Amorphous drug dispersions with mono- and diacyl lecithin: On molecular categorization of their feasibility and UV dissolution imaging

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

“…Depending on the preparation method, the phospholipid type and additional excipients used, the SPD may differ in the appearance of the solid material as well as the dissolution behavior (Fong et al, 2015b, Gautschi et al, 2015.…”

“…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).…”

“…Solid state analysis of CXB SPDs with low PC contents prepared by freeze drying (diacyl PC formulation) or solvent evaporation (mono-and diacyl PC formulations) has previously revealed that CXB is completely amorphous in formulations containing a low amount of PC (Fong et al, 2016, Gautschi et al, 2015.…”

Application of UV Imaging in Formulation Development

“…Lipid-based drug delivery systems constitute a versatile approach for increasing the bioavailability of poorly soluble APIs [38,71]. Gautschi et al studied drug release from drugphospholipid complexes by UV imaging [72]. Formulations were prepared using monoacyl or diacyl phosphatidylcholine (PC) as excipients and a series of poorly soluble compounds (BCS II and IV) to characterize the feasibility of forming drug-phospholipid dispersions at a 1:1 molar ratio.…”

“…The ability to form solid dispersions with the phospholipids was related to API physical chemical parameters such as frontier orbital energy, enthalpy of fusion, and log P [72]. Dissolution studies using UV imaging showed a remarkable surface swelling of the solid dispersions over the compact surface due to phospholipid hydration.…”