In vitro and in vivo evaluation of a simple microemulsion formulation for propofol

International Journal of Pharmaceutics

Volumn 425, Issue 1-2, 2012, Pages 53-61

  Li, Guiling ^a   Fan, Yating ^b   Li, Xinru ^b   Wang, Xiaoning ^b   Li, Yanfang ^c   Liu, Yan ^b   Li, Mei ^a  

^a INSTITUTE OF MEDICINAL BIOTECHNOLOGY   (China)

^b PEKING UNIVERSITY HEALTH SCIENCE CENTER   (China)

^c PEKING UNIVERSITY THIRD HOSPITAL   (China)

Author keywords

Microemulsion; Pharmacological effect; Propofol; Safety

Indexed keywords

LIPID EMULSION; POLOXAMER; PROPOFOL; PROPYLENE GLYCOL; SODIUM CHLORIDE;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DILUTION; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG SAFETY; DRUG SOLUBILITY; DRUG STABILITY; FLOW KINETICS; IN VITRO STUDY; IN VIVO STUDY; LD 50; MALE; MICROEMULSION; NONHUMAN; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RAT; SINGLE DRUG DOSE;

ANESTHETICS, INTRAVENOUS; ANIMALS; DRUG DELIVERY SYSTEMS; DRUG STABILITY; ELECTRIC CONDUCTIVITY; EMULSIONS; ERYTHROCYTES; HEMOLYSIS; LETHAL DOSE 50; MALE; MICE; MOTOR ACTIVITY; POLOXAMER; PROPOFOL; PROPYLENE GLYCOL; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; SODIUM CHLORIDE; SOLUBILITY; SURFACE-ACTIVE AGENTS; VISCOSITY;

EID: 84862818337     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2012.01.011     Document Type: Article

References (77)

1. R. Aboofazeli, D. Barlow, and M.J. Lawrence Particle size analysis of concentrated phospholipid microemulsions II. Photon correlation spectroscopy AAPS PharmSci 2 2000 1 10
2. M.J. Akers Excipient-drug interactions in parenteral formulations J. Pharm. Sci. 91 2002 2283 2300 (Pubitemid 35231192)
3. M.T. Baker, and M. Naguib Propofol: the challenges of formulation Anesthesiology 103 2005 860 876 (Pubitemid 41415536)
4. S.N. Bennett, M.M. McNeil, L.A. Bland, M.J. Arduino, M.E. Villarino, D.M. Perrotta, D.R. Burwen, S.F. Welbel, D.A. Pegues, and L. Stroud Postoperative infections traced to contamination of an intravenous anesthetic, propofol N. Engl. J. Med. 333 1995 147 154
5. H.N. Bhargava, A. Narukar, and L.M. Lieb Using microemulsions for drug delivery Pharm. Technol. 11 1987 46 54
6. J. Bielawski Two types of haemolytic activity of detergents Biochim. Biophys. Acta (BBA): Gen. Subj. 1035 1990 214 217 (Pubitemid 20251751)
7. F. Caboi, G. Capuzzi, P. Baglioni, and M. Monduzzi Microstructure of Ca-AOT/water/decane w/o microemulsions J. Phys. Chem. B 101 1997 10205 10212 (Pubitemid 127587703)
8. J.Y. Chang, Y.K. Oh, H.G. Choi, Y.B. Kim, and C.K. Kim Rheological evaluation of thermosensitive and mucoadhesive vaginal gels in physiological conditions Int. J. Pharm. 241 2002 155 163 (Pubitemid 34667075)
9. H. Chung, T.W. Kim, M. Kwon, I.C. Kwon, and S.Y. Jeong Oil components modulate physical characteristics and function of the natural oil emulsions as drug or gene delivery system J. Control. Release 71 2001 339 350 (Pubitemid 32276053)
10. G. Copetti, M. Grassi, R. Lapasin, and S. Pricl Synergistic gelation of xanthan gum with locust bean gum: a rheological investigation Glycoconj. J. 14 1997 951 961 (Pubitemid 28040016)
11. L. Djordjevic, M. Primorac, M. Stupar, and D. Krajisnik Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug Int. J. Pharm. 271 2004 11 19 (Pubitemid 38210080)
12. D.F. Driscoll Lipid injectable emulsions: pharmacopeial and safety issues Pharm. Res. 23 2006 1959 1969
13. D.F. Driscoll, H.N. Bhargava, L. Li, R.H. Zaim, V.K. Babayan, and B.R. Bistrian Physicochemical stability of total nutrient admixtures Am. J. Health Syst. Pharm. 52 1995 623 634
14. D.F. Driscoll, P.R. Ling, A.P. Silvestri, and B.R. Bistrian Fine vs. coarse complete all-in-one admixture infusions over 96 hours in rats: fat globule size and hepatic function Clin. Nutr. 27 2008 889 894
15. H.-F. Eicke, W. Meier, and H. Hammerich Charge transport as suitable tool to study near-percolation phenomena Colloids Surf. A: Physicochem. Eng. Aspect 156 1999 249 256 (Pubitemid 29397633)
16. M. Fanun Formulation and characterization of microemulsions based on mixed nonionic surfactants and peppermint oil J. Colloid Interface Sci. 343 2010 496 503
17. A.G. Floyd Top ten considerations in the development of parenteral emulsions J. Pharm. Sci. Technol. Today 4 1999 134 143 (Pubitemid 29195746)
18. D. Forster, C. Washington, and S.S. Davis Toxicity of solubilized and colloidal amphotericin B formulations to human erythrocytes J. Pharm. Pharmacol. 40 1988 325 328
19. G. Gaucher, M.-H. Dufresne, V.P. Sant, N. Kang, D. Maysinger, and J.-C. Leroux Block copolymer micelles: preparation, characterization and application in drug delivery J. Control. Release 109 2005 169 188 (Pubitemid 41742123)
20. R.P. Geyer Parenteral nutrition Physiol. Rev. 40 1960 150 186
21. W.J. Gibbs, and T.M. Hagemann Purified poloxamer 188 for sickle cell vaso-occlusive crisis Ann. Pharmacother. 38 2004 320 324 (Pubitemid 38112248)
22. K.J. Hamawy, L.L. Moldawer, M. Georgieff, A.J. Valicenti, V.K. Babayan, B.R. Bistrian, and G.L. Blackburn The effect of lipid emulsions on reticuloendothelial system function in the injured animal JPEN 9 1985 559 565 (Pubitemid 15019118)
23. J.H. Han, S.S. Davis, and C. Washington Physical properties and stability of two emulsion formulations of propofol Int. J. Pharm. 215 2001 207 220 (Pubitemid 32206618)
24. H.O. Ho, C.C. Hsiao, and M.T. Sheu Preparation of microemulsions using polyglycerol fatty acid esters as surfactant for the delivery of protein drugs J. Pharm. Sci. 85 1996 138 143
25. T.P. Hoar, and J.H. Schulman Transparent water in oil dispersions: the oleopathic hydro-micelle Nature 152 1943 102 103
26. C.-F. Hung, C.-L. Fang, M.-H. Liao, and J.-Y. Fang The effect of oil components on the physicochemical properties and drug delivery of emulsions: Tocol emulsion versus lipid emulsion Int. J. Pharm. 335 2007 193 202 (Pubitemid 46505069)
27. L. Ilium, S.S. Davis, C.G. Wilson, N.W. Thomas, M. Frier, and J.G. Hardy Blood clearance and organ deposition of intravenously administered colloidal particles. The effects of particle size, nature and shape Int. J. Pharm. 12 1982 135 146 (Pubitemid 12037337)
28. L. Illum, and S.S. Davis The targeting of drugs parenterally by use of microspheres J. Parenter. Sci. Technol. 36 1982 242 248 (Pubitemid 13202991)
29. B. Isomaa, H. Hágerstrand, G. Paatero, and A.C. Engblom Permeability alterations and antihaemolysis induced by amphiphiles in human erythrocytes Biochim. Biophys. Acta (BBA): Biomembr. 860 1986 510 524 (Pubitemid 16027960)
30. G.L. Jensen, E.A. Mascioli, D.L. Seidner, N.W. Istfan, A.M. Domnitch, K. Selleck, V.K. Babayan, G.L. Blackburn, and B.R. Bistrian Parenteral infusion of long- and medium-chain triglycerides and reticuloendothelial system function in man JPEN 14 1990 467 471
31. M. Jumaa, P. Kleinebudde, and B.W. Müller Physicochemical properties and hemolytic effect of different lipid emulsion formulations using a mixture of emulsifiers Pharm. Acta Helv. 73 1999 293 301 (Pubitemid 29324994)
32. P. Kandadi, M.A. Syed, S. Goparaboina, and K. Veerabrahma Brain specific delivery of pegylated indinavir submicron lipid emulsions Eur. J. Pharm. Sci. 42 2011 423 432
33. M. Kanke, G.H. Simmons, D.L. Weiss, B.A. Bivins, and P.P. DeLuca Clearance of 141C3-labeled microspheres from blood and distribution in specific organs following intravenous and intraarterial administration in beagle dogs J. Pharm. Sci. 69 1980 755 762 (Pubitemid 11237850)
34. S. Kiepert Microemulsions and the potential pharmaceutical use Pharmazie 44 1989 433 444
35. K.M. Kim, B.M. Choi, S.W. Park, S.H. Lee, L.V. Christensen, J. Zhou, B.H. Yoo, H.W. Shin, K.S. Bae, S.E. Kern, S.H. Kang, and G.J. Noh Pharmacokinetics and pharmacodynamics of propofol microemulsion and lipid emulsion after an intravenous bolus and variable rate infusion Anesthesiology 106 2007 924 934 (Pubitemid 46684058)
36. J.E. Kipp The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs Int. J. Pharm. 284 2004 109 122 (Pubitemid 39349144)
37. G.S. Kwon Polymeric micelles for delivery of poorly water-soluble compounds Crit. Rev. Ther. Drug Carrier Syst. 20 2003 357 403 (Pubitemid 38129592)
38. A. Lada, L. Lang, and R. Zana Relation between electric percolation and rate constant for exchange of material between drop lets in water in oil microemulsions J. Phys. Chem. 93 1989 10 12
39. M.S. Langley, and R.C. Heel Propofol. A review of its pharmacodynamic and pharmacokinetic properties and use as an intravenous anaesthetic Drugs 35 1988 334 372
40. M.J. Lawrence, and G.D. Rees Microemulsion-based media as novel drug delivery systems Adv. Drug Deliv. Rev. 45 2000 89 121
41. E.H. Lee, S.H. Lee, D.Y. Park, K.H. Ki, E.K. Lee, D.H. Lee, and G.J. Noh Physicochemical properties, pharmacokinetics, and pharmacodynamics of a reformulated microemulsion propofol in rats Anesthesiology 109 2008 436 447
42. X.R. Li, Y.H. Zhang, Y.T. Fan, Y.X. Zhou, X.N. Wang, C. Fan, Y. Liu, and Q.Z. Zhang Preparation and evaluation of novel mixed micelles as nanocarriers for intravenous delivery of propofol Nanoscale Res. Lett. 6 2011 275
43. Y. Masaki, M. Tanaka, and T. Nishikawa Changes in propofol concentration in a propofol-lidocaine 9:1 volume mixture Anesth. Analg. 90 2000 989 992 (Pubitemid 30190814)
44. H. Mays Dynamics and energetics of droplet aggregation in percolating AOT water-in-oil microemulsions J. Phys. Chem. B 101 1997 10271 10280 (Pubitemid 127587712)
45. S.C. Miller, and B.R. Drabik Rheological properties of poloxamer vehicles Int. J. Pharm. 18 1984 269 276 (Pubitemid 14190777)
46. T.E. Morey, J.H. Modell, D. Shekhawat, T. Grand, D.O. Shah, N. Gravenstein, S.P. McGorray, and D.M. Dennis Preparation and anesthetic properties of propofol microemulsions in rats Anesthesiology 104 2006 1184 1190 (Pubitemid 43852951)
47. T.E. Morey, M. Varshney, J.A. Flint, C.N. Seubert, W.B. Smith, D.G. Bjoraker, D.O. Shah, and D.M. Dennis Activity of microemulsion-based nanoparticles at the human bio-nano interface: concentration-dependent effects on thrombosis and hemolysis in whole blood J. Nanoparticle Res. 6 2004 159 170
48. S.P. Moulik, and B.K. Paul Structure, dynamics and transport properties of microemulsions Adv. Colloid Interface Sci. 78 1998 99 195 (Pubitemid 128431057)
49. S.P. Moulik, and S. Ray Thermodynamics of clustering of droplets in water/AOT/heptane microemulsions Pure Appl. Chem. 66 1994 521 525
50. D.H. Owen, J.J. Peters, and D.F. Katz Rheological properties of contraceptive gels Contraception 62 2000 321 326 (Pubitemid 32182420)
51. J.W. Park, E.S. Park, S.C. Chi, H.Y. Kil, and K.H. Lee The effect of lidocaine on the globule size distribution of propofol emulsions Anesth. Analg. 97 2003 769 771 (Pubitemid 37046443)
52. J. Peyrelasse, and C. Boned Conductivity, dielectric relaxation, and viscosity of ternary microemulsions: the role of the experimental path and the point of view of percolation theory Phys. Rev. A 41 1990 938
53. R.J. Prankerd, and V.J. Stella The use of oil-in-water emulsions as a vehicle for parenteral drug administration J. Parenter. Sci. Technol. 44 1990 139 149 (Pubitemid 20184494)
54. F. Quirion, and S. St-Pierre Reduction of the in vitro hemolytic activity of soybean lecithin liposomes by treatment with a block copolymer Biophys. Chem. 40 1991 129 134
55. F. Ravenelle, S. Gori, D. Le Garrec, D. Lessard, L. Luo, D. Palusova, J.R. Sneyd, and D. Smith Novel lipid and preservative-free propofol formulation: properties and pharmacodynamics Pharm. Res. 25 2008 313 319
56. F. Ravenelle, P. Vachon, A.E. Rigby-Jones, J.R. Sneyd, D. Le Garrec, S. Gori, D. Lessard, and D.C. Smith Anaesthetic effects of propofol polymeric micelle: a novel water soluble propofol formulation Br. J. Anaesth. 101 2008 186 193 (Pubitemid 351989669)
57. K.W. Reed, and S.H. Yalkowsky Lysis of human red blood cells in the presence of various cosolvents J. Parenter. Sci. Technol. 39 1985 64 69
58. R.E. Riter, J.R. Kimmel, E.P. Undiks, and N.E. Levinger Novel reverse micelles partitioning nonaqueous polar solvents in a hydrocarbon continuous phase J. Phys. Chem. B 101 1997 8292 8297 (Pubitemid 127578488)
59. D.L. Seidner, E.A. Mascioli, N.W. Istfan, K.A. Porter, K. Selleck, G.L. Blackburn, and B.R. Bistrian Effects of long-chain triglyceride emulsions on reticuloendothelial system function in humans JPEN 13 1989 614 619 (Pubitemid 20005560)
60. M. Singh, and L.J. Ravin Parenteral emulsions as drug carrier system J. Parenter. Sci. Technol. 40 1986 34 41 (Pubitemid 16145512)
61. R.G. Strickley Parenteral formulations of small molecule therapeutics marketed in the United States (1999) - Part I J. Parenter. Sci. Technol. 53 1999 324 349 (Pubitemid 30100071)
62. R.G. Strickley Solubilizing excipients in oral and injectable formulations Pharm. Res. 21 2004 201 230 (Pubitemid 38221966)
63. V. Suratkar, and S. Mahapatra Solubilization site of organic perfume molecules in sodium dodecyl sulfate micelles: new insights from proton NMR studies J. Colloid Interface Sci. 225 2000 32 38 (Pubitemid 30246737)
64. S. Sweetana, and M.J. Akers Solubility principles and practices for parenteral drug dosage form development PDA J. Pharm. Sci. Technol. 50 1996 330 342 (Pubitemid 26392756)
65. C.H. Tan, and M.K. Onsiong Pain on injection of propofol Anaesthesia 53 1998 468 476 (Pubitemid 28223077)
66. K.A. Thompson, and D.B. Goodale The recent development of propofol (DIPRIVAN) Intensive Care Med. 26 2000 S400 S404
67. G. Trapani, A. Latrofa, M. Franco, A. Lopedota, E. Sanna, and G. Liso Inclusion complexation of propofol with 2-hydroxypropyl-beta-cyclodextrin. Physicochemical, nuclear magnetic resonance spectroscopic studies, and anesthetic properties in rat J. Pharm. Sci. 87 1998 514 518 trapani@ippo.uniba. it (Pubitemid 28175815)
68. I.C. Tung Rheological behavior of poloxamer 407 aqueous solutions during sol-gel and dehydration processes Int. J. Pharm. 107 1994 85 90
69. L. Uvray, and W.M. Gelbart The structure of microemulsions experiments in micelles membranes, microemulsions and monolayers J. Solid State Chem. 347 1994 121 126
70. M.P. Vinardell, and M.R. Infante The relationship between the chain length of non-ionic surfactants and their hemolytic action on human erythrocytes Comp. Biochem. Physiol. C: Pharmacol. Toxicol. Endocrinol. 124 1999 117 120 (Pubitemid 29474053)
71. D. Vollmer, J. Vollmer, and H.-F. Eicke Droplet cluster vs. bicontinuous structures in percolating water-in-oil microemulsions Europhys. Lett. 26 1984 389
72. Y.C. Wang, and R.R. Kowal Review of excipients and pH's for parenteral products used in the United States J. Parenter. Drug Assoc. 34 1980 452 462 (Pubitemid 11177107)
73. C. Washington The stability of intravenous fat emulsions in total parenteral nutrition mixtures Int. J. Pharm. 66 1990 1 21
74. C. Weingarten, N.S. Santos Magalhaes, A. Baszkin, S. Benita, and M. Seiller Interactions of a non-ionic ABA copolymer surfactant with phospholipid monolayers: possible relevance to emulsion stabilization Int. J. Pharm. 75 1991 171 179
75. www.cytrx.com, 2003 May 15. Flocor technical brochure. CytRx Corporation.
76. B.Y. Zaslavsky, N.N. Ossipov, V.S. Krivich, L.P. Baholdina, and S.V. Rogozhin Action of surface-active substances on biological membranes. II. Hemolytic activity of nonionic surfactants Biochim. Biophys. Acta (BBA): Biomembr. 507 1978 1 7 (Pubitemid 8263724)
77. Q. Zhang, X. Jiang, W. Jiang, W. Lu, L. Su, and Z. Shi Preparation of nimodipine-loaded microemulsion for intranasal delivery and evaluation on the targeting efficiency to the brain Int. J. Pharm. 275 2004 85 96 (Pubitemid 38481522)