RESEARCH PAPER Nanocomposite Formulation System of Lipid-Regulating Drugs Based on Layered Double Hydroxide: Synthesis, Characterization and Drug Release Properties Mohamed R. Berber & Inas H. Hafez & Keiji Minagawa & Takeshi Mori & Masami Tanaka Received: 1 April 2010 / Accepted: 17 May 2010 # Springer Science+Business Media, LLC 2010 ABSTRACT Purpose To design a nanocomposite formulation system of lipid-regulating drugs with versatile approaches using layered double hydroxide (LDH) material. Methods The co-precipitation technique has been used to prepare the selected drugs [bezafibrate (BZF) and clofibric acid (CF)]-LDH nanocomposites. The nanocomposite materials (BZF-LDH and CF-LDH) were characterized by X-ray powder diffraction, infrared spectroscopy, thermogra- vimetric analysis, and scanning electron microscopy. The in vitro study was investigated in simulated gastrointestinal solutions at 36.8°C. Results X-ray measurement and spectroscopic analysis indi- cated the formation of fully monophase drug-nanocomposites. The nanocomposites’ gallery heights were calculated to be 23.5 and 16.3Å for BZF and CF, respectively. The new gallery heights indicated that BZF and CF drugs have been stacked into LDH as a monolayer with a staggered inter-digitated arrangement. The size of the nanocomposites described by SEM microscopy was ∼ 0.1 μm. The nanocomposite formula- tion has improved the drugs properties (thermal stability, dissolution, and controlled release) beside the achievement of drug target delivery. Conclusions Nanocomposites composed of lipid-regulating drugs (BZF and CF) with LDH were successfully synthesized as a new formulation system of this drug category. The LDH nanocomposite formulation system has improved the drugs release properties. KEY WORDS fibrates . LDH . nanocomposites . formulations . controlled delivery INTRODUCTION Coronary heart disease is associated with the elevation of serum lipid concentrations (cholesterol and triglycerides) resulting from smoking and some genetic disorders (1,2). In such disease cases, to reach the normal blood lipid target ratios, treatment with hypolipidemic drugs is required. Fibrates such as bezafibrate (BZF) and clofibric acid (CF) are a class of lipid-regulating drugs that have been used in the therapy in many forms of hyperlipoproteinemia (3). BZF (2-[4-(2-[4-chlorobenzamindo] ethyl)-phenoxy]-2- methyl-propanoic acid) is a well-known antihyperlipidaemic agent that lowers elevated blood serum lipid concentrations (cholesterol and triglycerides) (4). CF [2-(4-Chloro phe- noxy)-2-methylpropanoic acid] is the active metabolite of the blood lipid regulator colfibrate. It lowers elevated serum lipids by reducing the very low-density lipopro- tein fraction that is rich in triglycerides (5). Usually fibrates are administrated orally. Their maximal adsorp- tions mainly take place in the duodenum and the small intestine of the gastrointestinal tract (6). However, fibrates M. R. Berber : I. H. Hafez : K. Minagawa Institute of Technology and Science, The University of Tokushima Tokushima 770-8506, Japan T. Mori Department of Applied Chemistry, Kyushu University Fukuoka 819-0395, Japan M. Tanaka Faculty of Pharmaceutical Sciences, Tokushima Bunri University Tokushima 770-8514, Japan M. R. Berber (*) : K. Minagawa (*) Department of Chemical Science, and Technology, Institute of Technology and Science, The University of Tokushima, Tokushima 770-8506, Japan e-mail: mrberber@sy34.chem.tokushima-u.ac.jp e-mail: minagawa@chem.tokushima-u.ac.jp DOI 10.1007/s11095-010-0175-x Pharm Res (2010) 27:2394–2401 / Published online: 29 May 2010