Design Of Controlled Release Drug Delivery Systems

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ISBN: 9780071417594 | 0071417591
Cover: Hardcover
Copyright: 11/24/2005

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The goal of every drug delivery system is to deliver the precise amount of a drug at a pre-programmed rate to the desired location in order to achieve the drug level necessary for the treatment. An essential guide for biomedical engineers and pharmaceutical designers, this resource combines physicochemical principles with physiological processes to facilitate the design of systems that will deliver medication at the time and place it is most needed.

Contributors

Preface

Application of Pharmacokinetics and Pharmacodynamics in the Design of Controlled Delivery Systems

(40)

James A. Uchizono

Introduction

(1)

Pharmacokinetics and Pharmacodynamics

(1)

LADME Scheme and Meaning of Pharmacokinetic Parameters

(3)

Maximum concentration, time to maximum concentration, and first-order absorption rate constant Cp,max', tmax, ka

(1)

Bioavailability F

(1)

Volume of distribution Vd

(1)

Clearance Cl

(1)

First-order elimination rate constant K and half-life t1/2

(1)

Pharmacokinetics and Classes of Models

(4)

Linear versus nonlinear pharmacokinetics

(1)

Time- and state-varying pharmacokinetics and pharmacodynamics

(2)

Pharmacokinetics: Input, Disposition, and Convolution

(5)

Input

(2)

Disposition

(2)

Convolution of input and disposition

(1)

Compartmental Pharmacokinetic Modeling

(13)

Single-dose input systems

(9)

Multiple-dosing input systems and steady-state kinetics

(4)

Applications of Pharmacokinetics in the Design of Controlled Release Delivery Systems

(6)

Design challenges for controlled release delivery systems

(3)

Limitations of using pharmacokinetics only to design controlled release delivery systems

(1)

Examples of pharmacokinetic/pharmacodynamic considerations in controlled release delivery systems design

(2)

Conclusions

(6)

References

(6)

Physiological and Biochemical Barriers to Drug Delivery

(34)

Amit Kokate

Venugopal P. Marasanapalle

Bhaskara R. Jasti

Xiaoling Li

Introduction

(1)

Barriers to Peroral Controlled Release Drug Delivery

(10)

Anatomical organization of the gastrointestinal tract

(6)

Physiological and biochemical characteristics of the gastrointestinal tract

(4)

Barriers to peroral drug delivery

(1)

Barriers to Nonperoral Controlled Release Drug Delivery

(14)

Skin

(3)

Eye

(3)

Oral cavity

(3)

Nose

(2)

Lung

(2)

Vaginal mucosa

(1)

Physiological and Biochemical Barriers to Controlled Release Drug Delivery

(9)

Acknowledgments

(1)

References

(7)

Prodrugs as Drug Delivery Systems

(32)

Anant Shanbhag

Noymi Yam

Bhaskara Jasti

Introduction

(1)

Rationale for Prodrug Design

(1)

Principles of Prodrug Design

(10)

Ester-based prodrugs

(3)

Amide-based prodrugs

(2)

Salt-based prodrugs

(2)

Additional prodrug types

(2)

Prodrugs for Prolonged Therapeutic Action

(1)

Prodrug Design for Various Routes of Administration

(6)

Prodrugs for nasal delivery

(1)

Prodrugs for ocular delivery

(1)

Prodrugs for parenteral delivery

(1)

Prodrugs for transdermal delivery

(1)

Prodrugs for oral delivery

(1)

Prodrugs for buccal delivery

(1)

Recent Advances in Prodrugs as Drug Delivery Systems

(4)

Antibody-directed enzyme prodrug therapy (ADEPT)

(1)

Gene-directed enzyme prodrug therapy (GDEPT) and viral-directed enzyme prodrug therapy (VDEPT)

(1)

Macromolecule-directed enzyme prodrug therapy (MDEPT)

(2)

Lectin-directed enzyme-activated prodrug therapy (LEAPT)

(1)

Dendrimers

(1)

Conclusions and Future Prospects

(8)

References

100

(7)

Diffusion-Controlled Drug Delivery Systems

107

(32)

Puchun Liu

Tzuchi ``Rob'' Ju

Yihong Qiu

Diffusion Theory

108

(7)

Basic equations of diffusion

108

(2)

Diffusional release from a preloaded matrix

110

(2)

Diffusion across a barrier membrane

112

(3)

Oral Diffusion-Controlled Systems

115

(8)

Matrix systems

115

(5)

Reservoir systems

120

(1)

Current challenges and future trends

121

(2)

Transdermal Diffusion-Controlled Systems

123

(8)

Drug-in-adhesive systems

125

(1)

Semisolid matrix systems

126

(1)

Reservoir systems

127

(1)

Current challenges and future trends

127

(4)

Other Diffusion-Controlled Systems

131

(8)

Intrauterine devices and intravaginal rings

131

(1)

Intraocular inserts

132

(1)

Subcutaneous implants

132

(1)

References

133

(6)

Dissolution Controlled Drug Delivery Systems

139

(34)

Zeren Wang

Rama A. Shmeis

Introduction

140

(1)

Theoretical Considerations for Dissolution Controlled Release Matrix and Coated Systems

140

(9)

Dissolution of solid particles

140

(2)

Dissolution of coated systems

142

(4)

Dissolution of matrix systems

146

(3)

Parameters for Design of Dissolution Controlled Release Matrix and Coated Systems

149

(6)

Parameters affecting dissolution of solid particles

149

(1)

Parameters affecting dissolution of coated systems

150

(2)

Parameters affecting dissolution of matrix systems

152

(3)

Applications and Examples of Dissolution Controlled Release Matrix and Coated Systems/Technologies

155

(12)

Delivery systems based on dissolution controlled release solid particles

155

(1)

Delivery systems based on dissolution controlled release coated technologies

156

(9)

Delivery systems based on dissolution controlled release matrix technologies

165

(2)

Future Potential for Dissolution Controlled Release Drug Delivery Systems

167

(6)

Dissolution controlled release coated systems

167

(1)

Dissolution controlled release matrix systems

168

(1)

References

169

(4)

Gastric Retentive Dosage Forms

173

(30)

Amir H. Shojaei

Bret Berner

Introduction

173

(2)

Physiological Rationale for Gastric Retentive Delivery System Design: GI Motility

175

(2)

Fasting contractile activity

176

(1)

Fed mode

176

(1)

Design of Retentive Delivery System Based on Size

177

(8)

Tablet size and the fed mode

177

(5)

Retention of expanding systems in the fasted state

182

(3)

Design of Retentive Delivery System Based on Density Difference

185

(4)

Density greater than gastric fluid (submerged)

186

(1)

Density lower than gastric fluid (floating)

186

(3)

Design of Retentive Delivery System Based on Adhesion: Mucoadhesive Systems

189

(5)

Mucus and epithelial layers

189

(2)

Polymers as bioadhesives

191

(1)

Factors affecting bioadhesion

192

(1)

Applications of bioadhesion

193

(1)

Mechanism or Kinetics of Drug Release

194

(1)

Future Potential for Gastric Retentive Delivery Systems

195

(8)

References

195

(8)

Osmotic Controlled Drug Delivery Systems

203

(28)

Sastry Srikond

Phanidhar Kotamraj

Brian Barclay

Introduction

204

(1)

Rationale for Design of Osmotic Controlled Drug Delivery Systems

205

(1)

Mechanism of Osmotic Controlled Release

206

(7)

Quantitative aspects of osmosis

206

(1)

Release kinetics in elementary osmotic pumps

207

(2)

Release kinetics in OROS® Push-Pull™ systems

209

(2)

Key parameters that influence the design of osmotic controlled drug delivery systems

211

(2)

Components of Osmotic Systems

213

(2)

Osmotic components

213

(1)

Semipermeable membrane--forming polymers for osmotic pumps

213

(1)

Emulsifying agents

214

(1)

Flux-regulating agents

214

(1)

Plasticizers

215

(1)

Barrier layer formers

215

(1)

Osmotic Delivery Systems

215

(12)

Evolution of osmotic delivery systems

215

(5)

Classification of osmotic pumps

220

(2)

Oral osmotic delivery systems

222

(1)

Recent advances in osmotic drug delivery of liquid active components

223

(3)

Marketed products

226

(1)

Conclusions and Future Potential

227

(4)

References

227

(4)

Device Controlled Delivery of Powders

231

(40)

Rudi Mueller-Walz

Introduction

231

(4)

Design Rationale for Dry-Powder Delivery

235

(7)

Deposition mechanisms

235

(4)

Deposition efficiency

239

(1)

Physiological and pathological aspects of inhalation drug delivery

240

(2)

Design of Dry-Powder Inhalation Devices

242

(13)

Passive DPI devices

243

(9)

Active DPI devices

252

(3)

Powder Formation

255

(6)

Devices for Powder Injection

261

(3)

Future Potential of Device Controlled Delivery of Powders

264

(7)

References

265

(6)

Biodegradable Polymeric Delivery Systems

271

(34)

Harish Ravivarapu

Ravichandran Mahalingam

Bhaskara R. Jasti

Introduction

272

(1)

Rationale for the Use of Biodegradable Systems

272

(1)

Biodegradable Polymers Used in Drug Delivery

273

(7)

Polyesters and polyester derivatives

274

(3)

Polylactones

277

(1)

Poly(amino acids)

278

(1)

Polyphosphazenes

278

(1)

Poly(orthoesters)

279

(1)

Polyanhydrides

279

(1)

Design Principles [Diffusion versus Erosion (Surface versus Bulk)]

280

(13)

Diffusion Controlled Systems

280

(6)

Erosion and degradation controlled systems

286

(7)

Delivery Devices

293

(6)

Microparticles

293

(3)

Nanoparticles

296

(1)

Implants

297

(2)

Future Potential

299

(6)

References

299

(6)

Carrier-and Vector-Mediated Delivery Systems for Biological Macromolecules

305

(34)

Jae Hyung Park

Jin-Seok Kim

Ick Chan Kwon

Introduction

305

(1)

Carrier-Mediated Delivery Systems

306

(12)

Barriers to oral delivery of macromolecular drugs

307

(5)

Design of macromolecular drugs through chemical modification

312

(3)

Design of colloidal drug carriers

315

(3)

Design of Vector-Mediated Delivery Systems for Genetic Materials

318

(12)

Barriers to vector-mediated gene delivery

318

(1)

Viral vector

319

(2)

Nonviral vector

321

(9)

Future Directions

330

(9)

References

331

(8)

Physical Targeting Approaches to Drug Delivery

339

(36)

Xin Guo

Introduction

340

(1)

Rationale for the Design of a Drug Delivery System

340

(3)

Challenges of drug delivery systems for intravenous administration

341

(1)

Delivery across biomembranes

341

(1)

Biostability and bioresponsiveness

342

(1)

Design of a Physically Targeted Delivery System: Modulation of Physicochemical Parameters

343

(3)

Molecular weight and size

343

(1)

Surface hydrophobicity

344

(1)

Charge

345

(1)

Membrane destabilization

345

(1)

Physicochemical functionalities for triggered release

346

(1)

Current Drug Delivery Systems

346

(23)

Polymers

346

(10)

Lipidic colloids

356

(10)

Nanospheres

366

(3)

Future Outlook for Physically Targeted Drug Delivery Systems

369

(6)

References

369

(6)

Ligand-Based Targeting Approaches to Drug Delivery

375

(30)

Andrea Wamsley

Introduction

376

(1)

Rationale for Targeting Drug Delivery Systems

377

(1)

Concepts of active and passive targeting

377

(1)

Organ/cellular/subcellular targeting

377

(1)

Design of Ligand-Based Targeting Drug Delivery Systems

378

(14)

Ligand-receptor-based interaction

379

(12)

Targeted enzyme prodrug therapy

391

(1)

Factors Affecting Design of Ligand-Based Targeting Drug Delivery Systems

392

(6)

Kinetics of active targeting systems

392

(1)

Internalization of ligand-based targeting drug delivery systems

393

(3)

Drug release from delivery systems

396

(1)

Immunogenicity

397

(1)

Current Status and Future of Actively Targeted Drug Delivery Systems

398

(7)

References

398

(7)

Programmable Drug Delivery Systems

405

(24)

Shiladitya Bhattacharya

Appala Raju Sagi

Manjusha Gutta

Rajasekhar Chiruvella

Ramesh R. Boinpally

Introduction

406

(1)

Rationale for Programmed Drug Delivery Systems

406

(2)

Classification, Design, and Functioning of Programmed Drug Delivery Systems Based on Design Principles

408

(16)

Open-looped (pulsatile) systems

409

(11)

Closed-looped (feedback-controlled) systems

420

(4)

Current Systems and Future Potential

424

(2)

Conclusions

426

(3)

References

426

(3)

Index

429

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Design Of Controlled Release Drug Delivery Systems

Summary

Author Biography

Table of Contents

Supplemental Materials