Enhancement in Drug Delivery

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ISBN: 9780849332036 | 0849332036
Cover: Hardcover
Copyright: 11/27/2006

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Enhancement in Drug Delivery offers an accessible compendium covering a wide spectrum of methods to enhance drug delivery and absorption by various routes of administration. Drawing from a number of disciplines, it gives students and practitioners in pharmaceutics, medicine, and health-related disciplines a much-needed guide to current practices. It also provides a starting place for those working on delivery systems for new drugs or seeking to improve current systems by drawing on means applied in other routes. Organized by routes of delivery, the book covers oral, rectal, buccal and sublingual, dermal and transdermal, ocular, vaginal and uterine, nasal and brain administrations.

Part I Promoted Gastrointestinal Drug Absorption

(132)

Gastrointestinal Anatomy, Physiology and Permeation Pathways

(34)

Abraham Rubinstein

Introduction

(1)

Brief Longitudinal Overview

(3)

The Oral Cavity

(1)

The Stomach and Secretions Relevant to Drug Absorption

(1)

The Small Intestine and Secretions Relevant to Drug Absorption

(1)

The Colon

(1)

The Rectum

(1)

Relevant Longitudinal Aspects to Oral Delivery of Drugs and Drug Delivery Systems

(6)

Gastrointestinal Motility

(1)

Gastric Emptying of Liquids and Solids in the Fed State

(1)

Nonnutritional Factors Affecting Emptying of the Fed Stomach

(1)

Emptying of Liquids and Solids from the Fasted Stomach

(1)

Intestinal Transit of Liquids and Solids in Fed and Fasted States

(1)

Intestinal Spreading of Solid Dosage Forms

(1)

Motility of the Colon

(1)

Transit of Liquids and Solids in the Colon

(1)

Intestinal Microflora

(1)

Luminal pH

(1)

Intestinal Mucus and Turnover Rates

(1)

Relevant Transverse Aspects to Drug Absorption

(2)

Boundary Layers

(1)

Diffusional Path in Mucus Layers and Possible Drug Interactions

(1)

Transverse pH Gradient

(1)

Splanchnic Blood Flow and Drug Absorption

(1)

Mucosal Membranes and Drug Absorption

(11)

Oral Cavity Mucosa

(2)

Gastric Mucosa

(1)

Intestinal Mucosa

(1)

Transcellular Drug Absorption---Simple and Facilitated Diffusion

(3)

Transcellular Drug Absorption---Nondiffusional Processes

(1)

Carrier-Mediated Approaches to Drug Absorption

(2)

Receptor-Mediated Endocytosis and Drug Absorption

(1)

Paracellular Drug Absorption

(3)

Intestinal Efflux Processing of Absorbed Drugs and Brush-Border Metabolism

(1)

Physiological Insight on the Use of Absorption Enhancers in the GI Tract

(10)

References

(9)

Enhancers for Enteral Delivery of Macromolecules with Emphasis on Surfactants

(20)

Biana Godin

Elka Touitou

Various Approaches for Gastrointestinal-Promoted Absorption of Macromolecules

(4)

Surfactants for Enhanced Gastrointestinal Absorption of Macromolecules

(8)

Early Studies

(1)

Gastrointestinal Absorption Enhancement by Nonionic Surfactants

(4)

Anionic Surfactants as Promoters of Gastrointestinal Absorption

(3)

Toxicity of Surfactants for Gastrointestinal Mucosa

(1)

Concluding Remarks

(8)

References

(6)

Improvement of Oral Drug Absorption by Chitosan and its Derivatives

(12)

Hiraku Onishi

Yoshiharu Machida

Introduction

(1)

Enhancement of Absorption of Small Molecules

(2)

Poly(vinyl alcohol)-Gel Spheres with Chitosan

(1)

Chitosan-Coated Ethylcellulose Microparticles

(1)

Enhancement of Peptide Absorption by Chitosan

(2)

Chitosan-Coated Liposomes Containing Peptide Drugs

(1)

Chitosan-Coated Nanoparticles Containing Peptide Drugs

(1)

Enhancement of Intestinal Absorption by Chitosan Derivatives

(3)

N-trimethylchitosan as an Enhancer of Intestinal Absorption

(1)

Thiolated Chitosan as a Strongly Mucoadhesive Polymer and Its Applications

(1)

Perspectives for the Use of Chitosan and Its Derivatives for Oral Administration

(4)

References

(3)

Targeted GI Delivery

(16)

David R. Friend

Introduction

(1)

Background

(1)

Stomach

(5)

Floating Dosage Forms

(2)

Swellable and Expandable Dosage Forms

(1)

Mucoadhesive Dosage Forms

(2)

Small Intestine

(2)

Biospecific Mucoadhesive Approaches

(1)

Receptor-Mediated Targeting and Absorption

(1)

Polymer-Based Targeting

(1)

Electrically Based Drug Delivery

(1)

Colonic Delivery

(3)

Receptor-Mediated Colon Targeting

(3)

Conclusions

(5)

References

(5)

Inhibition of Enzymes and Secretory Transport

(26)

Martin Werle

Andreas Bernkop-Schnurch

Introduction

(1)

Enzyme Inhibition

(12)

Nuclease Inhibition

(1)

Protease Inhibition

(1)

Inhibitors That Are Not Based on Amino Acids

(3)

Amino Acids and Modified Amino Acids

(1)

Peptides and Modified Peptides

(1)

Polypeptide Protease Inhibitors

(1)

Complexing Agents

(1)

Mucoadhesive Polymers Exhibiting Enzyme Inhibitory Activity

(2)

Esterase Inhibition

(1)

Methods to Evaluate the Protective Effect of Inhibitory Agents and Dosage Forms toward Luminal Enzymatic Attack

(1)

In Vitro Test Models for Luminally Secreted Enzymes

(2)

In Vitro Test Models for Brush Border Membrane-Bound Enzymes

(1)

In Situ Test Models

(1)

In Vivo Test Models

(1)

Secretory Transport

(2)

Inhibition of Efflux Systems

(1)

Efflux Pump Inhibition to Improve Oral Bioavailability

(1)

Improving Oral Bioavailability by Using First-Generation Inhibitors

(1)

Improving Oral Bioavailability by Using Second- and Third-Generation Inhibitors

(1)

Improving Oral Bioavailability by Using Polymeric Agents

(1)

Methods to Evaluate Efflux Pump Inhibition

100

(1)

In Vitro Evaluation

100

(1)

In Vivo Evaluation

100

(1)

Conclusion and Future Trends

100

(11)

References

101

(10)

Enhanced Gastrointestinal Absorption of Lipophilic Drugs

111

(22)

Arik Dahan

Amnon Hoffman

Introduction

111

(1)

Barriers Facing Lipophilic Drug Absorption

112

(2)

Preenterocyte Barriers

112

(1)

Solubility

112

(1)

Limited Absorption Site

112

(1)

Unstirred Water Layer

113

(1)

Enterocyte Barriers

113

(1)

Cytochrome P450 3A4 and P-glycoprotein

113

(1)

Postenterocyte barriers

113

(1)

Techniques for Enhancing Lipophilic Drug Absorption

114

(13)

Preenterocyte Associated Solutions

114

(1)

Lipid-Based Formulation Approach

114

(6)

Prodrug Approach

120

(3)

Enterocyte-Associated Solutions

123

(1)

Lymphatic Transport

123

(3)

Cytochrome P450 3A4 and P-glycoprotein Inhibitors

126

(1)

Conclusions

127

(6)

References

127

(6)

Part II Promoted Rectal Absorption

133

(40)

Permeation Pathways in Rectal Absorption

135

(12)

Yoshiteru Watanabe

General Considerations

136

(3)

Anatomy and Physiology of the Rectum and Its Role in Drug Absorption

136

(2)

Effect of Dosage Form and Formulation on Drug Dissemination from Rectum to Colon

138

(1)

Rectal Permeability in Diseases

139

(2)

Inflammatory Diseases

139

(1)

Other Pathophysiological Conditions

140

(1)

Enhancement of Rectal Absorption

141

(3)

Rate-Controlled Rectal Drug Delivery

141

(1)

Absorption-Enhancing Agents

141

(3)

Conclusions

144

(3)

References

144

(3)

Cyclodextrins and Other Enhancers in Rectal Delivery

147

(26)

Hidetoshi Arima

Kaneto Uekama

Introduction

147

(1)

Cyclodextrins as Multifunctional Enhancers for Rectal Drug Absorption

148

(9)

Improvement of Drug Release from Suppositories and Drug Absorption by Cyclodextrins

150

(2)

Stabilization of Drugs by Cyclodextrins in Rectal Delivery

152

(1)

Cyclodextrins as Absorption Enhancers

152

(1)

Cyclodextrins as Absorption Coenhancers

153

(1)

Long-Acting Absorption-Enhancing Effects of Cyclodextrins

154

(1)

Enhancing Mechanism of Cyclodextrins for Rectal Absorption

154

(3)

Inhibitory Effects of Cyclodextrins of Drug Irritancy in Rectal Delivery

157

(1)

Other Absorption Enhancers

157

(5)

Surfactants

157

(2)

Bile Acids

159

(1)

Enamine Derivatives

160

(1)

Salicylate and Its Derivatives

160

(1)

Nonsteroidal Anti-Inflammatory Drugs

160

(1)

Caprate and Fatty Acids

161

(1)

Mixed Micelles

161

(1)

Ethylenediamine Tetraacetic Acid and Egtazic Acid

161

(1)

Other Absorption Enhancers

162

(1)

Enhancing Mechanism of Absorption Enhancers

162

(2)

Effect of Absorption Enhancers on Paracellular Routes

162

(1)

Effect of Absorption Enhancers on Transcellular Routes

163

(1)

Peptidase Inhibitors

164

(1)

Combinatorial Effects of Absorption Enhancers and Other Materials

164

(1)

Prolonged Rectal Drug Delivery

165

(1)

Conclusion

165

(8)

References

166

(7)

Part III Enhancement of Buccal and Sublingual Absorption

173

(42)

Basic Biopharmaceutics of Buccal and Sublingual Absorptions

175

(28)

Priya Batheja

Rashmi Thakur

Bozena Michniak

Introduction

176

(1)

Physiology of the Oral Mucosa

176

(3)

Structure

176

(1)

Physiological Importance of Mucins and Saliva

177

(1)

Tissue Permeability

178

(1)

Barriers to Permeation

179

(1)

Advantages and Disadvantages of Buccal and Sublingual Routes of Administration

179

(1)

Physicochemical Properties and Routes of Permeation

180

(1)

Biopharmaceutics of Buccal and Sublingual Absorption

180

(5)

Principles of Drug Absorption

180

(2)

Factors Affecting Drug Absorption

182

(1)

Degree of Ionization, pH, and Lipid Solubility

182

(1)

Molecular Size and Weight

183

(1)

Permeability Coefficient

184

(1)

Formulation Factors

184

(1)

Permeation Enhancement

184

(1)

In Vitro and In Vivo Study Methods

185

(2)

Animal Models for Studies

185

(1)

In Vivo Methods

185

(1)

In Vitro Methods

186

(1)

Cell and Tissue Culture Systems

187

(1)

Dosage Forms

187

(9)

Chewing Gums

188

(1)

Lozenges

189

(1)

Buccal and Sublingual Tablets

189

(1)

Mucoadhesive Systems

189

(1)

Films and Patches

190

(1)

Tablets

191

(2)

Hydrogels

193

(1)

Other Dosage Forms

194

(1)

Sprays

194

(1)

Carrier-Associated Suspensions

195

(1)

Liposomes

195

(1)

Nanoparticles

195

(1)

Microparticulate Delivery Systems

196

(1)

Iontophoresis

196

(1)

Buccal and Sublingual Delivery of Peptides and Proteins

196

(1)

Conclusion

197

(6)

References

198

(5)

Chemical Enhancers in Buccal and Sublingual Absorptions

203

(12)

John D. Smart

Introduction

203

(1)

Buccal and Sublingual Drug Delivery

204

(1)

Mechanisms of Absorption Enhancement

204

(1)

Types of Permeation Enhancers

205

(5)

Bile Salts

205

(2)

Fatty Acids and Their Salts and Esters

207

(1)

Azone

208

(1)

Other Surfactants

208

(1)

Complexing Agents

209

(1)

Cosolvents

209

(1)

Others

210

(1)

Enzyme Inhibition

210

(1)

Toxicity

210

(1)

Conclusions

211

(4)

References

211

(4)

Part IV Transdermal Enhanced Delivery

215

(138)

The Lipid Organization in Stratum Corneum and Model Systems Based on Ceramides

217

(16)

Miranda W. de Jager

Maja Ponec

Joke A. Bouwstra

Introduction

217

(1)

Keratinocyte Terminal Differentiation

218

(2)

The Viable Epidermis

218

(1)

The Stratum Corneum

219

(1)

Stratum Corneum Barrier Lipids

220

(3)

Penetration Pathway through the Stratum Corneum

220

(1)

Composition of the Intercellular Lipids in the Stratum Corneum

221

(2)

Lipid Organization of Stratum Corneum Lipids

223

(5)

Lipid Organization in Stratum Corneum of Normal Skin

223

(1)

Altered Lipid Composition and Organization in Stratum Corneum of Diseased and Dry Skin

223

(1)

In Vitro Lipid Organization of Lipid Mixtures Prepared with Isolated Ceramides

224

(2)

In Vitro Lipid Organization of Lipid Mixtures Prepared with Synthetic Ceramides

226

(2)

Conclusion

228

(5)

References

228

(5)

Chemical Permeation Enhancement

233

(22)

Adrian C. Williams

Brian W. Barry

Introduction

233

(1)

Background

234

(1)

Major Classes of Chemical Penetration Enhancers

234

(14)

Water

235

(2)

Sulfoxides and Similar Chemicals

237

(1)

Azone

238

(1)

Pyrrolidones

239

(1)

Fatty Acids

240

(2)

Alcohols, Fatty Alcohols, and Glycols

242

(1)

Surfactants

243

(1)

Urea

244

(1)

Essential Oils, Terpenes, and Terpenoids

244

(2)

Phospholipids

246

(1)

Ceramide Analogs

247

(1)

Solvents at High Concentrations

247

(1)

Metabolic Interventions

247

(1)

Enhancer Combinations

247

(1)

General Comments on Penetration Enhancers

248

(7)

References

251

(4)

Vesicular Carriers for Enhanced Delivery through the Skin

255

(24)

Elka Touitou

Biana Godin

Introduction

255

(1)

Liposomes---Phospholipid Vesicles for Topical Administration of Drugs

255

(4)

Niosomes and Elastic Niosomes---Nonionic Surfactant Vesicles

259

(4)

Tranfersomes---Ultradeformable Liposomes

263

(1)

Ethosomes---Soft Phospholipid Vesicles for Enhanced Dermal and Transdermal Delivery

264

(9)

Concluding Remarks

273

(6)

References

273

(6)

Iontophoresis in Transdermal Delivery

279

(24)

Blaise Mudry

Richard H. Guy

M. Begona Delgado-Charro

Introduction

279

(2)

Overview

281

(2)

Pathways of Transport during Transdermal Iontophoresis

283

(1)

Theoretical Models of Iontophoretic Drug Transport

283

(8)

Nernst-Planck Models

284

(1)

Constant Field Approximation

285

(1)

Electroneutrality Approximation

286

(1)

Single Ion and Multiple Competing Coions

286

(1)

Expansion of the Nernst--Planck Model to Incorporate Electroosmosis

287

(1)

Electroosmosis

288

(1)

Constant Current Iontophoresis: Application of Faraday's Law

288

(1)

Binary Case

289

(1)

Ionic Mobility--Pore Model

290

(1)

Key Parameters in Transdermal Iontophoresis

291

(5)

The Drug

291

(1)

Current Intensity

292

(1)

Current Density

293

(1)

Drug Concentration

293

(2)

Ionic Strength

295

(1)

295

(1)

Skin Permselectivity

295

(1)

Conclusion

296

(7)

Acknowledgment

297

(1)

References

297

(6)

Electroporation as a Mode of Skin Penetration Enhancement

303

(14)

Michael C. Bonner

Brian W. Barry

Introduction

303

(1)

Iontophoresis

304

(1)

Route of Iontophoretic Penetration

304

(1)

Electroporation

304

(13)

Mechanism of Skin Disorganization by Electroporation

304

(1)

Safety Concerns with Electroporation

305

(1)

Applications of Electroporation

306

(1)

Pulsing Protocols for Electroporation

306

(2)

Electroporation and Iontophoresis Combination

308

(5)

Chemical Enhancement of Electroporation-Mediated Delivery

313

(1)

Future Prospects for Electroporation-Mediated Delivery

313

(1)

References

313

(4)

Ultrasound in Percutaneous Absorption

317

(14)

Joseph Kost

Lior Wolloch

Introduction

317

(1)

Physical Characteristics of Ultrasound

317

(1)

Biological Effects of Ultrasound

318

(2)

Thermal Effects

318

(1)

Cavitational Effects

319

(1)

Acoustic Streaming Effects

319

(1)

Effect on Skin

319

(1)

Transdermal Drug Delivery

320

(1)

Immunization

321

(2)

Gene Therapy

323

(1)

Transdermal Monitoring

323

(1)

Mechanism

324

(2)

Synergistic Effects

326

(1)

Safety

327

(4)

References

327

(4)

Combined Chemical and Electroporation Methods of Skin Penetration Enhancement

331

(6)

Michael C. Bonner

Brian W. Barry

Introduction

331

(1)

Chemical Penetration Enhancers of Electroporation-Mediated Delivery

331

(4)

Macromolecules

331

(1)

Cyclodextrins

332

(1)

Keratolytic Agents

332

(1)

Electrolytes

333

(1)

Lipids and Lipid Vesicles

333

(2)

Concluding Remarks and Future Prospects

335

(2)

References

336

(1)

Stratum Corneum Bypassed or Removed

337

(16)

James C. Birchall

Introduction

337

(1)

The Skin as a Barrier to Gene Delivery

338

(1)

Methods for Enhancing Drug Delivery to Skin

338

(10)

Microfabricated Microneedle Arrays

339

(1)

Silicon Microneedle Structures

340

(1)

Microneedle Structures Prepared from Other Materials

340

(2)

Hollow Microneedles

342

(1)

Microneedle Application Forces

343

(1)

Medical Applications for the Use of Microneedles

343

(3)

Other Methods for Disrupting Stratum Corneum

346

(1)

Tape Stripping

346

(1)

Laser Methods

346

(1)

Abrasive Methods

346

(1)

Puncturing Methods

347

(1)

Ballistic Methods

348

(1)

Conclusion

348

(5)

Acknowledgments

348

(1)

References

349

(4)

Part V Nasal Absorption Optimization

353

(40)

Physiological Factors Affecting Nasal Drug Delivery

355

(18)

Sian Tiong Lim

Ben Forbes

Marc B. Brown

Gary P. Martin

Introduction

356

(1)

Anatomy and Physiology of the Nose

356

(3)

Nasal Passages

356

(1)

Blood Supply

357

(1)

Respiratory Epithelium

357

(1)

Mucus and Cilia

358

(1)

Physiological Barriers to Nasal Drug Delivery

359

(4)

Delivery to the Nasal Cavity

359

(1)

Permeability

360

(2)

Mucociliary Clearance

362

(1)

Metabolism

362

(1)

Toxicity

363

(1)

Strategies for Overcoming Nasal Delivery Barriers

363

(3)

Delivery Devices

363

(1)

Molecular Modification

364

(1)

Formulation Approaches

364

(1)

Absorption Enhancers

365

(1)

Experimental Models of Physiological Barriers to Nasal Drug Absorption

366

(2)

Nasal Epithelial Models

366

(1)

Mucociliary Clearance Measurement

367

(1)

In Situ Perfused Nasal Cavity

368

(1)

In Vivo Models

368

(1)

Special Considerations in Nasal Delivery

368

(2)

Nose--Brain Delivery

368

(1)

Disease

369

(1)

Conclusion and Challenges for the Future

370

(3)

References

370

(3)

Nasal Delivery of Peptide Drugs

373

(20)

Dennis J. Pillion

John J. Arnold

Elias Meezan

Introduction

373

(1)

Nasal Drug Delivery

374

(2)

Anatomy and Physiology of the Nasal Cavity

374

(1)

Mucociliary Clearance

375

(1)

Enzymatic Degradation

376

(1)

Epithelial Cell Layer

376

(1)

Absorption Enhancers

376

(6)

Cyclodextrins

377

(1)

Chitosan

377

(2)

Bile Salts and Derivatives

379

(1)

Saponins

379

(1)

Soybean-Derived Steryl Glucosides

380

(1)

Phosphatidylcholines

380

(1)

Alkylglycosides and Sucrose Esters of Fatty Acids

380

(2)

Intranasal Insulin Delivery

382

(2)

Mechanisms of Action of Alkylglycosides

383

(1)

Reversibility of Alkylglycoside Effects on Insulin Absorption and Nasal Morphology

383

(1)

Intranasal Delivery of Other Peptides

384

(4)

Peptides Currently Used in Nasal Formulations

384

(2)

Peptides Currently Used as Injectables

386

(1)

Peptides Currently in Development

387

(1)

The Future of Nasal Peptide Drug Delivery

388

(5)

Acknowledgment

388

(1)

References

388

(5)

Part VI Drug Absorption from Vagina and Uterus

393

(78)

Vagina and Uterus as Drug-Absorbing Organs

395

(46)

R. Karl Malcolm

Stephen D. McCullagh

Ryan J. Morrow

A. David Woolfson

Introduction

396

(1)

Vaginal Anatomy and Physiology

396

(6)

Vaginal Anatomy

396

(1)

Vaginal Histology

397

(1)

Vaginal Fluid

397

(4)

Vaginal Flora

401

(1)

Uterine Anatomy and Physiology

402

(1)

Vaginal Drug Absorption

403

(3)

Uterine Drug Absorption

406

(1)

First Uterine Pass Effect

406

(1)

Vaginal and Uterine Drug Delivery Platforms

407

(8)

Vaginal Tablets

408

(1)

Vaginal Pessaries and Suppositories

408

(4)

Intravaginal Gels

412

(1)

Vaginal Creams

412

(1)

Intravaginal Rings

412

(1)

Intrauterine Devices

413

(2)

Clinical Applications

415

(15)

Vaginal Microbicides

415

(1)

Killing or Inactivating the Pathogens

416

(2)

Enhancers of Natural Vaginal Defense Mechanisms

418

(1)

Inhibitors of HIV Binding and Entry

418

(1)

Inhibitors of Viral Replication

419

(1)

Physical Barriers

419

(1)

Vaginal Vaccination

420

(3)

Uterovaginal Vaccine Vectors

423

(1)

Attenuated Virus

423

(1)

Nonlive Vaccination

423

(1)

Commensal Bacteria

424

(1)

DNA/Plasmid Vectors

424

(1)

Protein Subunit/Peptides or Virus-Like Particle Vectors

424

(1)

Adjuvants

424

(1)

Vaginal Contraception

425

(1)

Vaginal Contraceptive Film

425

(1)

Contraceptive Vaginal Rings

426

(1)

Progesterone Vaginal Ring

426

(1)

Nesterone Vaginal Ring

426

(1)

NuvaRing

426

(1)

Hormone Replacement Therapy

427

(2)

Urinary Incontinence

429

(1)

Pain Relief

429

(1)

Antifungals

430

(1)

Pelvic Endometriosis

430

(1)

Conclusions

430

(11)

References

431

(10)

Strategies to Improve Systemic and Local Availability of Drugs Administered via Vaginal Route

441

(30)

Giuseppina Sandri

Silvia Rossi

Franca Ferrari

Maria Cristina Bonferoni

Carla Caramella

Introduction

442

(1)

Anatomy and Physiology of the Vagina Relevant to Drug Delivery

443

(1)

Vaginal Mucosa as a Route for Drug Administration

444

(1)

Conventional Drug Delivery Systems

445

(3)

Solutions and Foams

446

(1)

Creams and Gels

446

(1)

Tablets

447

(1)

Suppositories (Pessaries)

447

(1)

Modified Release Formulations

448

(2)

Films

448

(1)

Rings

448

(2)

Comparison of the Functionality of Conventional and Modified Delivery Systems

450

(1)

Bioadhesive Delivery Systems

451

(8)

Bioadhesion: Definition and Mechanisms

451

(1)

Bioadhesion Theories

452

(1)

Bioadhesive Drug Delivery Systems

453

(1)

Bioadhesive Gels

453

(2)

Bioadhesive Tablets

455

(1)

Bioadhesive Pessaries

455

(1)

Bioadhesive Films

455

(1)

Microparticulate Systems

456

(1)

Bioadhesion Testing

456

(3)

Vaginal Delivery of Peptides and Proteins

459

(2)

Immunization via the Vaginal Route

461

(2)

Experimental Models to Study Vaginal Tolerability and Absorption

463

(2)

Final Remarks

465

(6)

References

465

(6)

Part VII Systemic Absorption through the Ocular Route

471

(102)

Eye Structure and Physiological Functions

473

(16)

Clive G. Wilson

Ekaterina M. Semenova

Patrick M. Hughes

Orest Olejnik

Introduction

473

(1)

External Features of the Eye

474

(7)

Eyelids

474

(1)

Eyelashes

474

(1)

Nasolacrimal Apparatus

475

(2)

The Conjunctivae

477

(1)

Cornea and Sclera

477

(2)

The Corneal Tearfilm

479

(2)

The Internal Eye Structures

481

(8)

Uveal Tract

481

(1)

The Lens

481

(1)

Internal Humors

481

(2)

The Choroid and Retinal Blood Supply

483

(2)

The Retina

485

(1)

Retinal Pigmented Epithelium

485

(1)

Posterior Pole: the Optic Nerve and Fovea

486

(1)

References

486

(3)

Drug Delivery Systems for Enhanced Ocular Absorption

489

(38)

Muhammad Abdulrazik

Francine Behar-Cohen

Simon Benita

Introduction

490

(1)

Indication for Pharmacological Intervention in Modern Ophthalmology

490

(1)

Drug Delivery Related Ocular Parameters

491

(6)

Ocular Surface Parameters

492

(1)

Capacity of the Lower Conjunctival Sac

492

(1)

Blinking

492

(1)

Tear Secretion

493

(1)

Tear Drainage

493

(1)

Barriers to Drug Permeation

494

(1)

Ocular Surface Barriers

494

(1)

Ocular Wall Barriers

494

(1)

Retinal Barriers

495

(1)

Core of the Eye Parameters

496

(1)

Drug Delivery to Back of the Eye

497

(5)

Routes of Drug Permeation to the Posterior Segment

497

(1)

Routes of Drug Permeation to the Neurosensory Retina

498

(1)

Obstacles for the Permeation of Topically Applied Therapeutics

499

(1)

Surface Epithelium

499

(1)

The Corneoscleral Collagenous Shell

500

(1)

Role of Ocular Tissue Vessels

500

(1)

The Vitreoretinal Compartment

500

(1)

Barriers of the Vitreoretinal Compartment

501

(1)

Enhancement in Topical Ocular Drug Delivery

502

(14)

Polymeric Drug Delivery Systems

502

(1)

Introduction

502

(1)

Nanoparticles

503

(2)

Nanocapsules

505

(1)

Micelles

506

(1)

Dendrimers

507

(1)

Solid Precorneal Inserts

508

(1)

Particle-Laden Solid Inserts

509

(1)

Liposomes

510

(1)

Emulsions

511

(3)

Iontophoresis

514

(2)

Electroporation

516

(1)

Conclusion

516

(11)

References

517

(10)

Ocular Penetration Enhancers

527

(22)

Indu Pal Kaur

Anupam Batra

Introduction

527

(4)

Precorneal Barriers

528

(2)

Corneal Barriers

530

(1)

Improving the Availability of Drugs Using Various Formulation Approaches

531

(1)

Use of Penetration Enhancers

532

(2)

Basic Mechanisms in Drug Transport through the Cornea

532

(1)

Mechanisms of Action of Penetration Enhancers

533

(1)

Classes of Penetration Enhancers (Table 25.1)

534

(7)

Calcium Chelators

534

(1)

Surfactants

535

(2)

Preservatives

537

(1)

Glycosides

537

(1)

Fatty Acids

538

(1)

Miscellaneous

538

(3)

Effect of Absorption Promoters on Conjunctival Membranes and Its Significance

541

(1)

Other Applications

541

(1)

Limitations to Practical Applicability

542

(1)

Conclusion

543

(6)

References

543

(6)

Iontophoresis for Ocular Drug Delivery

549

(24)

Esther Eljarrat-Binstock

Joseph Frucht-Pery

Abraham J. Domb

Introduction

549

(1)

Limitations in Ocular Drug Delivery

550

(2)

Iontophoresis Transport Mechanism

552

(1)

The Iontophoretic Device

553

(4)

In Vitro Models

557

(1)

Animal Studies

558

(7)

Transcorneal Iontophoresis

559

(2)

Transscleral Iontophoresis

561

(4)

Clinical Studies

565

(1)

Toxicity

565

(3)

Conclusions

568

(5)

References

568

(5)

Part VIII Drug Delivery to the Central Nervous System

573

(42)

Structure and Function of the Blood-Brain Barrier

575

(18)

David J. Begley

Introduction

575

(3)

Blood--Brain Barrier Tight Junctions

578

(3)

Transport Across the Blood--Brain Barrier

581

(7)

Passive Partitioning into Brain

581

(1)

Solute Carriers in the Blood--Brain Barrier

582

(1)

ATP-binding Cassette Transporters in the Blood--Brain Barrier

582

(4)

Blood--Brain Barrier Transport of Macromolecules

586

(2)

Cell Movement Across the Blood--Brain Barrier

588

(1)

Development and Ontology of the Blood--Brain Barrier

588

(5)

References

589

(4)

Strategies to Overcome the Blood-Brain Barrier

593

(22)

Elena V. Batrakova

Alexander V. Kabanov

Introduction

593

(1)

Enhancing Drug Influx in the Blood--Brain Barrier

594

(10)

Drug Modification

594

(1)

Lipophilic Drug Modification

594

(1)

Prodrugs and Chemical Delivery Systems

595

(1)

Vector-Mediated Drug Delivery

596

(2)

Drug Delivery through Adsorptive-Mediated Transcytosis

598

(1)

Drug Solubilization in Nano- or Microcontainers

598

(1)

Liposomes

599

(1)

Polymeric Micelles

600

(1)

Nanoparticles

601

(1)

Cell-Mediated Central Nervous System Drug Delivery

602

(1)

Disrupting of the Blood--Brain Barrier

603

(1)

Restricting Drug Efflux in the Blood--Brain Barrier

604

(3)

Role of Drug Efflux Transport Systems in the Blood--Brain Barrier

604

(1)

Pluronic Block Copolymers

605

(2)

Conclusion

607

(8)

Acknowledgment

608

(1)

References

608

(7)

Index

615

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Enhancement in Drug Delivery

Summary

Table of Contents

Supplemental Materials