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. 2013:2013:340315.
doi: 10.1155/2013/340315. Epub 2013 Jun 27.

Polymeric micelles, a promising drug delivery system to enhance bioavailability of poorly water-soluble drugs

Wei Xu  1 , Peixue Ling, Tianmin Zhang
Affiliations

Polymeric micelles, a promising drug delivery system to enhance bioavailability of poorly water-soluble drugs

Wei Xu et al. J Drug Deliv. 2013.

Abstract

Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

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Figures

Figure 1
Figure 1
Schematic representation of the mechanisms involved in the absorption of exogenous drugs in the small intestine. (a) Transcellular transport; (b) active transport; (c) facilitated diffusion; (d) receptor-mediated endocytosis; (e) paracellular transport; (f) pinocytosis [3].
Figure 2
Figure 2
Formation and drug loading of PMs by self-assemble of amphiphilic block copolymers in aqueous solution.
Figure 3
Figure 3
Schematic representation of the mechanisms of pH sensitivity. (a) PMs with basic core units, (b) PMs with acidic core units.
Figure 4
Figure 4
Pluronic block copolymers available from BASF (Wyandotte, MI, USA) contain two hydrophilic EO blocks and a hydrophobic PO block [167].
Figure 5
Figure 5
Structure of D-a-tocopheryl polyethylene glycol succinate (TPGS).
See this image and copyright information in PMC

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