title: Evaluation of the in vitro differential protein adsorption patterns of didanosine-loaded nanostructured lipid carriers (NLCs) for potential targeting to the brain.
abstract: The preferential in vitro adsorption of apolipoprotein E (Apo E) onto the surface of colloidal drug carriers may be used as a strategy to evaluate the in vivo potential for such systems to transport drugs to the brain. The aim of this research was to investigate the in vitro protein adsorption patterns of didanosine-loaded nanostructured lipid carriers (DDI-NLCs), using two-dimensional polyacrylamide gel electrophoresis (2-D PAGE), in order to establish the potential for NLCs to deliver DDI to the brain. NLC formulations were manufactured using high-pressure homogenization using a lipid matrix consisting of a mixture of Precirol(®) ATO 5 and Transcutol(®) HP. The 2-D PAGE analysis revealed that NLCs in formulations stabilized using Solutol(®) HS 15 alone or with a ternary surfactant system consisting of Solutol(®) HS 15, Tween(®) 80, and Lutrol(®) F68, preferentially adsorbed proteins, such as Apo E. Particles stabilized with Tween(®) 80 and Lutrol(®) F68 did not adsorb Apo E in these studies, which could be related to the relatively large particle size and hence small surface area observed for these NLCs. These findings have revealed that DDI-loaded NLCs may have the potential to deliver DDI to the brain in vivo and, in addition, to Tween(®) 80, which has already been shown to have the ability to facilitate the targeting of colloidal drug delivery systems to the brain. Solutol(®) HS 15-stabilized nanoparticles may also achieve a similar purpose.
authors.affiliation: Department of Pharmaceutics, Biopharmaceutics, NutriCosmetics, Freie Universität Berlin, Berlin, Germany.
authors.forename: Kasongo Wa
authors.initials: KW
authors.lastname: Kasongo
authors.forename: Mirko
authors.initials: M
authors.lastname: Jansch
authors.forename: Rainer H
authors.initials: RH
authors.lastname: Müller
authors.forename: Roderick B
authors.initials: RB
authors.lastname: Walker
mesh_terms: D000327:Adsorption; D019380:Anti-HIV Agents / Q000737:chemistry* / Q000378:metabolism; D001921:Brain / Q000378:metabolism*; D016049:Didanosine / Q000737:chemistry* / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism; D016503:Drug Delivery Systems; D015180:Electrophoresis, Gel, Two-Dimensional; D006801:Humans; D008055:Lipids; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D011506:Proteins / Q000737:chemistry*; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D019380:Anti-HIV Agents; D004337:Drug Carriers; D008055:Lipids; D011506:Proteins; D013501:Surface-Active Agents; D016049:Didanosine