In vitro assessment of drug-free and fenofibrate-containing lipid formulations using dispersion and digestion testing gives detailed insights into the likely fate of formulations in the intestine

Optimization of a PGSS (particles from gas saturated solutions) process for a fenofibrate lipid-based solid dispersion formulation

“…Given that this type of lipid excipient is subject to digestion in vivo and that this physiological process may have an impact on the performance of the drug delivery system, these lipid-based formulations are, in most cases, evaluated by an in vitro digestion method (Devraj et al, 2013). However, it appears that this in vitro lipolysis test does not adequately predict the in vivo performance of lipid-based drug delivery systems containing fenofibrate (Griffin et al, 2014;Thomas et al, 2014).…”

“…Indeed, we can maintain sink conditions in octanol phase with a low volume of organic solvent. Finally, fenofibrate is soluble in supercritical CO 2 (Chen et al, 2010) and this API is often used in the literature as a model molecule for all processes involving the use of supercritical CO 2 (Dalvi et al, 2013;Hiendrawan et al, 2014;Sanganwar and Gupta, 2008) and for processes that attempt to increase the aqueous solubility of a compound by self-emulsification in a lipid-based formulation (Bahloul et al, 2014;Devraj et al, 2013;Griffin et al, 2014;Mu et al, 2013) or by any other techniques (Dong et al, 2014;Kalivoda et al, 2012;Niu et al, 2013).…”

Environment-responsive aza-BODIPY dyes quenching in water as potential probes to visualize the in vivo fate of lipid-based nanocarriers

“…The particle size was measured by Zetasizer Nano ® (Malvern Instruments, Malvem, UK) equipped with a 4-mW He-Ne laser (633 nm) at 25C.The entrapment efficiency( EE% ) was measured using ultrafiltration cells (Amicon ® Ultra-0.5, USA). The morphology of the SLNs was observed using a transmission electron microscope (TEM) (JEM-1230 Electron microscope, JEOL, Japan).In vitro lipolysis study of SLNs was performed according to a reported method with modifications in three digestive media of different bile salts and phospholipid content 28,29. The media were composed of pH 7.5 buffer (50 mM Tris-maleate, 150 mM NaCl, 5 mM CaCl 2 ) and STC/lecithin in the ratios of 6.25 mM / 1.563 mM, 25 mM / 6.25 mM and 0 mM / 0 mM for medium A, B and C, respectively.…”

Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug

“…6,7 Fenofibrate is a lipid-regulating agent that has chemical, pharmacological, and clinical similarities to the other fibrate drugs, such as clofibrate and gemfibrozil. 8 The chemical structure of fenofibrate is shown in Figure 1. Fenofibrate is a BCS Class II drug with various available doses (45 mg, 54 mg, 100 mg, 145 mg, 160 mg, and 200 mg).…”