, being prematurely metabolized. Such type of drug delivery
also allows for less frequent dosing or steady delivery profiles and
may be easily applied with a painless application. Moreover, transdermal DDS promote a fast absorption of drug in superficial tissues,
improving the wound healing process. The choice among these
patches can mostly depend on the drug properties (e.g., molecular
weight and physicochemical characteristics), as well as the required
amount and release rate to accomplish an effective treatment. Drug
carriers (either at nano- or micro-scale) can be incorporated in
patches in order to improve drug pharmacological properties,
prompting a more efficient treatment of such devices.
Significant progress
of hydrogels used for drug delivery and expanding the range of
drugs and kinetics which can be achieved using a hydrogel-based
delivery vehicle. However, several challenges remain to improve the
clinical applicability of hydrogels for drug delivery. One set of major
arge and readily accessible surface area for
has been made in improving the properties
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