Оглавление
Tamilvanan Shunmugaperumal. Oil-in-Water Nanosized Emulsions for Drug Delivery and Targeting
Table of Contents
List of Tables
List of Illustrations
Guide
Pages
OIL‐IN‐WATER NANOSIZED EMULSIONS FOR DRUG DELIVERY AND TARGETING
LIST OF CONTRIBUTORS
FOREWORD
PREFACE
CHAPTER 1 INTRODUCTION: AN OVERVIEW OF NANOSIZED EMULSIONS
EXPANSION OF ABBREVIATIONS
1.1. INTRODUCTION
1.1.1. Nanotechnology: Definition
1.1.1.1. Poorly Water‐Soluble Grease Ball and Brick Dust Molecules
1.1.2. Nanosized Emulsions
1.1.2.1. Nanosized Emulsions: Prime Candidates for Nanoparticle Engineering
1.1.2.2. Ostwald Ripening‐Adapted Droplet Destabilization Process for the Greater Stability of Nanosized Emulsions
1.1.2.3. Classification of Oil‐in‐Water Nanosized Emulsions
1.2. CONCLUSION
REFERENCES
CHAPTER 2 FORMULATION DEVELOPMENT OF OIL‐IN‐WATER NANOSIZED EMULSIONS
EXPANSION OF ABBREVIATIONS
2.1. INTRODUCTION
2.2. FDA‐APPROVED OILS, EMULSIFIERS, AND AUXILIARY OR MISCELLANEOUS EXCIPIENTS
2.2.1. Issues Related to Oil Selection to Make the O/W Nanosized Emulsions for Medical Application
2.2.2. Issues Related to Emulsifier Selection to Stabilize the O/W Nanosized Emulsions for Medical Application
2.2.3. Importance of Charge‐Stabilized Nanosized Emulsions
2.2.4. Importance of Neutral‐Charged (Sterically Stabilized) Nanosized Emulsions
2.2.5. Advantages of Nanosized Emulsions Stabilized by Mixed or Multicomponent Emulsifier Molecules
2.2.6. “Stealth” Property of Nanosized Emulsions: In Vitro Demonstrations
2.2.7. Advantages of Stabilizers in Nanosized Emulsions
2.2.8. Miscellaneous Additives
2.3. CURRENT AND NEAR FUTURE DIRECTION. 2.3.1. Colloidal Particle‐Stabilized Emulsions
2.4. LIPOPHILIC API INCORPORATION PATTERN INTO NANOSIZED EMULSIONS
2.4.1. Extemporaneous API Addition
2.4.2. De Novo Emulsion Preparation
2.4.3. Interfacial Incorporation Approach
2.4.4. Incorporation of Antibodies, DNA Protein, Oligonucleotide, or Heat Labile Molecules
2.5. QbD APPROACH TO OPTIMIZE EMULSION
2.5.1. Case Study for Optimizing Systematically a Formula to Make O/W Nanosized Emulsions
2.5.1.1. Initial Quality Risk Assessment Studies
2.5.1.2. Factor Screening Study
2.5.1.3. Factor Screening Studies by Taguchi Design
2.5.1.4. Formulation Optimization by QbD: Experimental Design
2.5.1.5. Systematic Optimization Using Face‐Centered CCD
2.5.1.6. Response Surface Plot Analysis
2.5.1.7. Optimization of Responses for Formulation of CsA‐Loaded Nanosized Emulsion
2.6. CONCLUSION
REFERENCES
Note
CHAPTER 3 CHARACTERIZATION AND SAFETY ASSESSMENT OF OIL‐IN‐WATER NANOSIZED EMULSIONS
EXPANSION OF ABBREVATIONS
3.1. INTRODUCTION
3.2. PHYSICAL AND VISUAL EVALUATIONS. 3.2.1. Refractive Index
3.2.2. Viscosity
3.2.3. pH
3.2.4. Creaming
3.2.5. Stability Testing
3.2.5.1. Stress Testing
3.2.6. Particle Size and Interfacial Charge
3.2.6.1. Emulsion Sample Preparation to Determine the MPS Value Using DLS/PCS
3.2.6.2. Emulsion Particle Size Measurement Using Laser Diffraction Technique
3.2.6.3. Measuring of ZP in Nanosized Emulsions
3.2.6.3.1. Understanding the EDL and slipping plane
3.2.6.3.2. Factors influencing ZP. 3.2.6.3.2.1. PH
3.2.6.3.2.2. IONIC STRENGTH
3.2.6.3.2.3. PARTICLE CONCENTRATION
3.2.6.3.3. ZP and colloid stability
3.2.6.3.4. ZP and surface charge of nanoformulations
3.2.6.3.5. Physical constraints in measuring the ZP
3.2.6.3.5.1. REFERENCE MATERIALS
3.2.6.3.5.2. REUSING SAMPLES AFTER MEASURING ZP
3.2.6.3.5.3. USING BUFFERS WITH METALLIC IONS
3.2.6.3.5.4. MEASURING ZP IN CELL CULTURE MEDIUM
3.2.6.4. Current Thought About DLS/PCL and ZP Determination in Nanoformulations
3.2.7. Microscopic Evaluations of Nanosized Emulsions. 3.2.7.1. Transmission Electron Microscopy (TEM)
3.2.7.1.1. Particle size reduction between emulsion preparation steps assessed by TEM
3.2.7.2. Atomic Force Microscopy (AFM)
3.2.7.2.1. Working principle of AFM
3.2.8. Emulsion Stability Evaluation/Prediction Using TurbiScan®
3.2.8.1. Instability Detection Using Turbiscan®
3.2.9. Spreading Coefficient
3.3. CHEMICAL AND BIOLOGICAL EVALUATIONS. 3.3.1. Confirmation of API Encapsulation into Emulsion
3.3.2. In Vitro API Release from Nanosized Emulsions
3.3.2.1. Ultrafiltration Technique as a Model to Study In Vitro API Release from Nanosized Emulsions
3.3.2.2. Membrane‐Free Model to Study the In Vitro API Release from Nanosized Emulsions
3.3.3. Techniques Used to Study the In Vitro API Leakage Before Release in the Targeted Site
3.3.4. Transcorneal Permeation Study
3.3.5. Ex Vivo Diffusion Studies Using Animal Tissues
3.3.6. Techniques Used to Study the In Vitro/In Vivo Integrity of the Droplets Before and After It Arrives on the Targeted Site
3.3.7. In Vitro Mono‐Layer Cell‐Culture/Transfection Efficiency Studies to Substantiate API Targeting Concept
3.3.7.1. Effects of Four Inhibitors on the Cellular Uptake of Lipid‐Based Emulsions
3.3.7.2. Effects of Temperature on the Cellular Uptake of Nanosized Emulsions
3.4. SAFETY AND EFFICACY ASSESSMENTS
3.4.1. Non‐ or Pre‐clinical Safety Assessments for Ophthalmic Emulsions
3.4.1.1. Draize Rabbit Eye Test
3.4.1.2. Schirmer Testing
3.4.1.3. Tear Break‐Up‐Time
3.4.1.3.1. Case study of nanosized emulsions with respect to Schirmer and TBUT tests
3.4.1.4. In Vitro Cytotoxicity Assay
3.4.1.4.1. Case study
3.4.1.5. Hen's Egg Test‐Chorioallantoic Membrane (HET‐CAM) Test Method
3.4.2. Non‐ or Pre‐clinical Safety Assessments for Parenteral Emulsions. 3.4.2.1. In Vitro and In Vivo Myotoxicity Studies
3.4.2.1.1. In vitro myotoxicity study
3.4.2.1.2. In vivo myotoxicity study
3.4.2.2. In Vitro Hemolysis Test
3.5. CONCLUSION
REFERENCES
Note
CHAPTER 4 MANUFACTURING AND POSITIONING (GENERATIONS) OF OIL‐IN‐WATER NANOSIZED EMULSIONS
EXPANSION OF ABBREVIATIONS
4.1. INTRODUCTION
4.2. GENERATIONS OF O/W NANOSIZED EMULSIONS
4.2.1. First‐Generation Nanosized Emulsions
4.2.2. Second‐Generation Nanosized Emulsions
4.2.2.1. Second‐Generation Nanosized Emulsions Versus Opsonization
4.2.2.2. Second‐Generation Nanosized Emulsions and Long Circulation Concept
4.2.2.3. Feasible Approaches for Making Long‐Circulating Second‐Generation Nanosized Emulsions
4.2.2.4. Long‐Circulating Second‐Generation Nanosized Emulsions Conjugated with Antibodies
4.2.2.5. RES‐Related Disease Management by Second‐Generation Nanosized Emulsions
4.2.3. Third‐Generation Nanosized Emulsions
4.2.3.1. Third‐Generation Nanosized Emulsions to Deliver Genetic Materials (Genes)
4.2.3.2. Third‐Generation Nanosized Emulsions and Their Distinctive/Typical Feature
4.2.4. Fourth‐Generation Nanosized Emulsions
4.2.4.1. Imaging
4.2.4.2. Inculcation of Theragnostic Concept Using Multifunctional O/W Nanosized Emulsions
4.2.4.3. IGDD or Theragnostic Concept in Breast Cancer Treatment
4.2.4.4. IGDD or Theragnostic Concept in AS
4.3. PREPARATION METHODS FOR API‐FREE/LOADED O/W NANOSIZED EMULSIONS
4.4. CONCLUSION
REFERENCES
Note
CHAPTER 5 BIOFATE OF NANOSIZED EMULSIONS
EXPANSION OF ABBREVIATIONS
5.1. INTRODUCTION
5.2. BIOFATE OF O/W NANOSIZED EMULSIONS
5.2.1. Issues Relevant to Ocular Nanosized Emulsions
5.2.1.1. Consequences of Nanosized Emulsions Following Ocular Topical Instillation
5.2.1.2. Consequences of Nanosized Emulsions Following Intraocular Injection
5.2.2. Issues Relevant to Parenteral Nanosized Emulsions
5.2.2.1. First‐Generation Nanosized Emulsion Metabolism
5.2.2.1.1. Interaction between nanosized emulsions and plasma apos
5.2.2.1.2. Apo E on nanosized emulsion metabolism
5.2.2.1.3. Apo E versus apo Cs, and LPL on nanosized emulsions metabolism
5.2.2.1.4. Apo E and apo Cs versus apo As
5.2.2.1.5. Apo E isoforms’ interaction with nanosized emulsions in vitro study
5.2.2.1.6. Other mechanism on nanosized emulsion metabolism
5.2.2.2. Newer Generation Nanosized Emulsion Metabolism
5.2.2.2.1. In vitro mimicking of opsonization process with surface (charged)‐modified nanosized emulsions
5.2.2.2.2. Influence of nanosized emulsions on monocyte‐macrophages and neutrophils functions
5.2.2.2.3. Immunomodulatory mechanism of nanosized emulsions
5.3. CLINICAL ISSUES OF FIRST‐GENERATION NANOSIZED EMULSIONS
5.4. CONCLUSION
REFERENCES
Note
CHAPTER 6 MEDICAL OR THERAPEUTICAL APPLICATIONS OF OIL‐IN‐WATER NANOSIZED EMULSIONS
EXPANSION OF ABBREVIATIONS
6.1. INTRODUCTION
6.2. MEDICAL OR THERAPEUTICAL APPLICATIONS OF O/W NANOSIZED EMULSIONS. 6.2.1. Medical or Therapeutical Applications of Parenteral O/W Nanosized Emulsions
6.2.2. Medical or Therapeutical Applications of Non‐parenteral O/W Nanosized Emulsions. 6.2.2.1. Intranasal Emulsions
6.2.2.1.1. Lipid/oil component
6.2.2.1.2. Emulsifiers
6.2.2.2. Ophthalmic Emulsions
6.2.2.2.1. Topical ophthalmic emulsions
6.2.2.2.2. Non‐topical ophthalmic emulsions
6.2.2.2.3. Future perspective of topical ophthalmic emulsions
6.2.2.2.3.1. TARGETED TOPICAL OPHTHALMIC EMULSIONS
6.2.2.3. Topical Dermal Emulsions
6.3. CONCLUSION
REFERENCES
Note
CHAPTER 7 OVERVIEW OF TOCOL‐BASED EMULSIONS, OXYGEN‐CARRYING EMULSIONS, EMULSIONS WITH DOUBLE OR TRIPLE CARGOS AND EMULSION‐LIKE DISPERSIONS
CHAPTER 7.1 TOCOL‐BASED NANOSIZED EMULSIONS
EXPANSION OF ABBREVIATIONS
7.1.1. INTRODUCTION
7.1.2. FORMULATION DEVELOPMENT USING TOCOL
7.1.3. NON‐ AND PRE‐CLINICAL SAFETY STUDIES. 7.1.3.1. Hemolytic Study
7.1.4. THERAPEUTIC APPLICATIONS. 7.1.4.1. Treatment to Critical or Intensive Care Unit Patients
7.1.4.2. As a Solvent, API Delivery Vehicle, and Therapeutic Agent
7.1.5. CONCLUSION
REFERENCES
Note
CHAPTER 7.2 OXYGEN‐CARRYING EMULSIONS
EXPANSION OF ABBREVIATIONS
7.2.1. INTRODUCTION
7.2.2. RATIONALE FOR SELECTING PERFLUOROCARBON FOR IN VIVO OXYGEN TRANSPORT
7.2.2.1. PFC Suitability Assessment for In Vivo Oxygen Transfer
7.2.3. FORMULATION OF STABLE INJECTABLE PERFLUOROCARBON EMULSIONS
7.2.4. MULTIFUNCTIONAL PERFLUOROCARBON‐BASED EMULSIONS
7.2.5. GENERATIONS AND HURDLES OF PERFLUOROCARBON‐BASED NANOSIZED EMULSIONS AS OXYGEN CARRIERS
7.2.6. PROPOSED SOLUTIONS TO OVERCOME THE HURDLES OF PERFLUOROCARBON‐BASED NANOSIZED EMULSIONS USED AS OXYGEN CARRIERS
7.2.7. CONCLUSION
REFERENCES
Note
CHAPTER 7.3 NANOSIZED EMULSIONS FOR MULTIPLE MEDICAMENT LOADINGS, IMAGING, AND THERANOSTIC PURPOSES
EXPANSION OF ABBREVIATIONS
7.3.1. INTRODUCTION
7.3.2. BRIEF REVIEW OF RESEARCH REPORTS ON NANOSIZED EMULSIONS FOR IMAGING AND THERANOSTIC PURPOSE
7.3.3. VARIOUS TOPOLOGIES OBSERVED IN DISPERSED OIL DROPLETS OF THE EMULSIONS
7.3.3.1. Janus Architecture
7.3.3.2. Cerberus Architecture
7.3.4. POSSIBLE THERAPEUTIC UTILITY OF JANUS EMULSION. 7.3.4.1. Status of Recent Research and Development in Janus Structure
7.3.4.2. Janus Emulsion for Atherosclerosis Theragnosis
7.3.5. CONCLUSION
REFERENCES
Note
CHAPTER 7.4 EMULSION‐LIKE DISPERSIONS
EXPANSION OF ABBREVIATIONS
7.4.1. INTRODUCTION
7.4.2. FORMULATION OF EMULSION‐LIKE DISPERSIONS
7.4.2.1. Projection of β‐Cyclodextrin as Emulsifier
7.4.2.2. Projection of Eutectic Mixture as Oil Phase
7.4.2.2.1. Case Study Using Oil‐Less Emulsions
7.4.2.3. Projection of β‐Cyclodextrin and Eutectic Mixture as Emulsifier and Oil Phase
7.4.2.4. Projection of β‐Cyclodextrin and Other Hydrophilic Macromolecules as Components to Make Multicomponent Multiphase System. 7.4.2.4.1. Water‐in‐Water Emulsion
7.4.2.4.2. Types of Phase Separation in Water‐in‐Water Emulsions
7.4.2.5. Formulation Realities of ATPS
7.4.2.5.1. ATPS Types
7.4.2.5.2. Stability Issues with ATPS
7.4.3. CONCLUSION
REFERENCES
Note
CHAPTER 8 SELECTED CASE STUDIES
CHAPTER 8.1 CASE STUDY 1 CATIONIC NANOSIZED EMULSIONS: NARRATION OF COMMERCIAL SUCCESS
EXPANSION OF ABBREVIATIONS
8.1.1. INTRODUCTION
8.1.2. SELECTION OF SUITABLE CATION‐CONFERRING AGENT
8.1.3. SELECTION OF SUITABLE PRESERVATIVE IF NEEDED
8.1.4. CLINICAL SAFETY ASSESSMENT
8.1.4.1. Clinical Evaluation of Cationorm
8.1.4.2. Clinical Evaluation of Cyclokat
8.1.5. CONCLUSION
REFERENCES
Note
CHAPTER 8.2 CASE STUDY 2 FISH OIL‐BASED NANOSIZED EMULSIONS
EXPANSION OF ABBREVIATIONS
8.2.1. INTRODUCTION
8.2.2. IMPORTANCE OF FISH OIL OR FISH OIL SUPPLEMENTS IN EVERYDAY HUMAN LIFE
8.2.3. OVERVIEW ON ENVIRONMENT‐FRIENDLY GREEN‐EXTRACTION METHODS OF FISH OIL FROM WHOLE FISH OR FISHERIES WASTE
8.2.4. RATIONALE FOR DEVELOPING NANOSIZED EMULSIONS BASED ON FISH OIL
8.2.5. FISH OIL‐BASED EMULSION PRODUCTS: COMPARATIVE LITERATURE SURVEY
8.2.6. COMPLICATIONS OF FISH OIL AND FISH OIL‐BASED PRODUCTS
8.2.7. REGULATORY ASPECTS RELATED TO THE SAFETY OF FISH OIL/FISH OIL‐BASED PRODUCTS
8.2.7.1. Biological Hazards Associated with Raw Materials of Fish
8.2.7.2. Chemical Hazards Associated with Raw Materials of Fish
8.2.8. THERAPEUTICAL APPLICATION OF FISH OIL OR FISH OIL‐BASED NANOSIZED EMULSIONS
8.2.8.1. Alzheimer's Disease
8.2.8.2. Cardiovascular Disease
8.2.8.3. Central Nervous System
8.2.8.4. Inflammatory Disease
8.2.8.5. Kidney/Renal Disease
8.2.8.6. Malignancy
8.2.8.7. Obesity
8.2.8.8. Sepsis
8.2.8.9. Type 2 Diabetes Mellitus
8.2.9. CONCLUSION
REFERENCES
Note
Index
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