Bridging Laboratory and Large Scale Production: Preparation and In Vitro-Evaluation of Photosensitizer-Loaded Nanocarrier Devices for Targeted Drug Delivery

Abstract

By adjusting all process parameters, a potent formulation for application in the GI tract was obtained. The essential steps of process development and scale-up were part of this formulation development.

Drug Release and Targeting: the Versatility of Polymethacrylate Nanoparticles for Peroral Administration Revealed by Using an Optimized In Vitro-Toolbox

“…With the help of this procedure an effective separation of particles from the supernatant and therefore encapsulated from free API, was accomplished (20). Filter adsorption was tested under comparable conditions.…”

“…The excipient composition assured optimal characteristics of the nanocarrier formulation with regards to particle size, size distribution, zeta potential, and encapsulation efficiency as described previously (20). Further characterization was undertaken in order to make sure that TMP-001 had no effect on relevant product characteristics of the selected formulation design.…”

“…Furthermore, biorelevant release testing was applied in order to investigate the interactions between drug, nanocarrier and the physiological environment, and their impact on the drug delivery paradigm. In this context, Eudragit® RS 100-nanoparticles were prepared by a scalable nanoprecipitation technique (20). Unloaded nanoparticles and a formulation containing the weak acid TMP-001 (pKa=4.22, logP=10.417) were investigated (20,21).…”

“…In this context, Eudragit® RS 100-nanoparticles were prepared by a scalable nanoprecipitation technique (20). Unloaded nanoparticles and a formulation containing the weak acid TMP-001 (pKa=4.22, logP=10.417) were investigated (20,21). TMP-001 is a model compound tested for its therapeutic relevance for several inflammatory diseases.…”

“…For other compounds such as the photosensitizer temoporfin, a slow release from the polymeric shell and low systemic availability combined with an effective uptake of the loaded nanoparticles into cancer cells are considered to be beneficial (20,24). Recently, budesonide was effectively delivered to the inflamed colonic mucosa after incorporation into Eudragit® S-coated chitosan-Ca-alginate-microparticles.…”