PLGA/TPGS nanoparticles for controlled release of paclitaxel: Effects of the emulsifier and drug loading ratio

Purpose. We successfully manufactured nanoparticles of biodegradable polymers for controlled release of paclitaxel. TPGS (d-alpha-tocopheryl polyethylene glycol 1000 succinate) could be a novel material to make nanoparticles of high drug encapsulation efficiency (EE) and desired physicochemical and pharmaceutical properties of the drug loaded nanoparticles. Among various controlling parameters in the process, the present work is to elucidate the effects of the surfactant stabilizer and the drug loading ratio. Methods. Paclitaxel loaded PLGA nanoparticles were formulated at various drug-loading ratios by a modified single emulsion solvent extraction/evaporation technique. TPGS was introduced either as the emulsifier or as a matrix material component by using different technique. Polyvinyl alcohol (PVA) was also used for a comparison. The nanoparticles of various recipes were characterized by various state-of-the-art instrument technology for their properties. Results. The EE and the in vitro release behavior were found significantly influenced by the drug loading ratio and the surfactant stabilizer encountered. TPGS involved nanoparticles can have high EE and other favorable properties. Conclusions. TPGS could be a novel and effective emulsifier, which can result in high EE and desired properties of paclitaxel-loaded polymeric nanoparticles.