Contents

17.1 Introduction 318

17.2 General Properties of Polymeric Micelles for Drug Formulation 319

17.2.1 Building Blocks for Polymeric Micelles 319

17.2.2 Physico-Chemical Properties of Polymeric Micelles 321

17.2.2.1 Size and Size Distribution 321

17.2.2.2 Morphology 321

17.2.2.3 Stability 322

17.2.3 Preparation of Block Copolymer Micelle Formulations 323

17.2.4 Properties of Micelle Formulations 324

17.2.4.1 Drug Partitioning 324

17.2.4.2 Factors Affecting Drug Loading 324

17.2.4.3 Factors Influencing Drug Release from Polymeric Micelles 325

17.3 Physical Characteristics of Polymeric Micelles for Clinical

Applications in Cancer Therapy 326

17.3.1 Doxorubicin 327

17.3.1.2 SP1049C 328

17.3.2 Paclitaxel 329

17.3.2.1 Genexol-PM 329

17.4 Interactions of Polymeric Micelles with Cancer Cells 330

17.4.1 Drug Diffusion 331

17.4.2 Cellular Internalization 332

17.4.3 In Vitro Cytotoxicity 334

17.4.4 Influence or Effect on Multi-Drug Resistance 335

17.5 In Vivo Biological Performance of Block Copolymer Micelles 336

17.5.1 Fate of Polymeric Micelles In Vivo 337

17.5.2 In Vivo Drug Release Profiles 338

17.5.3 Toxicity, Pharmacokinetics, and Anti-Cancer Efficacy of Drugs

Formulated in Block Copolymer Micelles 339

17.5.3.1 Doxorubicin Formulations (SP1049C and NK911) 339

17.5.3.2 Paclitaxel Formulations (Genexol-PM and NK105) 339

17.6 Evolution of Polymeric Micelles 340

17.6.1 Triggered Stimulation of Drug Activation or Release 340

17.6.1.1 Ultrasonic Irradiation 340

17.6.1.2 Thermosensitive Systems 341

17.6.1.3 Photodynamic Therapy 342

17.6.2 Active Targeting 342

17.6.2.1 Ligand Coupling 343

17.6.2.2 pH-Responsive Systems 344

17.7 Future Perspectives 345

Acknowledgments 345

References 345

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