Dermal and ocular safety of the new phospholipase A2 inhibitors PX-18 and PX-13 formulated as drug nanosuspension

Journal of Biomedical Nanotechnology

Volumn 5, Issue 4, 2009, Pages 437-444

  Pardeike, Jana ^a   Müller, Rainer H ^a  

^a FREIE UNIVERSITÄT BERLIN   (Germany)

Author keywords

EPISKIN test; HET CAM test; Nanocrystals; Nanosuspension; Phospholipase A2 inhibitors; PX 13; PX 18

Indexed keywords

ACTIVE CONTENT; AQUEOUS MEDIA; BULK MATERIALS; CONVENTIONAL TECHNIQUES; EPISKIN TEST; HIGH PRESSURE; HIGH PRESSURE HOMOGENIZATION; HOMOGENISATION; HUMAN STUDY; NANO METER RANGE; NANO-SUSPENSIONS; NANOSUSPENSION; NON-IRRITANT; PHOSPHOLIPASE A; PRE-CLINICAL; SAFETY ASSESSMENTS; TEST PROTOCOLS;

ASSOCIATIVE STORAGE; CAMS; HALL EFFECT DEVICES; MATERIALS HANDLING EQUIPMENT; NANOCRYSTALS; RADIO TELESCOPES; SKIN;

TESTING;

PHOSPHOLIPASE A2 INHIBITOR; PX 13; PX 18; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL REACTION; CONTROLLED STUDY; DRUG DETERMINATION; DRUG SAFETY; DRUG SYNTHESIS; EYE IRRITATION; HUMAN; HUMAN TISSUE; NONHUMAN; PARTICLE SIZE; SKIN IRRITATION; SUSPENSION; TOXICITY TESTING; WATER CONTENT;

ALKANESULFONATES; ALKANESULFONIC ACIDS; ANIMALS; BLOOD PROTEINS; CHICKENS; DRUG CARRIERS; EYE; HUMANS; NANOPARTICLES; OLEIC ACIDS; SKIN; SUSPENSIONS;

EID: 70450202087     PISSN: 15507033     EISSN: 15507041     Source Type: Journal    
DOI: 10.1166/jbn.2009.1054     Document Type: Article

References (48)

1. R. C. Franson and R. M. Ottenbrite, Cytoprotective compounds, USA, 632030 (1996), April.
2. R. C. Franson and R. M. Ottenbrite, Cytoprotective fatty moiety compounds, USA, 819313 (1997), March.
3. R. C. Franson and R. M. Ottenbrite, Cytoprotective compounds, USA, 017511 (1998), February.
4. R. C. Franson and R. M. Ottenbrite, Cytoprotective compounds, USA, 481824 (2000), January.
5. R. C. Franson and R. M. Ottenbrite, Cytoprotective compounds, USA, 043641 (2002), January.
6. A. Menter, A. Gottlieb, S. R. Feldman, A. S. Van Voorhees, C. L. Leonardi, K. B. Gordon, M. Lebwohl, J. Y. Koo, C. A. Elmets, N. J. Korman, K. R. Beutner, and R. Bhushan, Guidelines of care for the management of psoriasis and psoriatic arthritis: Section 1 overview of psoriasis and guidelines of care for the treatment of psoriasis with biologics. J. Am. Acad. Dermatol. 58, 826 (2008).
7. 2. Basic and Clinical Aspects in Inflammatory Diseases, edited by W. Uhl, T. J. Nevalainen and M. W. Büchler, Prog Surg. Basel, Karger (1997), Vol.24, p. 225.
8. K. Ikai, Psoriasis and the arachidonic acid cascade. J. Dermatol. Sci. 21, 135 (1999).
9. S. Andersen, W. Sjursen, A. Laegreid, G. Volden, and B. Johansen, Elevated expression of human nonpancreatic phospholipase A2 in psoriatic tissue. Inflammation 18, 1 (1994).
10. U. Haas, M. Podda, M. Behne, S. Gurrieri, A. Alonso, G. Furstenberger, J. Pfeilschifter, G. Lambeau, M. H. Gelb, and M. Kaszkin, Characterization and differentiation-dependent regulation of secreted phospholipases A in human keratinocytes and in healthy and psoriatic human skin. J. Invest. Dermatol. 124, 204 (2005).
11. K. E. Rys-Sikora, R. L. Konger, J. W. Schoggins, R. Malaviya, and A. P. Pentland, Coordinate expression of secretory phospholipase A(2) and cyclooxygenase-2 in activated human keratinocytes. Am. J. Physiol. Cell Physiol. 278, C822 (2000).
12. D. S. Grass, R. H. Felkner, M. Y. Chiang, R. E. Wallace, T. J. Nevalainen, C. F. Bennett, and M. E. Swanson, Expression of human group II PLA2 in transgenic mice results in epidermal hyperplasia in the absence of inflammatory infiltrate. J. Clin. Invest. 97, 2233 (1996).
13. W. Sjursen, O. L. Brekke, and B. Johansen, Secretory and cytosoHc phospholipase A(2) regulate the long-term cytokine-induced eicosanoid production in human keratinocytes. Cytokine 12, 1189 (2000).
14. J. Pardeike, Nanosuspensions and Nanostructured Lipid Carriers for Dermal Application, Freie Universität Berlin, Berlin (2008).
15. R. H. Müller and A. Akkar, Drug nanocrystals of poorly solible drugs. Encyclopedia Nanoscience Nanotechnology 2, 627 (2004).
16. C. M. Keck and R. H. Müller, Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation. Eur. J. Pharm. Biopharm. 62, 3 (2006).
17. R. H. Müller, R. D. Petersen, A. Hommoss, and J. Pardeike, Nanostructured lipid carriers (NLC) in cosmetic dermal products. Adv. Drug Deliv. Rev. 59, 522 (2007).
18. J. H. Draize, G. Woodward, and H. O. Calvery, Method for the study of irritation and toxicity of substances applied topically to the skin and mucous membranes. J. Pharm. Exp. Therap. 82, 377 (1944).
19. M. P. Vinardell and M. Mitjans, Alternative methods for eye and skin irritation tests: An overview. J. Pharm. Sci. 97, 46 (2006).
20. European Commission's European Centre for the Validation of Alternative Methods (ECVAM), Performance Standards for Applying Human Skin Models to in vitro Skin Irritation Testing (2007), pp. 1-13.
21. T. Hartung, Statement on the Validation of in-vitro Tests for Skin Irritation, European Commission's European Centre for the Validation of Alternative Methods (ECVAM), Ispra (2007), pp. 1-7.
22. W. Steiling, The Hen's Egg Test on the Chorioallantoic Membrane (HET-CAM) INCITTOX no 96, European Commission's European Centre for the Validation of Alternative Methods (ECVAM) DB-ALM (1994), p. 18.
23. M. Balls, N. Berg, L. H. Bruner, R. Curren, O. de Suva, K. E. Earl, D. J. Esdaile, J. H. Fentem, M. Liebsch, Y. Ohno, M. K. Prinsen, S. H. and A. P. Worth, Eye irritation testing: The way forward - The report and recommendation of the European Commission's European Centre for the Validation of Alternative Methods (ECVAM) Workshop 34, ATLA (1999), Vol.27, pp. 53-77.
24. R. H. Müller and R. Schuhmann, Teilchengrößenmessung in der Laborpraxis, edited by R. H. Müller, APV Paperback, Wissenschaftliche Verlagsgesellschaft mbH Stuttgart (1996).
25. R. Roguet, J. Cotovio, J. Fentem, P. Jones, and C. Robles, Validation of the EPISKIN irritation test 42 houres assay for the prediction of acute skin irritation of chemicals, European Commission's European Centre for the Validation of Alternative Methods (ECVAM) Skin Irritation Validation Study, L'ORÉAL Publications (2005), pp. 1-41.
26. N. Hernandez-Kirstein, Development and characterisation of buparvaquone nanosuspensions for pulmonary delivery in the treatment of Pneumocystis pneumonia, Ph.D. Thesis, Biology, Chemistry and Pharmacy, Free University of Berlin, Berlin (2006).
27. J. Möschwitzer, Drug nanocrystals preparation by high pressure homogenization - The universal formulation approach for poorly soluble drugs, Ph.D. Thesis, Biology, Chemistry and Pharmacy, Freie Universität Berlin, Berlin (2005).
28. E. Tinois, J. Tiollier, M. Gaucherand, H. Dumas, M. Tardy, and J. Thivolet, In vitro and post-transplantation differentiation of human keratinocytes grown on the human type IV collagen film of a bilayered dermal substitute. Exp. Cell Res. 193, 310 (1991).
29. M. Liebsch, D. Traube, and H. Kandarova, In vitro skin Irritation test: human skin model, BfR (2004), pp. 1-31.
30. F. Focher and S. Spadari, Thymidine Phosphorylase: A two-face Janus in anticancer chemotherapy. Curr. Cancer Drug Targets 1, 141 (2001).
31. A. Richardz, Ein neues Target zur Therapie von Basaliom und spinozellulärem Karzinom - Inhibition der humanen DNA Polymerase alpha, Ph.D. Thesis, Biology, Chemistry and Pharmacy, Freie Universität Berlin, Berlin (2007).
32. M. A. Perkins, R. Osborne, F. R. Rana, A. Ghassemi, and M. K. Robinson, Comparison of in vitro and in vivo human skin responses to consumer products and ingredients with a range of irritancy potential. Toxicol. Sci. 48, 218 (1999).
33. R. Roguet, M. Régnier, C. Cohen, K. G. Dossou, and A. Rougier, The use of in vitro reconstructed human skin in dermatoxicity testing. Toxicol. In Vitro 8, 635 (1994).
34. T. Weiss, D. A. Basketter, and K. R. Schroder, In vitro skin irritation: Facts and future. State of the art review of mechanisms and models. Toxicol. In Vitro 18, 231 (2004).
35. T. Watanabe, T. Hasegawa, H. Takahashi, T. Ishibashi, H. Itagaki, and K. Sugibayashi, Utility of MTT assay in three-dimensional cultured human skin model as an alternative for draize skin irritation test: Approach using diffusion law of irritant in skin and toxicokinetics-toxicodynamics correlation. Pharm. Res. 19, 669 (2002).
36. K. Sugibayashi, T. Watanabe, T. Hasegawa, H. Takahashi, and T. Ishibashi, Kinetic analysis on the in vitro cytotoxicity using living skin equivalent for ranking the toxic potential of dermal irritants. Toxicol. In Vitro 16, 759 (2002).
37. R. Roguet, C. Cohen, C. Robles, P. Couretellemont, M. Tolle, J. P. Guillot, and X. Pouradier Duteil, An interlaboratory study of the reproducibility and relevance of Episkin, a reconstructed human epidermis, in the assesment of cosmetic irritancy. Toxicol. In Vitro 12, 295 (1997).
38. C. Faller, M. Bracher, N. Dami, and R. Roguet, Predictive ability of reconstructed human epidermis equivalents for the assessment of skin irritation of cosmetics. Toxicol. In Vitro 16, 557 (2002).
39. A. Chatterjee, R. J. Babu, M. Klausner, and M. Singh, In vitro and in vivo comparison of dermal irritancy of jet fuel exposure using EpiDerm (EPI-200) cultured human skin and hairless rats. Toxicol. Lett. 167, 85 (2006).
40. C. S. Weil and R. A. Scala, Study of intra- and interlaboratory variability in the results of rabbit eye and skin irritation tests. Toxicol. Appl Pharmacol. 19, 276 (1971).
41. D. A. Basketter, M. Chamberlain, H. A. Griffiths, M. Rowson, E. Whittle, and M. York, The classification of skin irritants by human patch test. Food Chem. Toxicol. 35, 845 (1997).
42. N. P. Luepke, Hen's egg chorioallantoic membrane test for irritation potential. Food Chem. Toxicol. 23, 287 (1985).
43. H. Spielmann and M. Liebsch, HET-CAM Test - Test protocol used in phase II of the German validation study for replacement of the Draize eye test (1990-1992), Federal Health Office (BGA), Centre for Documentation and Evaluation of Alternatives to Animal Experiments (ZEBET) (1991), pp. 1-8.
44. P. Budai and L. Varnagy, In vitro ocular irritation toxicity study of some pesticides. Acta Vet. Hung 48, 221 (2000).
45. J. P. Hagino, S. Kinoshita, N. Tani, T. Nakumara, N. Ono, K. Konishi, H. Iimuara, H. Kojima, and Y. Ohno, Interlaboratory validation of in vitro eye irritation tests for cosmetic ingredients (2) Chorioallantoic membrane (CAM) test. Toxicol. In Vitro 13, 99 (1999).
46. L. Gilleron, S. Coecke, M. Sysmans, E. Hansen, S. van Oproy, D. Marzin, H. van Cauteren, and P. Vamparys, Evaluation of a modified HET-CAM assay as screening test for eye irritancy. Toxicol. In Vitro 10, 431 (1996).
47. M. P. Vinardell and M. Mitjans, The chorioallantonic membrane test as a model to predict the potential human eye irritation induced by commonly used laboratory solvents. Toxicol. In Vitro 20, 1066 (2006).
48. J. E. Dahl, Potential of dental adhesives to induce mucosal irritation evaluated by the HET-CAM method. Acta Odontol. Scand 1 (2007).