title: Practical preparation procedures for docetaxel-loaded nanoparticles using polylactic acid-co-glycolic acid.
abstract: BACKGROUND
  Nanoparticles fabricated from the biodegradable and biocompatible polymer, polylactic-co-glycolic acid (PLGA), are the most intensively investigated polymers for drug delivery systems. The objective of this study was to explore fully the development of a PLGA nanoparticle drug delivery system for alternative preparation of a commercial formulation. In our nanoparticle fabrication, our purpose was to compare various preparation parameters.
  
  
  METHODS
  Docetaxel-loaded PLGA nanoparticles were prepared by a single emulsion technique and solvent evaporation. The nanoparticles were characterized by various techniques, including scanning electron microscopy for surface morphology, dynamic light scattering for size and zeta potential, x-ray photoelectron spectroscopy for surface chemistry, and high-performance liquid chromatography for in vitro drug release kinetics. To obtain a smaller particle, 0.2% polyvinyl alcohol, 0.03% D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), 2% Poloxamer 188, a five-minute sonication time, 130 W sonication power, evaporation with magnetic stirring, and centrifugation at 8000 rpm were selected. To increase encapsulation efficiency in the nanoparticles, certain factors were varied, ie, 2-5 minutes of sonication time, 70-130 W sonication power, and 5-25 mg drug loading.
  
  
  RESULTS
  A five-minute sonication time, 130 W sonication power, and a 10 mg drug loading amount were selected. Under these conditions, the nanoparticles reached over 90% encapsulation efficiency. Release kinetics showed that 20.83%, 40.07%, and 51.5% of the docetaxel was released in 28 days from nanoparticles containing Poloxamer 188, TPGS, or polyvinyl alcohol, respectively. TPGS and Poloxamer 188 had slower release kinetics than polyvinyl alcohol. It was predicted that there was residual drug remaining on the surface from x-ray photoelectron spectroscopy.
  
  
  CONCLUSIONS
  Our research shows that the choice of surfactant is important for controlled release of docetaxel.
authors: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Gungdong, Yuseonggu, Daejeon, South Korea.
authors: Chang-Gu
authors: CG
authors: Keum
authors: Young-Wook
authors: YW
authors: Noh
authors: Jong-Suep
authors: JS
authors: Baek
authors: Ji-Ho
authors: JH
authors: Lim
authors: Chan-Ju
authors: CJ
authors: Hwang
authors: Young-Guk
authors: YG
authors: Na
authors: Sang-Chul
authors: SC
authors: Shin
authors: Cheong-Weon
authors: CW
authors: Cho
mesh_terms: D000085:Acetates; D002498:Centrifugation; D002725:Chloroform; D000077143:Docetaxel; D019344:Lactic Acid / Q000737:chemistry*; D053769:Nanocapsules / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D056951:Photoelectron Spectroscopy; D020442:Poloxamer; D011092:Polyethylene Glycols; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011142:Polyvinyl Alcohol; D013010:Sonication; D013500:Surface Tension; D013501:Surface-Active Agents; D043823:Taxoids / Q000737:chemistry*; D014810:Vitamin E / Q000031:analogs & derivatives
chemical_list: D000085:Acetates; D053769:Nanocapsules; D013501:Surface-Active Agents; D043823:Taxoids; D020442:Poloxamer; D014810:Vitamin E; D000077143:Docetaxel; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; C007650:ethyl acetate; D002725:Chloroform; D011142:Polyvinyl Alcohol; C014225:tocophersolan