Nano-amorphous spray dried powder to improve oral bioavailability of itraconazole

Poly(ε-benzyloxycarbonyl-L-lysine)-grafted branched polyethylenimine as efficient nanocarriers for indomethacin with enhanced oral bioavailability and anti-inflammatory efficacy

“…The oral bioavailability of drugs in amorphous formulations relative to its crystalline form can be enhanced as a result of the improved saturation solubility and dissolution rate [19,20]. In the present study, DSC thermograms of lyophilized nanoparticles from different initial feeding ratios (w:w) of IND to PEI-g-PZLL were scanned; the results are shown in Fig.…”

“…A combination of an amorphization approach with nanotechnology is highly desirable to enhance the oral bioavailability of drugs [20]. When PEI-g-PZLL star-block copolymers are utilized as nanocarriers for IND, the sub-100 nm particle size with increased interfacial surface area and the molecular or amorphous state of the encapsulated IND will enhance the dissolution rate and solubility of poorly water-soluble drugs and thus, their oral bioavailability.…”

Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

“…Spray-drying can induce polymorphic changes or amorphization of the encapsulated drug and enhance its solubility and dissolution rate [85,114,125]. For example, Tran et al developed solid dispersion NPs to enhance the physicochemical properties and bioavailability of raloxifene (poorly water-soluble) using spray-drying [114].…”

Bioavailability enhancement of itraconazole-based solid dispersions produced by hot melt extrusion in the framework of the Three Rs rule

“…Regarding the in vivo testing of ITZ-based formulations on vertebrates, the most common animals used are rabbits (Sun Dong et al, 2000), rats (Hassan et al, 2007;Sun Dong et al, 2000;Van Eerdenbrugh et al, 2009;Sarnes et al, 2014;Zhang et al, 2013;DiNunzio et al, 2008;Mou et al, 2011;Miller et al, 2007;Kumar et al, 2015;Kumar et al, 2014) and dogs (Engers et al, 2010;Linn et al, 2012;Zhong et al, 2016). In all these studies, the Three Rs rule was not really taken into account since a lot of blood was retrieved from the animals and often in an uncomfortable way (frontal or jugular vein).…”