title: Nanostructured lipid carriers as delivery system for the phopholipase A2 inhibitors PX-18 and PX-13 for dermal application.
abstract: PX-18 and PX-13 are secretory phospholipase A2-IIA (sPLA2-IIA) inhibitors. An increased expression of sPLA2 in psoriatic skin has been reported. The selective inhibition of this enzyme is a new therapeutic approach. For dermal application PX-18 and PX-13 have been loaded to Nanostructured lipid carriers (NLC). The PX-18-loaded and PX-13-loaded NLC possessed an average particles size of about 250 nm, a narrow particle size distribution (PI < 0.2), a high entrapment efficiency as well as a good physical stability, as already indicated by their high zeta potential. Both NLC formulations have been incorporated into a hydroxyethyl cellulose gel and an o/w cream. In the gel and in the o/w cream PX-18-loaded and PX-13-loaded NLC showed a good physical stability. Neither aggregation nor dissolution of NLC took place.
authors.affiliation: Department of Pharmaceutical Technology, Biopharmaceutics and Nutricosmetics, Freie Universität Berlin, Germany. jana.pardeike@uni-graz.at
authors.forename: J
authors.initials: J
authors.lastname: Pardeike
authors.forename: C
authors.initials: C
authors.lastname: Schmidt
authors.forename: I
authors.initials: I
authors.lastname: Volz
authors.forename: R H
authors.initials: RH
authors.lastname: Müller
mesh_terms: D000287:Administration, Topical; D000476:Alkanesulfonates / Q000008:administration & dosage* / Q000737:chemistry; D017738:Alkanesulfonic Acids / Q000008:administration & dosage* / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000031:analogs & derivatives; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004563:Electrochemistry; D004655:Emulsions; D007834:Lasers; D008081:Liposomes / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D009829:Oleic Acids / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D064801:Phospholipase A2 Inhibitors; D017785:Photons; D012869:Skin Absorption; D013053:Spectrophotometry; D013816:Thermodynamics
chemical_list: C545517:2-(N,N-bis(oleoyloxyethyl)amino)-1-ethanesulfonic acid; D000476:Alkanesulfonates; D017738:Alkanesulfonic Acids; D004337:Drug Carriers; D004655:Emulsions; D008081:Liposomes; D009829:Oleic Acids; C105902:PX 13; D064801:Phospholipase A2 Inhibitors; D002482:Cellulose; C002283:hydroxyethylcellulose