Do Phospholipids Boost or Attenuate Drug Absorption? In Vitro and In Vivo Evaluation of Mono- and Diacyl Phospholipid-Based Solid Dispersions of Celecoxib

Abstract Phospholipids are amphiphilic lipids with versatile properties making them promising excipients for enabling formulations oral drug delivery. Unfortunately, systematic studies on how phospholipid type and content affect absorption rare. Often, only one is used the formulation development formulation, optimized according to in vitro parameters, included bioavailability studies. Using this approach, it unclear if a certain parameter predictive vivo performance. In study, labor-saving permeation screening method was combined pharmacokinetic study rats first time systematically compare two types of phospholipid-based solid dispersions. The dispersions contained celecoxib monoacyl or diacyl phosphatidylcholine at different drug-to-phospholipid ratios. revealed: 1) none high increased permeation, 2) negatively correlated 3) mono diacyl-phosphatidylcholine performed equally. At low enhanced, absorption, Apart from reference (suspension), thus predicted