Polymeric micelles for oral drug delivery: Why and how
M. F. Francis, M. Cristea, and F. M. Winnik
Faculty of Pharmacy, University of Montreal, C.P.
6128 Succ. Centreville, Montreal, Quebec H3C 3J7, Canada; Department
of Chemistry, University of Montreal, C.P.6128 Succ. Centreville, Montreal,
Quebec H3C 3J7, Canada; Petru Poni Institute of Macromolecular Chemistry,
Iasi 6600, Romania
Abstract: The oral delivery of drugs is regarded as the optimal
means for achieving therapeutic effects owing to increased patient compliance.
Unfortunately, the oral delivery route is beset with problems such as
gastrointestinal (GI) destruction of labile molecules, low levels of
macromolecular absorption, etc. To reduce the impact of digestive enzymes
and to ensure the absorption of bioactive agents in an unaltered form,
molecules may be incorporated into microparticulate carriers. Many approaches
to achieve the oral absorption of a wide variety of drugs are currently
under investigation. Among the different polymer-based drug delivery
systems, polymeric micelles represent a promising delivery vehicle especially
intended for poorly water-soluble pharmaceutical active ingredients
in order to improve their oral bioavailability. Recent findings of a
dextran-based polymeric micelle study for solubilization of a highly
lipophilic drug, cyclosporin A (CsA), will be discussed.
*Lecture presented at the symposium "Controlling the self assembly in macromolecular systems: From nature to chemistry to functional properties", as part of the 39th IUPAC Congress and 86th Conference of the Canadian Society for Chemistry: Chemistry at the Interfaces, Ottawa, Canada, 10-15 August 2003. Other Congress presentations are published in this issue, pp. 1295-1603.
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