PLGA/TPGS nanoparticles for controlled release of paclitaxel: effects of the emulsifier and drug loading ratio.
OBJECTIVE
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.
Mu
Li
L
Division of Bioengineering, The National University of Singapore, 9 Engineering Drive 1, Singapore 117576.
Feng
Si-Shen
SS
D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods; D045703:Emulsifying Agents / Q000737:chemistry / Q000493:pharmacokinetics*; D019344:Lactic Acid / Q000737:chemistry / Q000493:pharmacokinetics*; D036103:Nanotechnology / Q000379:methods*; D017239:Paclitaxel / Q000737:chemistry / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics*; D011100:Polyglycolic Acid / Q000737:chemistry / Q000493:pharmacokinetics*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics*; D014810:Vitamin E / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D045703:Emulsifying Agents; D011108:Polymers; D014810:Vitamin E; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; C014225:tocophersolan; D017239:Paclitaxel