title: Lipid-based formulations solidified via adsorption onto the mesoporous carrier Neusilin® US2: effect of drug type and formulation composition on in vitro pharmaceutical performance.
abstract: The current study determined the extent to which the desorption of lipid-based formulations (LBFs) from a mesoporous magnesium aluminometasilicate (Neusilin®-US2) carrier is governed by drug properties, LBF composition, and LBF-to-adsorbent ratio. A secondary objective was to evaluate the impact of testing parameters (medium composition, pH, dilution, and agitation) on in vitro LBF performance. Two self-emulsifying LBFs, with high/low lipid-surfactant ratios were studied in detail using danazol, fenofibrate, cinnarizine, and mefenamic acid as model drugs. A wider range of 38 different danazol-containing LBF were also evaluated, where desorption was evaluated immediately after preparation and after 1 month of storage. The results revealed that incomplete desorption from Neusilin® was a feature of all drugs and LBFs tested. Desorption was insensitive to agitation but increased under conditions where ionizable drugs were charged. In addition, formulations containing a higher proportion (>30%) of hydrophilic surfactant consistently exhibited higher desorption, and were least susceptible to decreased desorption on storage. In summary, although Neusilin® is an effective vehicle for LBF solidification, its use is accompanied by a risk of incomplete desorption of the vehicle from the carrier, irrespective of the drug. Lipid Formulation Classification System (LFCS)Type IIIB LBFs comprising higher quantities of hydrophilic surfactants appear to desorb most from Neusilin®. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci.
authors.affiliation: Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
authors.forename: Hywel D
authors.initials: HD
authors.lastname: Williams
authors.forename: Michiel
authors.initials: M
authors.lastname: Van Speybroeck
authors.forename: Patrick
authors.initials: P
authors.lastname: Augustijns
authors.forename: Christopher J H
authors.initials: CJ
authors.lastname: Porter
mesh_terms: D000327:Adsorption; D017607:Aluminum Compounds / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers; D008055:Lipids / Q000737:chemistry*; D017616:Magnesium Compounds / Q000737:chemistry*; D017640:Silicates / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D017607:Aluminum Compounds; D004337:Drug Carriers; D008055:Lipids; D017616:Magnesium Compounds; D017640:Silicates; D013501:Surface-Active Agents; C033065:aluminum magnesium silicate
keywords: adsorbents; adsorption; lipid-based formulations; lipids; neusilin®; poorly water-soluble drugs; self-emulsifying; self-emulsifying drug delivery systems