In vitro and in vivo performance of monoacyl phospholipid-based self-emulsifying drug delivery systems

A dynamic in vitro permeation study on solid mono- and diacyl-phospholipid dispersions of celecoxib

“…there was no significant difference in CXB permeation between CXB SPDs of corresponding mono-or diacyl ratios). A lack of correlation between emulsion droplet size and fenofibrate in vivo bioavailability has previously been found for monoacyl PC containing self-nanoemulsifying drug delivery systems (Tran et al, 2017, Park, 2017. Our data suggest that up to a certain threshold, the presence of colloidal assemblies, assumptively…”

“…Page 3 of 19 monoacyl-and diacyl-phospholipids would have a different influence on the SPDs´ biopharmaceutical performance, specifically on solubility and in vitro permeability of poorly soluble drug substances as postulated in a number of publications (Gautschi et al, 2015;Tran et al, 2017;Van Hooegevest, 2017).…”

“…Mostly, only the formulation with best solubilization properties was then chosen for in vivo bioavailability testing. Although recent publications (Tran et al, 2017, Park, 2017 acknowledge that this formulation design approach likely is wrong and misleading, it is still debated what the reasons behind this divergence are and which alternative formulation evaluating-approaches, with better predictive potential, may be used. The topic gets even more complex when considering "phospholipid complexes" e.g.…”

Sistemas de entrega de fármacos autoemulsificables: una plataforma de desarrollo alternativa para la industria farmacéutica colombiana

“…Los aceites de cadena larga (CL) son menos susceptibles a la degradación enzimática por lo cual son menos propensos a presentar precipitación del fármaco en comparación con los aceites de cadena media (CM), debido a que los ácidos grasos productos de su digestión, tienen mayor afinidad por la interface aceite-agua, bloqueando así la actividad enzimática [82,104]. Sin embargo, los CM al ser hidrolizados con mayor rapidez permiten una absorción más rápida del fármaco, aunque esto implica un mayor riesgo de presentar precipitación del fármaco.…”

Using Potentiometric Free Drug Sensors to Determine the Free Concentration of Ionizable Drugs in Colloidal Systems

“…[7][8][9] In order to quantify the amount of solubilized drug generated during in vitro lipolysis, samples are taken and lipase activity is inhibited, thereafter the sample is separated into 2 different phases (i.e., a supernatant phase and a pellet phase) and the drug is quantified using HPLC. 10 This method allows measuring the total drug concentration in supernatant phase, including both free drug and drug entrapped in colloidal structures.…”