Lipospheres in Drug Targets and Delivery: Approaches, Methods, and Applications

Lipospheres in Drug Targets and Delivery: Approaches, Methods, and Applications......Page 2
Preface......Page 4
Editor......Page 6
Contributors......Page 8
Table of Contents......Page 10
CONTENTS......Page 11
1.2 INTRODUCTION TO COLLOIDAL DRUG CARRIERS......Page 12
1.3 FROM NANOEMULSIONS TO NANOPELLETS: SLN ? HISTORY AND SCOPE......Page 13
1.4.2.1 High-Shear Homogenization and Ultrasound......Page 14
1.4.2.2.1 Hot Homogenization......Page 15
1.4.2.3 SLN Prepared by Solvent Emulsification/Evaporation......Page 16
1.4.2.6 Comparison of Different Formulation Procedures......Page 17
1.4.2.7.1 Influence of the Lipid......Page 19
1.4.2.7.2 Influence of the Emulsifier......Page 20
1.4.3 STERILIZATION......Page 21
1.4.4 STABILIZATION BY DRYING......Page 22
1.5 CHARACTERIZATION OF SLN......Page 24
1.6 ADVANTAGES AND DISADVANTAGES OF SLN AND NLC......Page 27
REFERENCES......Page 28
2.1 INTRODUCTION......Page 33
2.2 MELT DISPERSION TECHNIQUE......Page 34
2.2.1 EFFECT OF THE STIRRING CONDITIONS......Page 40
2.2.2 EFFECT OF THE STABILIZER TYPE AND CONCENTRATION......Page 41
2.3 SOLVENT EVAPORATION TECHNIQUE......Page 43
2.4 DRUG-CONTAINING LS......Page 45
2.5 IN VITRO DRUG RELEASE......Page 47
2.6 CONCLUSIONS......Page 48
REFERENCES......Page 49
3.1 GENERAL CONSIDERATIONS......Page 51
3.2 PARTICLE SIZE......Page 52
3.2.1 PHOTON CORRELATION SPECTROSCOPY......Page 53
3.2.2 LASER LIGHT SCATTERING......Page 54
3.3 ZETA POTENTIAL......Page 56
3.4 CRYSTALLINITY AND POLYMORPHISM......Page 57
3.4.1 DSC......Page 59
3.4.2 X-RAY DIFFRACTION......Page 60
3.5.1 TRANSMISSION ELECTRON MICROSCOPY......Page 63
3.5.3 OPTICAL MICROSCOPY......Page 67
3.6 INTERACTION WITH INCORPORATED DRUGS......Page 68
3.7 CONCLUSION......Page 70
REFERENCES......Page 71
4.1 INTRODUCTION......Page 77
4.2.1 GENERAL CONSIDERATIONS......Page 79
4.2.2 PROTEIN STABILITY DURING FORMULATION PROCEDURES......Page 80
4.3.1 PREPARATION METHODS......Page 81
4.3.1.2 Multiple Microemulsion......Page 82
4.3.1.3 Cosolvent Method......Page 83
4.3.2.1 Preparation Method......Page 84
4.3.2.2 Phospholipid Content......Page 85
4.3.3 STABILITY OF PROTEIN DRUGS DURING PREPARATION......Page 87
4.4.1 CLASSIC LIPOSPHERES......Page 88
4.4.2 POLYMER LIPOSPHERES......Page 90
4.5 CONCLUSION......Page 91
REFERENCES......Page 94
5.1 INTRODUCTION......Page 97
5.2.1 FORMULATIONS......Page 98
5.2.2 ANTIGENS......Page 100
5.2.3 ADJUVANTS......Page 101
5.3.1 EFFECT OF LIPOSPHERE FAT COMPOSITION......Page 102
5.3.4 EFFECT OF PARTICLE SIZE DISTRIBUTION......Page 103
5.4.1 ADJUVANT ACTIVITY OF LIPID A......Page 104
5.5 POLYMERIC BIODEGRADABLE LIPOSPHERE VACCINES......Page 105
5.6 CONCLUSIONS......Page 106
REFERENCES......Page 107
CONTENTS......Page 110
6.1 INTRODUCTION......Page 111
6.2.1 ON CYTOTOXICITY......Page 112
6.2.2 ON BIODEGRADATION......Page 114
6.3.1 ON CYTOTOXICITY......Page 116
6.3.2 ON BIODEGRADATION......Page 117
6.3.3 ON I N VITRO TRANSFECTION EFFICACY......Page 119
6.4.1 ON CYTOTOXICITY......Page 120
6.4.2 ON BIODEGRADATION......Page 125
6.4.3 ON IN VITRO TRANSFECTION EFFICACY......Page 127
6.6 MECHANISM OF UPTAKE AND FATE IN THE CELL......Page 129
REFERENCES......Page 131
CONTENTS......Page 135
7.1 INTRODUCTION......Page 136
7.3.3 SLN PREPARED BY SOLVENT EMULSIFICATION /EVAPORATION......Page 137
7.4 ALTERNATIVE SYSTEMS: NANOSTRUCTURED LIPID CARRIERS......Page 138
7.5.1 MEASUREMENT OF PARTICLE SIZE , PARTICLE SHAPE , AND ZETA POTENTIAL......Page 139
7.5.2 DETERMINATION OF CRYSTALLINITY AND LIPID MODIFICATIONS......Page 140
7.6 DRUG RELEASE......Page 141
7.7 STORAGE STABILITY......Page 142
7.9 METHODS FOR EVALUATING CUTANEOUS UPTAKE......Page 143
7.10.3 INFLUENCE OF CARRIER SYSTEMS ON EPIDERMAL INPUT AND SKIN PERMEATION......Page 144
7.10.5 ANTIACNE DRUGS AND COSMETICS......Page 145
7.10.7 COLLOIDAL CARRIERS IN COSMETICS......Page 146
REFERENCES......Page 147
8.1 INTRODUCTION......Page 151
8.2 NUCLEIC ACID STABILITY: GENERAL CONSIDERATIONS AND IMPROVEMENT......Page 153
8.3.1 MATERIALS AND PREPARATION METHODS......Page 155
8.3.2 FORMATION OF CLS/DNA COMPLEX......Page 156
8.4 CYTOTOXICITY OF NUCLEIC ACIDS FROM CLS......Page 159
8.5 TRANSFECTION EFFICIENCY......Page 161
REFERENCES......Page 164