Mucoadhesive Materials and Drug Delivery Systems

Dr Vitaliy Khutoryanskiy is a Reader in Pharmaceutical Materials at the Reading School of Pharmacy, the University of Reading, UK. His expertise is on water-soluble polymers and hydrogels, mucoadhesive polymeric materials, stimuli-responsive polymers and polymeric nanomaterials.Khutoryanskiy has taught modules in Dosage Form Design and Advanced Pharmaceutics to MPharm students for the past 5 years, as well as being invited to give talks relating to mucoadhesion at various universities, companies and scientific conferences. He has written 79 peer reviewed papers, 6 reviews, 3 book chapters, 1 edited book, and 2 patent applications. Prior to joining the University of Reading he worked as a postdoctoral researcher and lecturer at many universities including the Kazakh National Technical University, Khazakhstan, where he received a PhD in polymer chemistry.

• List of Contributors xvPreface xviiSection One Structure and Physiology of Mucosal Surfaces in Relation to Drug Delivery 11 Oral Mucosa: Physiological and Physicochemical Aspects 3Gleb E. Yakubov, Hannah Gibbins, Gordon B. Proctor and Guy H. Carpenter1.1 Anatomical and Histological Aspects of Oral Cavity Tissues 31.2 Production and Composition of Saliva 81.3 Surface Architecture, Mechanical, Rheological and Transport Properties of Salivary Pellicle 161.4 Future Perspective 27References 272 Anatomy of the Eye and the Role of Ocular Mucosa in Drug Delivery 39Peter W.J. Morrison and Vitaliy V. Khutoryanskiy2.1 Introduction 392.2 Anatomy of the Eye 402.3 Introduction to Ocular Mucosa 452.4 The Role of Ocular Mucosa in Drug Delivery 472.5 Models for Ocular Drug Delivery 482.6 Recent Advances in Topical Ocular Drug Delivery 512.7 Conclusions 55References 553 Drug Delivery Across the Nasal Mucosa 61Michelle Armstrong, Shonagh Walker, Jenifer Mains and Clive G. Wilson3.1 Introduction 613.2 Drug Delivery via the Nasal Mucosa 633.3 Anatomy and Physiology of the Nasal Cavity 663.4 Disease States of the Nasal Cavity 703.5 Transport Across the Membrane 733.6 Nose-to-Brain Drug Delivery 753.7 Conclusion 76References 764 Gastrointestinal Mucosa and Mucus 83Felipe O. Varum and Abdul W. Basit4.1 Introduction 834.2 The Gastrointestinal Mucus 864.3 Conclusions 94References 945 Vaginal Mucosa and Drug Delivery 99José das Neves, Rita Palmeira-de-Oliveira, Ana Palmeira-de-Oliveira, Francisca Rodrigues and Bruno Sarmento5.1 Introduction 995.2 Drug Delivery and the Human Vagina 1005.3 Vaginal Drug Dosage Forms 1055.4 Novel Strategies for Enhanced Vaginal Drug Delivery 1105.5 Mucoadhesion and the Vaginal Environment 1115.6 Vaginal Microbicides 1145.7 Users’ Acceptability and Preferences 1165.8 Conclusions and Future Perspectives 118Acknowledgements 118References 119Section Two Understanding of Mucoadhesion and Methods of Investigation 1336 Structure and Properties of Mucins 135Monica Berry and Anthony Corfield6.1 Introduction 1356.2 General Characteristics of Mucins 1366.3 Mucin Glycosylation – Changes in Disease 1396.4 Dynamics of Mucin Synthesis and Function 1426.5 Mucin Gel Formation on Cell Surfaces 1436.6 Mucin Therapeutics 1486.7 Polysaccharide Coatings to Enable Probiotic Delivery 1496.8 Gene Cloning and Drug Delivery 1496.9 Chemo-Enzymatic Synthesis of O-Glycans for Drug Delivery 1496.10 Glycan Legislation 150References 1517 Theories of Mucoadhesion 159John D. Smart7.1 Introduction 1597.2 Mucous Membranes 1597.3 Mucoadhesives 1607.4 The Adhesive Interaction 1607.5 Mucoadhesion 1627.6 Solid Mucoadhesion 1627.7 Semi-solid Mucoadhesion 1687.8 Liquid Mucoadhesion 1697.9 Modified Materials 1697.10 Conclusions 170References 1708 Methods to Study Mucoadhesive Dosage Forms 175Maya Davidovich-Pinhas and Havazelet Bianco-Peled8.1 Introduction 1758.2 Model Surfaces for Mucoadhesion Evaluation 1768.3 Methods to Evaluate Mucoadhesion Dosage Form 1778.4 Summary 189References 1899 Methods for Assessing Mucoadhesion: The Experience of an Integrative Approach 197Gleb E. Yakubov, Scott Singleton and Ann-Marie Williamson9.1 Mucins and Mucosal Architecture 1979.2 Concept of Length and Time Scales in Mucoadhesion 1989.3 Experimental Approaches to Measuring Mucosal Interactions 2019.4 Integrative Approaches. Layer-by-Layer Assembled Multilayers: A Tool for Studying Mucoadhesion 2089.5 Future Perspective 224References 225Section Three Mucoadhesive Materials 23310 Chitosan 235Joshua Boateng, Isaac Ayensu and Harshavardhan Pawar10.1 Introduction 23510.2 Material and Physicochemical Properties of Chitosan 23610.3 Applications 24010.4 Material Characterisation of Bioadhesive Chitosan Formulations 24510.5 Summary 247References 24711 Thiomers 255Christiane Müller and Andreas Bernkop-Schnürch11.1 Introduction 25511.2 Thiolated Polymers 25711.3 Sulfhydryl Group Contribution 26011.4 Mechanism of Mucoadhesion 26211.5 Mucoadhesive Properties 26311.6 Additional Properties of Thiolated Polymers 26411.7 Mucoadhesive Dosage Forms Based on Thiomers 26711.8 Biopharmaceutical Use of Thiomers 26911.9 Safety and Stability 27211.10 Conclusion 273References 27312 Boronate-Containing Polymers 279Alexander E. Ivanov12.1 Introduction 27912.2 Fundamentals of Borate and Boronate Interactions with Monoand Oligosaccharides 28012.3 Multipoint Association of BCPs with Polysaccharides 28212.4 Formation of Interpolymer Complexes of BCPs with Mucin Glycoprotein 28412.5 Interaction of BCPs with Animal Cells 28612.6 Polymeric Mucoadhesive Materials and Devices Employing Boronate – Carbohydrate Interactions 28912.7 Conclusions 291References 29213 Liposome-Based Mucoadhesive Formulations 297Kohei Tahara and Hirofumi Takeuchi13.1 Introduction 29713.2 Oral Administration of Surface-Modified Liposomes with the Mucoadhesive Properties 29813.3 The Behaviour of Liposomes After Oral Administration 30013.4 Pulmonary Administration of Peptide Drugs with Liposomal Formulations: Effective Surface Modification Using Chitosan or Poly(Vinyl Alcohol) with a Hydrophobic Anchor 30113.5 Modification of Liposomes Using Mucoadhesive Polymer– Wheat Germ Agglutinin Conjugates for Pulmonary Drug Delivery 30413.6 Conclusions 306References 30614 Acrylated Polymers 309Maya Davidovich-Pinhas and Havazelet Bianco-Peled14.1 Introduction 30914.2 Mucoadhesion 31014.3 Types of Interactions Involved in the Mucoadhesion Process 31014.4 Interactions Between Acrylate and Mucin Glycoprotein 31114.5 Acrylated Alginate (Alginate-PEGAc) 31414.6 Summary 325References 325Index 329