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Review
. 2015 Aug 10;20(8):14451-73.
doi: 10.3390/molecules200814451.

Absorption-Enhancing Effects of Bile Salts

Eskandar Moghimipour  1 , Abdulghani Ameri  2 , Somayeh Handali  3
Affiliations
Review

Absorption-Enhancing Effects of Bile Salts

Eskandar Moghimipour et al. Molecules. .

Abstract

Bile salts are ionic amphiphilic compounds with a steroid skeleton. Among the most important physiological properties of bile salts are lipid transport by solubilization and transport of some drugs through hydrophobic barriers. Bile salts have been extensively studied to enhance transepithelial permeability for different marker molecules and drugs. They readily agglomerate at concentrations above their critical micelle concentration (CMC). The mechanism of absorption enhancement by bile salts appears to be complex. The aim of the present article was to review bile salt structure and their application as absorption enhancers and the probable mechanism for increasing permeation based on previous studies.

Keywords: absorption enhancers; bile salts; drug delivery.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Common chemical structure of bile acids.
Scheme 1
Scheme 1
Schematic representation of bile acids biosynthesis from cholesterol.
Figure 2
Figure 2
Primary and secondary aggregation model of bile salt micelles [18].
Figure 3
Figure 3
Effect of various surfactants on the Merit index of sCT.SLS: sodium lauryl sulfate, Bza: benzalkonium chloride, Bze: benzetonium chloride, NaGC: sodium glycocholate, NaC: sodium cholate, NaTC: sodium taurocholate, NaDHC: sodium dehydrocholate, UDC: ursodeoxycholate, LCC: lauroylcarnitine chloride, NaTUDC: sodium tauroursodeoxycholate, NaDC: sodium deoxycholate, NaTCDC: sodium taurochenodeoxycholate, NaGDC: sodium glycodeoxycholate, NaTDC: sodium taurodeoxycholate [53].
Figure 4
Figure 4
Preparation of DCT-loaded nanomicelles containing NaTC [88].
Figure 5
Figure 5
Anti-tumor efficacy of DCT-loaded nanomicelles with and without NaTC after rectal administration [88].* Significantly smaller than control group (p < 0.01).
Figure 6
Figure 6
The most common transport mechanisms of bile salts; (A) micelle formation; (B) reverse micellization; (C) enzyme inhibition; (D) viscosity reduction of the mucus layer.
Figure 7
Figure 7
Percentage haemolysis of red blood cells caused by incubation with differing concentrations of NaDOC and NaTCDC (mean ± SE, n = 8) (data are taken from [106]).
Figure 8
Figure 8
Effects of 0.2 mM mixed micelles with different lecithin/NaDC ratios on the apoptosis of Caco-2 cells (n = 5) [108]. * p < 0.05, ** p < 0.01.
See this image and copyright information in PMC

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