STUDY ON IN VIVO RELEASE AND IN VIVO ABSORPTION OF CAMPTOTHECIN-LOADED POLYMERIC NANOPARTICLES: LEVEL A IN VITRO - IN VIVO CORRELATION

ABSTRACTObjectives: The aim of this study was to develop an in vitro - in vivo correlation (IVIVC) for the prepared Camptothecin (CPT)-loaded polymericnanoformulation.Methods: In this study, CPT-loaded polymeric nanoformulation was prepared by nanoprecipitation method using containing poly (methacrylic acidco-methylmethacrylate) (polymer), poloxamer 188 (non-ionic surfactant), and β-cyclodextrin (stabilizer). In vitro release rate data were obtainedfrom prepared polymeric nanoformulation using the USP apparatus type 2. A single-dose, crossover pharmacokinetic study for the nanoformulationwas carried out in six albino rats. These data were used as the basis for the IVIVC model development.Results: The plasma concentration of CPT was estimated by high-performance liquid chromatography. The pharmacokinetic parameters werecalculated from the plasma concentration of CPT and time data. Furthermore, the deconvolution of the in vivo concentration-time data was performedusing Wagner–Nelson method to estimate the in vivo drug release profile.Conclusion: Therefore, a level A IVIVC was developed for CPT-loaded polymeric nanoformulation between dissolution percentage and intestinalabsorption in rats. The simplest way to demonstrate a correlation is to plot the percentage absorbed in vivo versus the percentage released in vitro atthe same time.Keywords: Camptothecin, In vitro - in vivo correlation, Wagner–Nelson, Dissolution, Pharmacokinetics