Comparison of effects of different ointment bases on the penetration of ketoprofen through heat-separated human epidermis and artificial lipid barriers

Journal of Pharmaceutical Sciences

Volumn 92, Issue 7, 2003, Pages 1396-1406

  Jaeckle, Elke ^a   Schaefer, Ulrich F ^a   Loth, Helmut ^a  

^a SAARLAND UNIVERSITY   (Germany)

Author keywords

Artificial lipid mixtures; Heat separated epidermis; In vitro test; Interactions with topical vehicles; Ketoprofen; Permeability

Indexed keywords

CERAMIDE; CHOLESTEROL OLEATE; EDENOR C14; EDENOR C16; EDENOR C18; EDENOR SB 05; EDENOR TI 05; KETOPROFEN; LANOLIN ALCOHOL; LINOLEIC ACID; MYRISTIC ACID; OINTMENT BASE; OLEIC ACID; PALMITIC ACID; PALMITOLEIC ACID; PETROLATUM; STEARIC ACID; TRIACYLGLYCEROL; WITEPSOL; WITEPSOL H 5;

ARTICLE; CONTROLLED STUDY; DENSITY; DIFFUSION COEFFICIENT; DRUG PENETRATION; DRUG SOLUBILITY; EPIDERMIS; HEAT; HUMAN; HUMAN TISSUE; LIPID MEMBRANE; PARTITION COEFFICIENT; STEADY STATE; STRATUM CORNEUM; THICKNESS;

EID: 0038082964     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1002/jps.10398     Document Type: Article

References (48)

1. Asbill C, Kim N, El-Kattan A, Creek K, Wertz P, Michniak B. 2000. Evaluation of human bioengineered skin equivalent for drug permeation studies. Pharm Res 17:1092-1097.
2. Mak VHW, Cumpstone MB, Kennedy AH, Harmon CS, Guy RH, Potts RO. 1991. Barrier function of human keratinocyte cultures grown at the air-liquid interface. J Invest Dermatol 96:323-327.
3. Bouwstra JA, Gooris GS, Weerheim A, Kempenaar J, Ponec M. 1995. Characterization of stratum corneum structure in reconstructed epidermis by X-ray diffraction. J Lipid Res 36:496-504.
4. Monteiro-Riviere NA, Inman AO, Mak V, Wertz P, Riviere JE. 2001. Effect of selective lipid extraction from different body regions on epidermal barrier function. Pharm Res 18:992-998.
5. Schmook FP, Meingassner JG, Billich A. 2001. Comparison of human skin or epidermis models with human and animal skin in in vitro percutaneous absorption. Int J Pharm 215:51-56.
6. Abraham W, Downing DT. 1989. Preparation of model membranes for skin permeability studies using stratum corneum lipids. J Invest Dermatol 93:809-813.
7. Friberg SE, Kayali IH, Margosiak M, Osborne DW, Ward AJI. 1990. Stratum corneum structure and transport properties. In: Osborne DW, Amann AH, editors. Topical drug delivery formulations (Vol. 42 of the series Drugs and the Pharmaceutical Sciences). New York, Basel: Marcel Dekker, pp 29-45.
8. Kittayanond D, Dowton SM, Ramachandran C, Flynn GL, Weiner N. 1992. Development of a model of the lipid constituent phase of the stratum corneum: II. Preparation of artificial membranes from synthetic lipids and assessment of permeability properties using in vitro diffusion experiments. J Soc Cosmet Chem 43:237-249.
9. Lieckfeldt R, Villalain J, Gomez-Fernandes JC, Lee G. 1993. Diffusivity and structural polymorphism in some model stratum corneum lipid systems. Biochem Biophys Acta 1150:182-188.
10. Matsuzaki K, Imaoka T, Asano M, Miyajima K. 1993. Development of a model membrane system using stratum corneum lipids for estimation of drug skin permeability. Chem Pharm Bull 41:575-579.
11. Moghimi HR, Williams AC, Barry BW. 1996. A lamellar matrix for stratum corneum intercellular lipids. I. Characterization and comparison with stratum corneum intercellular structure. Int J Pharm 131:103-115.
12. Norlen L, Nicander I, Rozell BL, Ollmar S, Forslind B. 1999. Inter- and intra-individual differences in human stratum corneum lipid content related to physical parameters of skin barrier function in vivo. J Invest Dermatol 112:72-77.
13. Cornwell PA, Barry BW. 1995. Effects of penetration enhancer treatment on the statistical distribution of human skin permeabilities. Int J Pharm 117:101-112.
14. Williams AC, Cornwell PA, Barry BW. 1992. On the non-Gaussian distribution of human skin permeabilities. Int J Pharm 86:69-77.
15. Southwell D, Barry BW, Woodford R. 1984. Variations in permeability of human skin within and between specimens. Int J Pharm 18:299-309.
16. Bouwstra JA, Gooris GS, Bras W, Downing DT. 1995. Lipid organization in pig stratum corneum. J Lipid Res 36:685-695.
17. Winkler A, Müller-Goymann CC. 2002. Comparative permeation of δ-aminolevulinic acid and its n-butyl ester through stratum corneum and artificial skin constructs. Eur J Pharm Biopharm 53:281-287.
18. Ponec M, Weerheim A, Kempenaar J, Mommaas AM, Nugteren DM. 1988. Lipid composition of cultured human keratinocytes in relation to their differentiation. J Lipid Res 29:949-961.
19. Ponec M. 1991. Reconstruction of human epidermis: Expression of differentiation-specific protein markers and lipid composition. Toxicol In Vitro 5:597-606.
20. Potts RO, Guy RH. 1992. Predicting skin permeability. Pharm Res: 9:663-669.
21. Liversidge GG. 1981. Ketoprofen. In: Florey K, editor. Analytical profiles of drug substances, Vol. 10. New York: Academic Press, pp 443-471.
22. 3 Präparatevolumen. Z Angew Physik 4:273-276.
23. Loth H, Euschen A. 1990. Liquid-crystalline sidechain silastomers, largely modifiable diffusion media for the control of drug delivery. Drug Dev Ind Pharm 16:2077-2095.
24. Schaefer U, Loth H. 1996. An ex-vivo model for the study of drug penetration into human skin. Pharm Res 13(Suppl.):366.
25. Theobald F. 1998. In vitro Methoden zur biopharmazeutischen Qualitaetspruefung von Dermatika unter Beruecksichtigung der Lipidzusammensetzung des Stratum corneum. Doctoral Thesis, Saarbruecken, Germany.
26. Harrison SM, Barry BW, Dugard PH. 1984. Effects of freezing on human skin permeability. J Pharm Pharmacol 36:261-262.
27. Bronaugh RL, Stewart RF, Simon M. 1986. Methods for in vitro percutaneous absorption studies. VII. Use of excised human skin. J Pharm Sci 75:1094-1097.
28. Wester RC, Christoffel J, Hartway T, Poblete N, Maibach HI, Forsell J. 1998. Human cadaver skin viability for in vitro percutaneous absorption: Storage and detrimental effects of heat-separation and freezing. Pharm Res 15:82-84.
29. Kligman A, Christophers E. 1963. Preparation of isolated sheets of human stratum corneum. Arch Dermatol 88:702-705.
30. Wagner H, Kostka KH, Lehr CM, Schaefer UF. 2001. Interrelation of permeation and penetration parameters obtained from in vitro experiments with human skin and skin equivalents. J Controlled Release 75:283-295.
31. Elias PM. 1990. The importance of epidermal lipids for the stratum corneum barrier. In: Osborne DW, Amann AH, editors. Topical drug delivery formulations (Vol. 42 of the series Drugs and the Pharmaceutical Sciences). New York, Basel: Marcel Dekker, pp 13-28.
32. Watkinson AC, Brain KR, Walters KA. 1993. The penetration of ibuprofen through human skin in vitro: Vehicle, enhancer, and pH effects. In: Brain KR, James V, Walters KA, editors. Prediction of percutaneous penetration, Vol. 3B. Cardiff: STS Publishing, pp 335-341.
33. a and dermal delivery. Int J Pharm 200:243-247.
34. Hadgraft J, du Plessis J, Goosen C. 2000. The selection of non-steroidal anti-inflammatory agents for dermal delivery. Int J Pharm 207:31-37.
35. Cordero JA, Alarcon L, Escribano E, Obach R, Domenech J. 1997. A comparative study of the transdermal penetration of a series of nonsteroidal antiinflammatory drugs. J Pharm Sci 86:503-508.
36. Rehfeldt SJ, Williams ML, Elias PM. 1986. Interactions of cholesterol and cholesterol sulfate with free fatty acids: Possible relevance for the pathogenesis of recessive X-linked ichthyosis. Arch Dermatol Res 278:259-263.
37. Wertz PW. 1996. The nature of the epidermal barrier: Biochemical aspects. Adv Drug Delivery Rev 18:283-294.
38. Suhonen TM, Bouwstra JA, Urtti A. 1999. Chemical enhancement of percutaneous absorption in relation to stratum corneum structural alterations. J Controlled Release 59:149-161.
39. Parrott DT, Turner JE. 1993. Mesophase formation by ceramides and cholesterol: A model for stratum corneum lipid packing? Biochim Biophys Acta 1147:273-276.
40. Swartzendruber DC, Wertz PW, Kitko DJ, Madison KC, Downing DT. 1989. Molecular models of the intercellular lipid lamellae in mammalian stratum corneum. J Invest Dermatol 92:251-257.
41. Higuchi T. 1960. Physical chemical analysis of percutaneous absorption process from creams and ointments. J Soc Cosmet Chem 11:85-97.
42. Higuchi WI, Higuchi T. 1960. Theoretical analysis of diffusional movement through heterogeneous barriers. J Am Pharm Assoc 49:598-606.
43. Sherertz EF, Sloan KB, McTiernan RG. 1987. Effect of skin pretreatment with vehicle alone or drug in vehicle on flux of a subsequently applied drug: Results of hairless mouse skin and diffusion cell studies. J Invest Dermatol 89:249-252.
44. Wild T. 1988. Einfluß der physiko-chemischen Eigenschaften von Arzneistoffen und Vehikeln auf die Permeabilitaet der menschlichen Hornschicht. Doctoral Thesis, Saarland University, Saarbruecken, Germany.
45. Loth H. 1991. Vehicular influence on transdermal drug penetration. Int J Pharm 68:1-10.
46. Loth H, Hauck G, Borchert D, Theobald F. 2000. Statistical testing of drug accumulation in skin tissues by linear regression versus contents of stratum corneum lipids. Int J Pharm 209:95-108.
47. Santoyo S, Ygartua P. 2000. Effect of skin pretreatment with fatty acids on percutaneous absorption and skin retention of piroxicam after its topical application. Eur J Pharm Biopharm 50:145-250.
48. Clark EW. 1992. Short-term penetration of lanolin into human stratum corneum. J Soc Cosmet Chem 43:219-227.