Preparation and characterization of fenofibrate-loaded zeolitic imidazolate frameworks and their evaluation in dissolution enhancement of the formulation

Abstract

The purpose of this study was to develop zeolitic imidazolate frameworks (ZIFs) incorporated with poorly water-soluble drug fenofibrate (FEN), belonging to Biopharmaceutical Classification System (BCS) class II, to improve drug dissolution, intended to be orally administrated. FEN-loaded ZIF-8 were characterized with N2 adsorption-desorption analysis, fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD), and dynamic light scattering (DLS) with the results demonstrating the successful incorporation of FEN into the ZIF-based host. Different parameters including similarity factor (f2), difference factor (f1), dissolution efficiency (DE%) and mean dissolution time (MDT) were employed to analyze drug release tests, confirming a significant enhancement in the release profile of FEN with ZIF-8 as drug dissolution enhancer. Compared to enzyme-free simulated intestinal fluid (SIF), remarkable dissolution enhancement of FEN was observed in enzyme-free simulated gastric fluid (SGF) as drug release media. Fitting the experimental data from the release studies to different kinetic models showed the best fitting with Weibull, First order with Fmax and Korsmeyer-Peppas models.

Keywords

• fenofibrate
• dissolution rate
• poorly water-soluble drug
• zeolitic imidazolate frameworks
• zif-8