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A Novel One-Step Drug-Loading Procedure for Water-Soluble Amphiphilic Nanocarriers

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Abstract

Purpose. 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.

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Authors and Affiliations

  1. Canada Research Chair in Drug Delivery, Faculty of Pharmacy, University of Montreal, C.P. 6128, Succ. Centre-Ville, Montreal, Quebec, H3C 3J7, Canada

    Elvire Fournier, Marie-Hélène Dufresne, Maxime Ranger & Jean-Christophe Leroux

  2. Labopharm Inc., Laval, Quebec, H7V 4B4, Canada

    Damon C. Smith

Authors
  1. Elvire Fournier
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  2. Marie-Hélène Dufresne
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  3. Damon C. Smith
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  4. Maxime Ranger
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  5. Jean-Christophe Leroux
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Correspondence to Jean-Christophe Leroux.

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Fournier, E., Dufresne, MH., Smith, D.C. et al. A Novel One-Step Drug-Loading Procedure for Water-Soluble Amphiphilic Nanocarriers. Pharm Res 21, 962–968 (2004). https://doi.org/10.1023/B:PHAM.0000029284.40637.69

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