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Pure Appl. Chem., 2004, Vol. 76, No. 7-8, pp. 1321-1335

Polymeric micelles for oral drug delivery: Why and how

M. F. Francis, Mariana 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.