Dermal and Ocular Safety of the New Phospholipase A₂ Inhibitors PX-18 and PX-13 Formulated as Drug Nanosuspension

Authors: Pardeike, Jana; Müller, Rainer H.

Source: Journal of Biomedical Nanotechnology, Volume 5, Number 4, August 2009 , pp. 437-444(8)

Publisher: American Scientific Publishers

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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.

Keywords: NANOCRYSTALS; NANOSUSPENSION; PHOSPHOLIPASE A2 INHIBITORS; PX-18; PX-13; EPISKIN TEST; HET-CAM TEST

Document Type: Research article

DOI: http://dx.doi.org/10.1166/jbn.2009.1054

Publication date: 2009-08-01

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Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
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