In-vitro permeability screening of melt extrudate formulations containing poorly water-soluble drug compounds using the phospholipid vesicle-based barrier

Journal of Pharmacy and Pharmacology

Volumn 62, Issue 11, 2010, Pages 1591-1598

  Kanzer, Johanna ^a,b   Tho, Ingunn ^a   Flaten, Gøril Eide ^a   Hölig, Peter ^c   Fricker, Gert ^b   Brandl, Martin ^a,d  

^a UNIVERSITY OF TROMSØ   (Norway)

^b UNIVERSITY OF HEIDELBERG   (Germany)

^c ABBOTT GMBH AND CO KG   (Germany)

^d UNIVERSITY OF SOUTHERN DENMARK   (Denmark)

Author keywords

artificial membrane; melt extrudate; permeability; poorly water soluble drug; surfactant

Indexed keywords

1 VINYL 2 PYRROLIDINONE; ANTIRETROVIRUS AGENT; CALCEIN; CALCIUM ION; EXCIPIENT; MAGNESIUM ION; PHOSPHOLIPID; PLACEBO; POLYMER; SODIUM CHLORIDE; SURFACTANT; VINYL ACETATE; WATER;

ANIMAL CELL; ARTICLE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; DIFFUSION; DISPERSION; DRUG FORMULATION; DRUG SOLUBILITY; ELECTRIC RESISTANCE; HYDROGENATION; HYDROPHILICITY; ION TRANSPORT; MELTING POINT; METHODOLOGY; NONHUMAN; OSMOLARITY; PERMEABILITY; PHOSPHOLIPID VESICLE; SCREENING; SOLID;

CACO-2 CELLS; CALCIUM; CASTOR OIL; CHEMISTRY, PHARMACEUTICAL; DIFFUSION; DOSAGE FORMS; ELECTRIC IMPEDANCE; EXCIPIENTS; FLUORESCEINS; FREEZING; HUMANS; HYDROPHOBIC AND HYDROPHILIC INTERACTIONS; MAGNESIUM; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; PHOSPHOLIPIDS; SOLUBILITY; SURFACE-ACTIVE AGENTS; WATER;

EID: 78649666113     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.2042-7158.2010.01172.x     Document Type: Article

References (37)

1. Hidalgo IJ, et al. Characterization of the human-colon carcinoma cell-line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 1989; 96: 736-749.
2. Artursson P, Karlsson J,. Correlation between oral-drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Commun 1991; 175: 880-885.
3. Cho MJ, et al. The Madin Darby canine kidney (Mdck) epithelial-cell monolayer as a model cellular-transport barrier. Pharm Res 1989; 6: 71-77.
4. Kansy M, et al. Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. J Med Chem 1998; 41: 1007-1010.
5. Pidgeon C, et al. IAM chromatography-an in-vitro screen for predicting drug membrane-permeability. J Med Chem 1995; 38: 590-594.
6. Flaten GE, et al. Drug permeability across a phospholipid vesicle based barrier: a novel approach for studying passive diffusion. Eur J Pharm Sci 2006; 27: 80-90.
7. Flaten GE, et al. Drug permeability across a phospholipid vesicle based barrier: 3. Characterization of drug-membrane interactions and the effect of agitation on the barrier integrity and on the permeability. Eur J Pharm Sci 2007; 30: 324-332.
8. Flaten GE, et al. Drug permeability across a phospholipid vesicle-based barrier-2. Characterization of barrier structure, storage stability and stability towards pH changes. Eur J Pharm Sci 2006; 28: 336-343.
9. Lipinski CA, et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 1997; 23: 3-25.
10. Rasenack N, Muller BW,. Micron-size drug particles: common and novel micronization techniques. Pharm Dev Technol 2004; 9: 1-13.
11. Pouton CW,. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur J Pharm Sci 2000; 11: S93-S98.
12. Leuner C, Dressman J,. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm 2000; 50: 47-60.
13. Breitenbach J,. Melt extrusion: from process to drug delivery technology. Eur J Pharm Biopharm 2002; 54: 107-117.
14. Chiou WL, Riegelman S,. Pharmaceutical applications of solid dispersion systems. J Pharm Sci 1971; 60: 1281-1302.
15. Serajuddin ATM, et al. Effect of vehicle amphiphilicity on the dissolution and bioavailability of a poorly water-soluble drug from solid dispersions. J Pharm Sci 1988; 77: 414-417.
16. Ghebremeskel AN, et al. Use of surfactants as plasticizers in preparing solid dispersions of poorly soluble API: selection of polymer-surfactant combinations using solubility parameters and testing the processability. Int J Pharm 2007; 328: 119-129.
17. Tho I, et al. Formation of nano/micro dispersions with improved dissolution properties upon dispersion of ritonavir melt extrudate in aqueous media. Eur J Pharm Sci 2010; 40: 25-32.
18. Kanzer J, et al. In situ formation of nanoparticles upon dispersion of melt extrudate formulations in aqueous medium assessed by asymmetrical flow field-flow fractionation. J Pharm Biomed Anal 2010; 53: 359-365.
19. Iglicar P, et al. Permeability of a novel beta-lactamase inhibitor LK-157 and its ester prodrugs across rat jejunum in vitro. J Pharm Pharmacol 2009; 61: 1211-1218.
20. Tonsberg H, et al. Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats. J Pharm Pharmacol 2010; 62: 63-70.
21. Barakat NS,. Self-emulsifying system for improving drug dissolution and bioavailability: in vitro/in vivo evaluation. Drug Dev Res 2010; 71: 149-158.
22. Anderberg EK, et al. Epithelial transport of drugs in cell-culture. 7. Effects of pharmaceutical surfactant excipients and bile-acids on transepithelial permeability in monolayers of human intestinal epithelial (Caco-2) cells. J Pharm Sci 1992; 81: 879-887.
23. Sakai M, et al. Cytotoxicity of absorption enhancers in Caco-2 cell monolayers. J Pharm Pharmacol 1998; 50: 1101-1108.
24. Flaten GE, et al. Drug permeability across a phospholipid vesicle-based barrier: 4. The effect of tensides, co-solvents and pH changes on barrier integrity and on drug permeability. Eur J Pharm Sci 2008; 34: 173-180.
25. New RRC. Preparation of liposomes. In: New RRC, ed. Liposomes-A Practical Approach. New York: Oxford University Press, 1990: 33-67.
26. Flaten GE, et al. The phospholipid vesicle-based drug permeability assay: 5. Development toward an automated procedure for high-throughput permeability screening. J Assoc Lab Autom 2009; 14: 12-21.
27. Krueger P, et al. Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2. Eur J Pharm Sci 2009; 36: 275-284.
28. Hara M, et al. Interaction between a novel amphiphilic polymer and liposomes. Supramol Sci 1998; 5: 777-781.
29. Kuhl T, et al. Direct measurement of polyethylene glycol induced depletion attraction between lipid bilayers. Langmuir 1996; 12: 3003-3014.
30. Thomas JL, Tirrell DA,. Polymer-induced leakage of cations from dioleoyl phosphatidylcholine and phosphatidylglycerol liposomes. J Control Release 2000; 67: 203-209.
31. Sagrista ML, et al. Surface modified liposomes by coating with charged hydrophilic molecules. Cell Mol Biol Lett 2000; 5: 19-33.
32. Zhang L, et al. Destabilization of liposomes by uncharged hydrophilic and amphiphilic polymers. J Phys Chem B 2004; 108: 7763-7770.
33. Avdeef A,. Permeability. In:, Avdeef A, ed. Absorption and Drug Development: Solubility, Permeability, and Charge State. Hoboken, NJ: John Wiley & Sons, Inc, 2003: 116-246.
34. Hunter J, et al. Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells-kinetics of vinblastine secretion and interaction with modulators. J Biol Chem 1993; 268: 14991-14997.
35. Lee CGL, et al. HIV-1 protease inhibitors are substrates for the MDR1 multidrug transporter. Biochemistry 1998; 37: 3594-3601.
36. Perloff ES, et al. Atazanavir: effects on P-glycoprotein transport and CYP3A metabolism in vitro. Drug Metab Dispos 2005; 33: 764-770.
37. Storch CH, et al. Comparison of the inhibitory activity of anti-HIV drugs on P-glycoprotein. Biochem Pharmacol 2007; 73: 1573-1581.