title: In vitro-in vivo correlations of self-emulsifying drug delivery systems combining the dynamic lipolysis model and neuro-fuzzy networks.
abstract: The aim of the current study was to evaluate the potential of the dynamic lipolysis model to simulate the absorption of a poorly soluble model drug compound, probucol, from three lipid-based formulations and to predict the in vitro-in vivo correlation (IVIVC) using neuro-fuzzy networks. An oil solution and two self-micro and nano-emulsifying drug delivery systems were tested in the lipolysis model. The release of probucol to the aqueous (micellar) phase was monitored during the progress of lipolysis. These release profiles compared with plasma profiles obtained in a previous bioavailability study conducted in mini-pigs at the same conditions. The release rate and extent of release from the oil formulation were found to be significantly lower than from SMEDDS and SNEDDS. The rank order of probucol released (SMEDDS approximately SNEDDS > oil formulation) was similar to the rank order of bioavailability from the in vivo study. The employed neuro-fuzzy model (AFM-IVIVC) achieved significantly high prediction ability for different data formations (correlation greater than 0.91 and prediction error close to zero), without employing complex configurations. These preliminary results suggest that the dynamic lipolysis model combined with the AFM-IVIVC can be a useful tool in the prediction of the in vivo behavior of lipid-based formulations.
authors: Department of Pharmaceutics and Analytical Chemistry, University of Copenhagen, Copenhagen, Denmark. df@dfuni.dk
authors: Dimitrios G
authors: DG
authors: Fatouros
authors: Flemming Seier
authors: FS
authors: Nielsen
authors: Dionysios
authors: D
authors: Douroumis
authors: Leontios J
authors: LJ
authors: Hadjileontiadis
authors: Anette
authors: A
authors: Mullertz
mesh_terms: D000465:Algorithms; D000818:Animals; D000924:Anticholesteremic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001185:Artificial Intelligence; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004655:Emulsions; D005079:Excipients; D017143:Fuzzy Logic; D008049:Lipase / Q000737:chemistry; D008055:Lipids / Q000737:chemistry; D008066:Lipolysis; D008297:Male; D008823:Micelles; D015233:Models, Statistical; D016571:Neural Networks, Computer; D009821:Oils / Q000737:chemistry; D011341:Probucol / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D012972:Sodium Hydroxide / Q000737:chemistry; D013552:Swine
chemical_list: D000924:Anticholesteremic Agents; D004655:Emulsions; D005079:Excipients; D008055:Lipids; D008823:Micelles; D009821:Oils; D012972:Sodium Hydroxide; D008049:Lipase; D011341:Probucol