Innovations in Oral Solid Drug Delivery: Advances in nanotechnology, controlled formulations & peptide delivery

Table of Contents :

Innovations in oral solid drug delivery
Executive summary 18
Market overview, dynamics and outlook 18
Advances in nanotechnology 19
Innovations in transitioning injectables to oral delivery 20
Advances in delayed & controlled release delivery 21
Advances in oral prodrug delivery 22
Advances in taste masking technologies 23
Innovative companies 24
Chapter 1 Market overview, dynamics and outlook 28
Summary 28
Market overview 29
Market dynamics 31
Key indications 33
Key trends 38
Nanomedicine 38
Transitioning from injectables 39
Prodrugs 40
Chrono release 41
ODT 41
OSF 42
Funding issues 42
Poor patient compliance 42
Injections 42
Poor absorbption 42
Pediatric 43
Geriatric 43
Solubility and variable absorption 43
Reduction of side effect profiles 44
Non-invasive protein delivery 45
Transition from injectables to preferred route of oral drug delivery 45
Directed delivery and delayed delivery to reduce side effect potential 46
Formulation technologies for poorly soluble compounds 46
Taste masking for pediatric and geriatric formulations 47
Competitive landscape 48
Conclusions and key findings 50
Chapter 2 Advances in nanotechnology 56
Summary 56
Introduction 57
Nanotechnology platforms with application for oral drug delivery 59
Self-Emulsifying Controlled Release Tablet system (SECRET) 59
Technology 59
Application 59
Biotransport nanomedicine technology 60
Technology 60
Application 60
Nanobodies 61
Technology 61
Application 61
NanoDel nanoparticles 62
Technology 62
Application 62
P-gpMask 63
Technology 63
Application 64
NanoDRY and NanoCOAT 64
Technology 64
Application 64
Solumer 67
Technology 67
Application 67
Nanocells 69
Technology 69
Application 70
Polymeric Nano-Delivery System (PNDS) 70
Technology 70
Application 71
FluidCrystal NP Oral nanoparticles 71
Technology 71
Application 72
CaP Technology and BioOral 72
Technology 72
Application 73
Nab Technology and Protospheres 73
Technology 73
Application 73
NanoCrystal Technology 74
Technology 74
Application 74
Bioral 75
Technology 75
Application 75
Squalenoyl nanoparticles 76
NanoMega 76
NOD Pharmaceutical 76
Chapter 3 Innovations in transitioning injectables to oral delivery 80
Summary 80
Introduction 81
Drivers 81
Patient acceptability & compliance 81
Cost savings 81
Restraints 82
Advances in injectable delivery 82
Challenges of oral drug delivery 83
Technologies used in oral drug delivery of peptides and proteins 84
Enzyme inhibitors 84
Permeation enhancers 85
Mucoadhesives 85
Encapsulation technologies 85
M-cell targeting 86
Competitive landscape 86
Osteoporosis and other bone related conditions 88
Calcitonin 88
Current therapies & market landscape 89
Oral products in development 91
Parathyroid hormone 94
Current therapies & market landscape 94
Oral products in development 96
Combined oral calcitonin and PTH approaches 97
Bisphosphonates 97
Current therapies & market landscape 97
Novel oral products in development 99
Diabetes and other metabolic diseases 104
Oral insulin 104
Oramed Pharmaceuticals 104
Biocon Ltd 105
Emisphere Technologies 105
Diabetology 106
NOD Pharmaceuticals 106
Access Pharmaceuticals 107
NanoMega Medical Corporation 107
Biodel Inc 108
Metabolic Pharmaceuticals Ltd 108
Glucagon-like peptide-1 (GLP-1) and GLP-1 analogs 108
Oral GLP-1 & GLP-1 analogs 110
Obesity 114
Alzheimer's and other CNS conditions 115
Oligotropin 115
Endometriosis and prostate cancer 115
Leuprolide 115
Cardiovascular 116
Angiotensin analogs 116
Innovative approaches to oral vaccine development 118
Mucosis B.V. 119
Plug-and-Play Technology 119
GEM Particles 119
Mimopath 119
Ondek Pty Ltd 120
Helicobacter pylori Platform Technology (HPPT) 120
Infexion 121
Kancer 121
Immune Solutions 121
Liporale 122
Chapter 4 Advances in delayed & controlled release delivery 124
Summary 124
Introduction 125
Types of controlled release systems 125
Sustained release 125
Pulsatile release 125
Modified drug delivery 126
Fast disintegrating technologies 126
Pediatric formulations - ODT 126
Schizophrenia and bipolar disorder – ODT 127
Alzheimer's disease - ODT 128
Parkinson's disease - ODT 129
Anxiety and panic disorder - ODT 129
Major depressive disorder - ODT 130
Nausea and vomiting - ODT 131
Migraine - ODT 131
Autism – ODT 132
GERD and gastroparesis – ODT 133
Release control mechanisms 135
Zero order 135
Congestive heart failure and hypertension – sustained release 135
Pain – sustained release 138
ADHD – sustained release 141
Multiple sclerosis – sustained release 141
Muscle relaxant – sustained release 142
Parkinson's disease - sustained release 144
Depression – sustained release 144
Binary 147
Diabetes type 2 - combination products 147
Hypertension - combination products 149
Other 150
Biphasic release of drugs 150
Asthma – biphasic release 151
Pain – biphasic release 151
ADHD – biphasic release 152
Hypertension – biphasic release 152
Positioned 153
Parkinson's disease – positioned biphasic release 154
Insomnia – positioned biphasic release 155
Spasticity – positioned biphasic release 156
GERD – positioned release 156
Diabetes type 2 - positioned extended release 157
Hot flashes – positioned extended release 157
Pain – positioned extended release 158
GERD – positioned extended release 158
Parkinson's disease – positioned extended release 158
Others 159
Accelerated 159
Timed 159
Multiple pulse 160
Targeted delivery to the colon 160
Ulcerative colitis, gastroenteritis – targeted colon release 161
Nutraceutical – targeted colon release 162
Polysaccharide colon selective 163
COLAL technology 163
Chrono release 164
Rheumatoid arthritis – chrono release 165
Severe asthma – chrono release 166
Polymyalgia rheumatica – chrono release 166
Insomnia – chrono release 166
Sublingual formulations 167
Formulations to counteract opiate or psychostimulant abuse 167
Trigger-Lock 168
OraGuard 169
NanoDRY and NanoCOAT 170
ORADUR 170
Aversion Technology 171
Egalet ADPREM 172
DETERx 173
Avert 174
Strategic alliances 174
Chapter 5 Advances in oral prodrug delivery 178
Summary 178
Introduction 179
Classification based on site of conversion to active drug 181
Classification based on chemical linkages or promoiety/carriers that attach to
the active drug 182
Classification based on the deficiency in the active drug 183
Classification based on carrier-linked or bioprecursor categories 183
Applications of prodrug technology 185
Reducing side effect profile 185
Introducing site specificity – colon 185
Taste masking applications 186
Marketed products and market share 186
Antiviral prodrugs 186
Oseltamivir 186
Valaciclovir 187
Valganciclovir 189
Famciclovir 190
Anticancer prodrugs 191
TS-1 192
Cardiovascular prodrugs 194
ACE inhibitors 194
Angiotensin II receptor antagonists 194
HMG Co A reductase inhibitors 195
Respiratory prodrugs 195
Bambuterol 195
CNS prodrugs 195
Lisdexamfetamine 195
Late and early stage development product formulations 197
Improving oral bioavailability/reducing toxicity of older marketed injectable drugs 197
Antiviral prodrugs 197
Cidofovir 197
Vidarabine 200
Zanamivir 200
Anticancer prodrugs 201
Triciribine 201
Camptothecin 202
Gemcitabine 204
Docetaxel 206
Methotrexate 208
Aimpila 210
FAP activated ultra-smart prodrug cytotoxic agent 211

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