A novel one-step drug-loading procedure for water-soluble amphiphilic nanocarriers.
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.
Fournier
Elvire
E
Faculty of Pharmacy, University of Montreal, C.P. 6128, Succ. Centre-Ville, Montreal, Quebec H3C 3J7, Canada.
Dufresne
Marie-Hélène
MH
Smith
Damon C
DC
Ranger
Maxime
M
Leroux
Jean-Christophe
JC
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
D001952:Bridged-Ring Compounds; D000440:Butanols; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D043823:Taxoids; D014867:Water; C080625:taxane