Handbook of Pharmaceutical Controlled Release Technology

executive editor Donald L. Wise Cambridge Scientific, Inc. Cambridge, Massachusetts

associate editors Lisa Brannon-Peppas DebraJ. Trantolo Biogel Technology, Inc. Cambridge Scientific, Inc. Indianapolis, Indiana Cambridge, Massachusetts Alexander M. Klibanov Gary E. Wnek Robert S. Langer Virginia Commonwealth University Massachusetts Institute of Technology Richmond, Virginia Cambridge, Massachusetts Michael J. Yaszemski Antonios G. Mikos Mayo Clinic Rice University Rochester, Minnesota Houston, Texas Nicholas A. Peppas Purdue University West Lafayette, Indiana

MARCEL

MARCEL DEKKER, INC. NEW YORK • BASEL mD E K K E R Contents

Preface m

Part I: Polymers as Drug Delivery Carriers

1. Hydrophilic Cellulose Derivatives as Drug Delivery Carriers: 1 Influence of Substitution Type on the Properties of Compressed Matrix Tablets Carmen Ferrero Rodriguez, Nathalie Bruneau, Jerome Barra, Dowthee Alfonso, and Eric Doelker

2. Poly(Vinyl Alcohol) as a Drug Delivery Carrier 31 Surya K. Mallapragada and Shannon McCarthy-Schroeder

3. Development of Aery late and Methacrylate Polymer Networks for 47 Controlled Release by Photopolymerization Technology Robert Scott, Jennifer H. Ward, and Nicholas A. Peppas

4. Smart Polymers for Controlled Drug Delivery 65 Joseph Kost and SmadarA. Lapidot

5. Complexing Polymers in Drug Delivery 89 Anthony M. Lowman

6. Polylactic and Polyglycolic Acids as Drug Delivery Carriers 99 Lisa Brannon-Peppas and Michel Vert

1 • Use of Infrared and Raman Spectroscopy for Characterization of 131 Controlled Release Systems A. B. Scranton, B. Drescher, E. W. Nelson, and J. L. Jacobs

8. Accurate Models in Controlled Drug Delivery Systems 155 Balaji Narasimhan

Part II: Mechanism-Based Classification of Controlled Release Devices

9. Drug Release from Swelling-Controlled Systems 183 Paolo Colombo, Patrizia Sand, Ruggero Bettini, Christopher S. Brazel, and Nicholas A. Peppas

vii viii Contents

10. Superporous Hydrogels as a Platform for Oral Controlled Drug Delivery 211 Jun Chen, Haesun Park, and Kinam Park

11. Osmotic Implantable Delivery Systems 225 Cynthia L. Stevenson, Felix Theeuwes, and Jeremy C. Wright

12. Bioadhesive Controlled Release Systems 255 Nicholas A. Peppas, Monica D. Little, and Yanbin Huang

Part III: Micro- and Nanoparticulate Release Systems

13. Microencapsulation Technology: Interfacial Polymerization Method 271 A. Atilla Hincal and H. Siiheyla Kas

14. Nanoparticulate Controlled Release Systems for Cancer Therapy 287 C. Dubernet, E. Fattal, and P. Couvreur

15. Microencapsulation Using Coacervation/Phase Separation: An Overview 301 of the Technique and Applications H. Siiheyla Kas, and Levent Oner

16. Microsphere Preparation by Solvent Evaporation Method 329 A. Atilla Hincal and Sema

17. Nanosuspensions: A Formulation Approach for Poorly Soluble 345 and Poorly Bioavailable Drugs R. H. Mullen B. H. L. Bohm, and M. J. Grau

18. Large-Scale Production of Solid Lipid Nanoparticles (SLN) 359 and Nanosuspensions (DissoCubes) R. H. Miiller, A. Dingier, T. Schneppe, and S. Gohla

19. Solid Lipid Nanoparticles (SLN) as a Carrier System for the Controlled 377 Release of Drugs R. H. Miiller, A. Lippacher, and S. Gohla

20. Stability of Encapsulated Substances in Poly(Lactide-co-Glycolide) 393 Delivery Systems Steven P. Schwendeman, Anna Shenderova, Gaozhong Zhu, and Wenlei Jiang

21. Development of Polysaccharide Nanoparticles as Novel Drug Carrier Systems 413 C. Vauthier and P. Couvreur

Part IV: Classification of Controlled Release Devices According to Administration Site

22. An Overview of Controlled Release Systems 431 S. Venkatraman, N. Davar, A. Chester, and L. Kleiner Contents ix

23. Research and Development Aspects of Oral Controlled-Release Dosage Forms 465 Yihong Qiu and Guohua Zhang

24. A Gastrointestinal Retentive Microparticulate System to Improve Oral 505 Drug Delivery Y. Kawashima, H. Takeuchi, and H. Yamamoto

25. In Vitro-In Vivo Correlations in the Development of Solid Oral Controlled 527 Release Dosage Forms Yihong Qiu, Emil E. Samara, and Guoliang Cao

26. Gamma Scintigraphy in the Analysis of the Behavior of Controlled 551 Release Systems C. G. Wilson and N. Washington

27. Electrically Assisted Transdermal Delivery of Drugs 567 Ajay K. Banga

28. A Novel Method Based on Artificial Neural Networks for Optimizing 583 Transdermal Drug Delivery Systems Kozo Takayama and Tsuneji Nagai

29. Transdermal Drug Delivery by Skin Electroporation 597 Tani Chen, Robert Longer, and James C. Weaver

30. Enhancement of Transdermal Transport Using Ultrasound in Combination 607 with Other Enhancers Samir Mitragotri, Robert Langer, and Joseph Kost

31. Electrotransport Systems for Transdermal Delivery: 617 A Practical Implementation of Iontophoresis Erik R. Scott, J. Bradley Phipps, J. Richard Gyory, and Rama V. Padmanabhan

Part V: Peptide and Protein Release Systems

32. Controlled Release Protein Therapeutics: Effects of Process 661 and Formulation on Stability Paul A. Burke

33. Solid-State Chemical Stability of Peptides and Proteins: Application 693 to Controlled Release Formulations Elizabeth M. Topp, Yuan Song, Ashley Wilson, Rong Li, Michael J. Hageman, and Richard L. Schowen

34. Growth Factor Release from Biodegradable Hydrogels 725 to Induce Neovascularization Yoshito Ikada and Yasuhiko Tabata x Contents

35. Biopolymers for Release of Interleukin-2 for Treatment of Cancer 743 Debra J. Trantolo, Joseph D. Gresser, A. Ganiyu Jimoh, Donald L. Wise, and James C. Yang

Part VI: Medical Applications of Drug Delivery

36. Osmotic Drug Delivery from Asymmetric Membrane Film-Coated 751 Dosage Forms Mary Tanya am Ende, Scott M. Herbig, Richard W. Korsmeyer, and Mark B. Chidlaw

37. Controlled Release Pain Management Systems 787 Vasif Hasirci, Dilek Sendil, Leonidas C. Goudas, Daniel B. Carr, and Donald L. Wise

38. Biodegradable Systems for Long-Acting Nestorone 807 Debra J. Trantolo, Donald L. Wise, A. J. Moo-Young, Yung-Yueh Hsu, and Joseph D. Gresser

39. Preparation and Evaluation of Buprenorphine Microspheres 821 for Parenteral Administration William R. Ravis, Yuh-Jing Lin, and Ram Murty

40. Prolonged Release of Hydromorphone from a Novel Poly(Lactic-co-Glycolic) 837 Acid Depot System: Initial In Vitro and In Vivo Observations Leonidas C. Goudas, Daniel B. Carr, Richard M. Kream, Louis Shuster, William M. Vaughan, Joseph D. Gresser, Donald L. Wise, and Debra J. Trantolo

41. Incorporation of an Active Agent into a Biodegradable Cement: 849 Encapsulation of the Agent as Protection from Chemical Degradation During Cure and Effect on Release Profile Joseph D. Gresser, Debra J. Trantolo, Pattisapu R. J. Gangadharam, Hisanori X. Nagaoka, Yung-Yueh Hsu, and Donald L. Wise

42. The Pharmacoeconomic Value of Controlled Release Dosage Forms 865 Laura B. Gardner

Index 873