title: A novel one-step drug-loading procedure for water-soluble amphiphilic nanocarriers.
abstract: OBJECTIVE
  The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited by the incorporation methods available, especially when sterile dosage forms are sought.
  
  
  METHODS
  In this manuscript, we describe a straightforward, economical, and innovative drug-loading procedure that consists in dissolving both the drug and an amphiphilic diblock copolymer in a water/tert-butanol mixture that is subsequently freeze-dried.
  
  
  RESULTS
  We demonstrate that monodisperse 20-60 nm-sized drug-loaded polymeric micelles are produced directly and spontaneously upon rehydration of the freeze-dried cake. To establish the proof-of-principle, two hydrophobic taxane derivatives were solubilized in the micelles, and their partition coefficient was determined.
  
  
  CONCLUSIONS
  This approach is efficient yet astonishingly simple and may be of great interest for scientists working in nanotechnology and pharmaceutical sciences.
authors.affiliation: Faculty of Pharmacy, University of Montreal, C.P. 6128, Succ. Centre-Ville, Montreal, Quebec H3C 3J7, Canada.
authors.forename: Elvire
authors.initials: E
authors.lastname: Fournier
authors.forename: Marie-Hélène
authors.initials: MH
authors.lastname: Dufresne
authors.forename: Damon C
authors.initials: DC
authors.lastname: Smith
authors.forename: Maxime
authors.initials: M
authors.lastname: Ranger
authors.forename: Jean-Christophe
authors.initials: JC
authors.lastname: Leroux
mesh_terms: D001952:Bridged-Ring Compounds / Q000737:chemistry / Q000145:classification; D000440:Butanols / Q000737:chemistry; D002627:Chemistry, Physical / Q000191:economics / Q000379:methods; D003460:Crystallization; D003681:Dehydration / Q000517:prevention & control; D003692:Delayed-Action Preparations / Q000627:therapeutic use; D004337:Drug Carriers / Q000737:chemistry* / Q000191:economics; D004339:Drug Compounding / Q000191:economics / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods* / Q000639:trends*; D005612:Freeze Drying / Q000379:methods; D008823:Micelles; D036103:Nanotechnology / Q000191:economics / Q000379:methods; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D012995:Solubility; D043823:Taxoids / Q000737:chemistry / Q000145:classification; D013678:Technology, Pharmaceutical / Q000191:economics / Q000379:methods; D014867:Water
chemical_list: D001952:Bridged-Ring Compounds; D000440:Butanols; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D043823:Taxoids; D014867:Water; C080625:taxane