Dermal and ocular safety of the new phospholipase A2 inhibitors PX-18 and PX-13 formulated as drug nanosuspension.
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| Abstract |
PX-18 and PX-13 are new secreted phospholipase A2 inhibitors. An increased expression of secreted phospholipase A2 in psoriatic epidermis and dermis was reported in the literature, hence the dermal application of PX-18 and PX-13 seems to be a promising approach for psoriasis treatment. Both compounds are practically insoluble in aqueous media and hard to formulate using conventional techniques. Therefore, nanosuspensions were prepared by high pressure homogenization. Pre-clinical skin and eye irritation tests were performed with PX-18 and PX-13 bulk material and 5% (w/w) PX-18 and PX-13 nanosuspensions using the EPISKIN and the HET-CAM test to aid safety assessment and to facilitate the design of safe and efficient human studies. It could be shown that nanosuspensions with an active content of 5% (w/w) with a particle size well in the nanometer range can be produced applying high pressure homogenisation. The results of the EPISKIN test allow the classification of PX-18 and PX-13 bulk material and the according nanosuspensions as non irritant to the skin. According to the test protocol applied for the HET-CAM test, the bulk material of the new secreted phospholipase A2 inhibitors as well as the nanosuspensions can be classified as non/slightly irritant to the eye.
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| Authors | Jana Pardeike, Rainer H Müller |
| Journal | Journal of biomedical nanotechnology (J Biomed Nanotechnol) Vol. 5 Issue 4 Pg. 437-44 (Aug 2009) ISSN: 1550-7033 [Print] United States |
| PMID | 20055091 (Publication Type: Journal Article) |
| Chemical References |
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