Lipid nanoparticles for the delivery of poorly water-soluble drugs

Journal of Pharmacy and Pharmacology

Volumn 62, Issue 11, 2010, Pages 1637-1645

  Bunjes, Heike ^a  

^a TECHNICAL UNIVERSITY OF BRAUNSCHWEIG   (Germany)

Author keywords

lipid drug carrier systems; parenteral fat emulsions; poorly soluble drugs; solid lipid nanoparticles; solubilisation

Indexed keywords

AMPHOTERICIN B; BETAMETHASONE VALERATE; BROMOCRIPTINE; CAMPTOTHECIN; CLOBETASOL PROPIONATE; CLORICROMEN; CLOZAPINE; CYCLOSPORIN; DEXAMETHASONE; DIAZEPAM; DOCETAXEL; ESTRADIOL; ETOMIDATE; ETOPOSIDE; IDARUBICIN; INDOMETACIN; MENADIONE; NIFEDIPINE; PACLITAXEL; PREDNICARBATE; PREDNISOLONE; PROPOFOL; RETINOID DERIVATIVE; SOLID LIPID NANOPARTICLE; TAMOXIFEN; TETRACAINE; TRIPTOLIDE; UBIDECARENONE; UNINDEXED DRUG; VINPOCETINE;

DRUG DELIVERY SYSTEM; DRUG DISTRIBUTION; DRUG RELEASE; NANOEMULSION; PARTICLE SIZE; PHYSICAL CHEMISTRY; REVIEW; SOLID STATE; TRANSMISSION ELECTRON MICROSCOPY;

BIOLOGICAL AVAILABILITY; COLLOIDS; CRYSTALLIZATION; DOSAGE FORMS; DRUG DELIVERY SYSTEMS; EMULSIONS; LIPIDS; NANOPARTICLES; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; TECHNOLOGY, PHARMACEUTICAL; WATER;

EID: 78649648145     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.2042-7158.2010.01024.x     Document Type: Review

References (103)

1. Wretlind A,. Development of fat emulsions. J Parent Ent Nutr 1981; 5: 230-235.
2. Carpentier YA, Dupont IE,. Advances in intravenous lipid emulsions. World J Surg 2000; 24: 1493-1497.
3. Driscoll DF,. Lipid injectable emulsions: 2006. Nutr Clin Pract 2006; 21: 381-386.
4. Lyons RT, Carter EG,. Lipid emulsions for intravenous nutrition and drug delivery. In:, Gunstone FD, Padley FB, eds. Lipid Technologies and Applications. New York: Marcel Dekker, 1997: 535-556.
5. Férézou J, et al. Lipid composition and structure of commercial parenteral emulsions. Biochim Biophys Acta 1994; 1213: 149-158.
6. Klang S, Benita S,. Design and evaluation of submicron emulsions as colloidal drug carriers for intravenous administration. In:, Benita S, ed. Submicron Emulsions in Drug Targeting and Delivery. Amsterdam: Harwood Academic Publishers, 1998: 119-152.
7. Szebeni J, et al. Formation of complement-activating particles in aqueous solutions of Taxol: possible role in hypersensitivity reactions. Int Immunopharmacol 2001; 1: 721-735.
8. Malcomson C, et al. Effect of oil on the level of solubilization of testosterone propionate into nonionic oil-in-water microemulsions. J Pharm Sci 1998; 87: 109-116.
9. Larsen DB, et al. Characteristics of drug substances in oily solutions. Drug release rate, partitioning and solubility. Int J Pharm 2002; 232: 107-117.
10. Constantinides PP, et al. Tocol emulsions for drug solubilization and parenteral delivery. Adv Drug Deliv Rev 2004; 56: 1243-1255.
11. Müller RH, et al. SolEmuls®- novel technology for the formulation of i.v. emulsions with poorly soluble drugs. Int J Pharm 2004; 269: 293-302.
12. Washington C,. Stability of lipid emulsions in drug delivery. Adv Drug Deliv Rev 1996; 20: 131-145.
13. Drummond DC, et al. Pharmacokinetics and in vivo drug release rates in liposomal nanocarrier development. J Pharm Sci 2008; 97: 4696-4740.
14. Owens DE, Peppas NA,. Opsonization, biodistribution, and pharmacokinetics of polymeric nanoparticles. Int J Pharm 2006; 307: 93-102.
15. Tamilvanan S,. Formulation of multifunctional oil-in-water nanosized emulsions for active and passive targeting of drugs to otherwise inaccessible internal organs of the body. Int J Pharm 2009; 381: 62-76.
16. Magenheim B, et al. A new in vitro technique for evaluation of drug release profile from colloidal carriers-ultrafiltration technique at low pressure. Int J Pharm 1993; 94: 115-125.
17. Takino T, et al. Long circulating emulsion carrier systems for highly lipophilic drugs. Biol Pharm Bull 1994; 17: 121-125.
18. Washington C, Evans K,. Release rate measurements of model hydrophobic solutes from submicron triglyceride emulsions. J Control Release 1995; 33: 383-390.
19. Lundberg BB, et al. A lipophilic paclitaxel derivative incorporated in a lipid emulsion for parenteral administration. J Control Release 2003; 86: 93-100.
20. Drug Bank. (accessed October 2009).
21. Westesen K, Siekmann B,. Biodegradable colloidal drug carrier systems based on solid lipids. In:, Benita S, ed. Microencapsulation. New York: Marcel Dekker, 1996: 213-258.
22. Speiser P,. Lipidnanopellets als Trägersystem für Arzneimittel zur peroralen Anwendung. European Patent Application EP 0,167,825, 1986.
23. Gasco MR, Morel S,. Lipospheres from microemulsions. Farmaco 1990; 45: 1127-1128.
24. Siekmann B, Westesen K,. Submicron-sized parenteral carrier systems based on solid lipids. Pharm Pharmacol Lett 1992; 1: 123-126.
25. Müller RH, et al. Solid lipid nanoparticles (SLN)-an alternative colloidal carrier system for controlled drug delivery. Eur J Pharm Biopharm 1995; 41: 62-69.
26. Sjöström B, BergenstÃhl B,. Preparation of submicron drug particles in lecithin-stabilized o/w emulsions. I. Model studies of the precipitation of cholesteryl acetate. Int J Pharm 1992; 8: 53-62.
27. Siekmann B, Westesen K,. Investigations on solid lipid nanoparticles prepared by precipitation in o/w emulsions. Eur J Pharm Biopharm 1996; 42: 104-109.
28. Zur Mühlen A, et al. Solid lipid nanoparticles (SLN) for controlled drug delivery-drug release and release mechanism. Eur J Pharm Biopharm 1998; 45: 149-155. (Pubitemid 28167741)
29. Hu FQ, et al. Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization. Int J Pharm 2002; 239: 121-128.
30. Schubert MA, Müller-Goymann CC,. Solvent injection as a new approach for manufacturing lipid nanoparticles-evaluation of the method and process parameters. Eur J Pharm Biopharm 2003; 55: 125-131.
31. Siekmann B, Westesen K,. Melt-homogenized solid lipid nanoparticles stabilized by the nonionic surfactant tyloxapol. II. Physicochemical characterization and lyophilisation. Pharm Pharmacol Lett 1994; 3: 225-228.
32. Schwarz C, Mehnert W,. Freeze-drying of drug-free and drug-loaded solid lipid nanoparticles (SLN). Int J Pharm 1997; 157: 171-179.
33. Cavalli R, et al. Sterilization and freeze-drying of drug-free and drug-loaded solid lipid nanoparticles. Int J Pharm 1997; 148: 47-54.
34. Freitas C, Müller RH,. Spray-drying of solid lipid nanoparticles (SLN). Eur J Pharm Biopharm 1998; 46: 145-151.
35. Lim S, Kim CK,. Formulation parameters determining the physicochemical characteristics of solid lipid nanoparticles loaded with all-trans retinoic acid. Int J Pharm 2002; 243: 135-146.
36. Bunjes H, Siekmann B,. Manufacture, characterization and applications of solid lipid nanoparticles as drug delivery systems. In: Microencapsulation, 2nd edition., Benita S, ed. New York: Taylor & Francis, 2006: 213-268.
37. Westesen K, Wehler T,. Physicochemical characterization of a model intravenous oil-in-water emulsion. J Pharm Sci 1992; 81: 777-786.
38. Han J, Washington C,. Partition of antimicrobial additives in an intravenous emulsion and their effect on emulsion physical stability. Int J Pharm 2005; 288: 263-271.
39. Hagemann J,. Thermal behavior and polymorphism of acylglycerides. In:, Garti N, Sato K, eds. Crystallization and Polymorphism of Fats and Fatty Acids. New York: Marcel Dekker, 1988: 9-95.
40. Hernqvist L,. Crystal structures of fats and fatty acids. In:, Garti N, Sato K, eds. Crystallization and Polymorphism of Fats and Fatty Acids. New York: Marcel Dekker, 1988: 97-137.
41. Bunjes H, Unruh T,. Characterization of lipid nanoparticles by differential scanning calorimetry, X-ray and neutron scattering. Adv Drug Deliv Rev 2007; 59: 379-402.
42. Siekmann B, Westesen K,. Thermoanalysis of the recrystallization process of melt homogenized glyceride nanoparticles. Colloids Surf B: Biointerfaces 1994; 3: 159-175.
43. Freitas C, Müller RH,. Correlation between long-term stability of solid lipid nanoparticles (SLN) and crystallinity of the lipid phase. Eur J Pharm Biopharm 1999; 47: 125-132.
44. Rosenblatt KM, Bunjes H,. Poly(vinyl alcohol) as emulsifier stabilizes solid triglyceride drug carrier nanoparticles in the α-modification. Mol Pharmaceutics 2009; 6: 105-120.
45. Bunjes H, Koch MHJ,. Saturated phospholipids promote crystallization but slow down polymorphic transitions in triglyceride nanoparticles. J Control Release 2005; 107: 229-243.
46. Bunjes H, et al. Crystallization tendency and polymorphic transitions in triglyceride nanoparticles. Int J Pharm 1996; 129: 159-173.
47. Westesen K, et al. Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release potential. J Control Release 1997; 48: 223-236.
48. Bunjes H, et al. Influence of emulsifiers on the crystallization of solid lipid nanoparticles. J Pharm Sci 2003; 92: 1509-1520.
49. Bunjes H, et al. Incorporation of the model drug ubidecarenone into solid lipid nanoparticles. Pharm Res 2001; 18: 287-293.
50. Müller RH, et al. Cyclosporine-loaded solid lipid nanoparticles (SLN): Drug-lipid physicochemical interactions and characterization of drug incorporation. Eur J Pharm Biopharm 2008; 68: 535-544.
51. Jenning V, et al. Vitamin A loaded solid lipid nanoparticles for topical use: drug release properties. J Control Release 2000; 66: 115-126.
52. Bunjes H, et al. Visualizing the structure of triglyceride nanoparticles in different crystal modifications. Langmuir 2007; 23: 4005-4011.
53. Westesen K, et al. Investigations on the physical state of lipid nanoparticles by synchrotron radiation X-ray diffraction. Int J Pharm 1993; 93: 189-199.
54. Bunjes H, et al. Effects of surfactants on the crystallization and polymorphism of lipid nanoparticles. Progr Colloid Polym Sci 2002; 121: 7-10.
55. Unruh T, et al. Observation of size-dependent melting in lipid nanoparticles. J Phys Chem B 1999; 103: 10373-10377.
56. Bunjes H, et al. Effect of particle size on colloidal solid triglycerides. Langmuir 2000; 16: 5234-5241.
57. Bunjes H,. Characterization of solid lipid nano- and microparticles. In:, Nastruzzi C, Esposito E, eds. Lipospheres in Drug Targets and Delivery. Boca Raton: CRC Press, 2004: 41-66.
58. Zur Mühlen A, et al. Atomic force microscopy studies of solid lipid nanoparticles. Pharm Res 1996; 13: 1411-1416.
59. Illing A, Unruh T,. Investigations on the flow behavior of dispersions of solid triglyceride nanoparticles. Int J Pharm 2004; 284: 123-131.
60. Westesen K, Siekmann B,. Investigation of the gel formation of phospholipid stabilized solid lipid nanoparticles. Int J Pharm 1997; 151: 35-45.
61. Unruh T, et al. Self-assembly of triglyceride nanocrystals in suspension. Langmuir 2002; 18: 1796-1800.
62. Schubert MA, et al. Structural investigations on lipid nanoparticles containing high amounts of lecithin. Eur J Pharm Sci 2006; 27: 226-236.
63. Jores K, et al. Investigations on the structure of solid lipid nanoparticles (SLN) and oil-loaded solid lipid nanoparticles by photon correlation spectroscopy, field-flow fractionation and transmission electron microscopy. J Control Release 2004; 95: 217-227.
64. Esposito E, et al. Solid lipid nanoparticles as delivery systems for bromocriptine. Pharm Res 2008; 25: 1521-1530.
65. Lippacher A, et al. Semisolid SLN dispersions for topical application: influence of the formulation and production parameters on viscoelastic properties. Eur J Pharm Biopharm 2002; 53: 155-160.
66. Illing A, et al. Investigation on particle self-assembly in solid lipid based colloidal drug carrier systems. Pharm Res 2004; 21: 592-597.
67. Petersen S, et al. The physical state of lipid nanoparticles affects their in vitro cell viability. Proc 36th Annual Meeting & Exposition of the Controlled Release Society, Copenhagen, Denmark, 2009.
68. Jenning V, Gohla SH,. Encapsulation of retinoids in solid lipid nanoparticles (SLN). J Microencaps 2001; 18: 149-158.
69. Rosenblatt KM, Bunjes H,. A screening approach to determine the solubilization capacity of lipid nanoparticles for poorly water soluble drugs. Proc 6th World Meeting Pharm. Biopharm. Pharm. Technol., Barcelona, Spain, 2008.
70. Ahlin P, et al. Influence of spin probe structure on its distribution in SLN dispersions. Int J Pharm 2000; 196: 241-244.
71. Jores K, et al. Physicochemical investigations on solid lipid nanoparticles and on oil-loaded solid lipid nanoparticles: A nuclear magnetic resonance and electron spin resonance study. Pharm Res 2003; 20: 1274-1283.
72. Jores K, et al. Solid Lipid Nanoparticles (SLN) and oil-loaded SLN studied by spectrofluorometry and raman spectroscopy. Pharm Res 2005; 22: 1887-1897.
73. Sivaramakrishnan R, et al. Glucocorticoid entrapment into lipid carriers-characterisation by parelectric spectroscopy and influence on dermal uptake. J Control Release 2004; 97: 493-502.
74. Hu L, et al. Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs. J Pharm Pharmacol 2004; 56: 1527-1535.
75. Yang SC, et al. Body distribution in mice of intravenously injected camptothecin solid lipid nanoparticles and targeting effect on brain. J Control Release 1999; 59: 299-307.
76. Ugazio E, et al. Incorporation of cyclosporin A in solid lipid nanoparticles (SLN). Int J Pharm 2002; 241: 341-344.
77. Venkateswarlu V, Manjunath K,. Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles. J Control Release 2004; 95: 627-638.
78. Luo Y, et al. Solid lipid nanoparticles for enhancing vinpocetine's oral bioavailability. J Control Release 2006; 114: 53-59.
79. Boyd BJ,. Characterisation of drug release from cubosomes using the pressure ultrafiltration method. Int J Pharm 2003; 260: 239-247.
80. Rosenblatt K, et al. Drug release from differently structured monoolein/poloxamer nanodispersions studied with differential pulse polarography and ultrafiltration at low pressure. J Pharm Sci 2007; 96: 1565-1575.
81. Chen DB, et al. In vitro and in vivo study of two types of long-circulating solid lipid nanoparticles containing paclitaxel. Chem Pharm Bull 2001; 49: 1444-1447.
82. Washington C,. Evaluation of non-sink dialysis methods for the measurement of drug release from colloids: effects of drug partition. Int J Pharm 1989; 57: 71-74.
83. Bondì ML, et al. Preparation and characterization of solid lipid nanoparticles containing cloricromene. Drug Delivery 2003; 10: 245-250.
84. Petersen S, et al. Flow cytometry as a new approach to investigate drug transfer between lipid particles. Mol Pharmaceutics (accessed February 2010, epub ahead of print).
85. Rosenblatt KM, Bunjes H,. Comparison of drug release from trimyristin nanosuspensions and nanoemulsions with differential pulse polarography, Proc 33th Annual Meeting & Exposition of the Controlled Release Society, Vienna, Austria, 2006.
86. Koziara JM, et al. Paclitaxel nanoparticles for the potential treatment of brain tumors. J Control Release 2004; 99: 259-269.
87. Koziara JM, et al. In-vivo efficacy of novel paclitaxel nanoparticles in paclitaxel-resistant human colorectal tumors. J Control Release 2006; 112: 312-319.
88. Xu Z, et al. The performance of docetaxel-loaded solid lipid nanoparticles targeted to hepatocellular carcinoma. Biomaterials 2009; 30: 226-232.
89. Rote Liste. (accessed October 2009).
90. SciFinder Scholar, 2007, American Chemical Society.
91. Harivardhan Reddy L, et al. Influence of administration route on tumor uptake and biodistribution of etoposide loaded solid lipid nanoparticles in Dalton's lymphoma tumor bearing mice. J Control Release 2005; 105: 185-198.
92. Zara GP, et al. Pharmacokinetics and tissue distribution of idarubicin-loaded solid lipid nanoparticles after duodenal administration to rats. J Pharm Sci 2002; 91: 1324-1333.
93. Ma P, et al. Development of idarubicin and doxorubicin solid lipid nanoparticles to overcome Pgp-mediated multiple drug resistance in leukemia. J Biomed Nanotechnol 2009; 5: 151-161.
94. Cavalli R, et al. Preparation and characterization of solid lipid nanospheres containing paclitaxel. Eur J Pharm Sci 2000; 10: 305-309.
95. Serpe L, et al. Cytotoxicity of anticancer drugs incorporated in solid lipid nanoparticles on HT-29 colorectal cancer cell line. Eur J Pharm Biopharm 2004; 58: 673-680.
96. Lee MK, et al. Preparation, characterization and in vitro cytotoxicity of paclitaxel-loaded sterically stabilized solid lipid nanoparticles. Biomaterials 2007; 28: 2137-2146.
97. Fontana G, et al. Solid lipid nanoparticles containing tamoxifen. Characterization and in vitro antitumoral activity. Drug Delivery 2005; 12: 385-392.
98. Bekerman T, et al. Cyclosporin nanoparticulate lipospheres for oral administration. J Pharm Sci 2004; 93: 1264-1270.
99. Sznitowska M, et al. Bioavailability of diazepam from aqueous-organic solution, submicron emulsion and solid lipid nanoparticles after rectal administration in rabbits. Eur J Pharm Biopharm 2001; 52: 159-163.
100. Friedrich I, et al. Drug release and permeation studies of nanosuspensions based on solidified reverse micellar solutions (SRMS). Int J Pharm 2005; 305: 167-175.
101. Castelli, et al. Characterization of indomethacin-loaded lipid nanoparticles by differential scanning calorimetry. Int J Pharm 2005; 304: 231-238.
102. Cavalli R, et al. Study by X-ray powder diffraction and differential scanning calorimetry to two model drugs, phenothiazine and nifedipine, incorporated into lipid nanoparticles. Eur J Pharm Biopharm 1995; 41: 329-333.
103. Mei Z, et al. The research on the anti-inflammatory activity and hepatotoxicity of triptolide-loaded solid lipid nanoparticles. Pharmacol Res 2005; 51: 345-351.