How does bile salt penetration affect the self-assembled architecture of pluronic P123 micelles? – light scattering and spectroscopic investigations

2015 ◽  
Vol 17 (30) ◽  
pp. 19977-19990 ◽  
Author(s):  
Arpita Roy ◽  
Niloy Kundu ◽  
Debasis Banik ◽  
Jagannath Kuchlyan ◽  
Nilmoni Sarkar
Keyword(s):  
Light Scattering ◽  
Bile Salt ◽  
Bile Salts ◽  
Triblock Copolymer ◽  
Sodium Taurocholate ◽  
Sodium Deoxycholate ◽  
The Self ◽  
Spectroscopic Investigations ◽  
Pluronic P123 ◽  
Supramolecular Aggregate

The triblock copolymer of the type (PEO)20–(PPO)70–(PEO)20 (P123) forms a mixed supramolecular aggregate with different bile salts, sodium deoxycholate (NaDC) and sodium taurocholate (NaTC), having different hydrophobicity.

Investigation of the enhanced ability of bile salt surfactants to solubilize phospholipid bilayers and forming mixed micelles

Soft Matter ◽  
2021 ◽  
Author(s):  
Vahid Forooqi Motlaq ◽  
Mattia Ortega Holmberg ◽  
Katarina Edwards ◽  
Lars Gedda ◽  
Jeppe Lyngsoe ◽  
...  
Keyword(s):  
Light Scattering ◽  
Bile Salt ◽  
Self Assembly ◽  
Mixed Micelles ◽  
Saline Solution ◽  
Physiological Saline ◽  
Sodium Deoxycholate ◽  
Phospholipid Bilayers ◽  
The Self ◽  
Physiological Saline Solution

The self-assembly in mixtures of the anionic bile salt surfactant sodium deoxycholate (NaDC) and the zwitterion-ic phospholipid 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) in physiological saline solution has been investigated using light scattering, small-angle...

Effect of intestinal resection on bile salt absorption in dogs

1965 ◽  
Vol 208 (2) ◽  
pp. 363-369 ◽  
Author(s):  
M. R. Playoust ◽  
Leon Lack ◽  
I. M. Weiner
Keyword(s):  
Bile Salt ◽  
Bile Salts ◽  
Enterohepatic Circulation ◽  
Sodium Taurocholate ◽  
Intestinal Resection ◽  
High Fat ◽  
Salt Absorption ◽  
Complete Failure ◽  
Fat Meal

The efficiency of intestinal absorption of bile salts was evaluated by studying the rate of disappearance of radioactivity from the bile of dogs after the intravenous administration of sodium taurocholate-24-C14. Bile was sampled through an indwelling tube in the gall bladder. One day after a high-fat meal normal dogs retained 48% of the radioactivity; dogs with resection of the jejunum retained 48%, whereas those with resection of the ileum retained only 3% in the bile. This is consistent with previous observations that the ileum is the site of bile salt absorption in vitro and in anesthetized animals. Animals with resection of the ileum exhibited significant steatorrhea; however, three-fourths of the ingested fat was absorbed in spite of almost complete failure to absorb bile salts. This indicates that fat and bile salts are not normally absorbed together. Elimination of enterohepatic circulation of bile salts by resection of the ileum contributes to the observed steatorrhea.

Effect of glycodihydrofuisidate on sulfobromophthalein transport maximum in the hamster

1976 ◽  
Vol 231 (6) ◽  
pp. 1875-1878 ◽  
Author(s):  
Y Delage ◽  
M Dumont ◽  
S Erlinger
Keyword(s):  
Bile Salt ◽  
Transport System ◽  
Bile Salts ◽  
Sodium Taurocholate ◽  
Specific Effect ◽  
Biliary Secretion ◽  
Biliary Lipid ◽  
Lipid Secretion ◽  
Dye Transport ◽  
Cholesterol Secretion

The effect on sulfobromophathalein transport maximum (Tm) and biliary lipid secretion of sodium glyco-24,25-dihydrofusicate, a micelle-forming compound secreted into bile, has been studied in the hamster and compared to that of a physiological bile salt, sodium taurocholate. Biliary phospholipid and cholesterol secretion increased both during glycodihydrofusidate and taurocholate administration, an observation which suggest that both compounds increased th biliary secretion of micelle-forming compounds. In contrast, only taurocholate increased sulfobromophthalein Tm into bile, while glycodihydrofusidate administration decreased it. This observation suggests that the increase in sulfobromophthalein Tm observed during taurocholate administration is not the result of micellar sequestration. It could rather be the consequence of a specific effect of bile salts on the dye transport system.

Comparison of In Vitro Binding of Bile Salt by Pectins from Various Sources

2012 ◽  
Vol 506 ◽  
pp. 274-277 ◽  
Author(s):  
K. Cheewatanakornkool ◽  
A. Chaidedgumjorn ◽  
U. Sotanaphun ◽  
S. Limsirichaikul ◽  
C. Wessapan ◽  
...  
Keyword(s):  
Bile Salt ◽  
Bile Salts ◽  
Serum Cholesterol Level ◽  
Sodium Deoxycholate ◽  
Sodium Cholate ◽  
Experimental Animals ◽  
Hypocholesterolemic Action ◽  
Acid Reaction ◽  
Layer Chromatography

Binding of bile salts by dietary fiber is believed to promote their excretion and hence to reduce the serum cholesterol level in man and experimental animals. In this study, the binding efficiency of soluble pectin from various sources, i.e., apple, citrus and pomelo, was examined. Sodium deoxycholate and sodium cholate hydrate were used as a model to represent bile salt in human body. The binding efficiency was assayed by acid reaction, thin layer chromatography (TLC) and enzyme cycling method. The results demonstrated that enzyme cycling method was the most suitable for assaying the in-vitro binding of bile salts while the TLC was not very sensitive, i.e., low amount of bile salts cannot be detected by TLC. Excess pectin from binding test could also interfere the acid reaction method even though the centrifugation was used to remove the excess pectin. When the concentration of pectin was increased, the binding efficiency with sodium deoxycholate increased. However, at 1% w/w of pectin, the binding efficiency decreased. The exception is for pomelo pectin in which the binding efficiency increased when the pectin concentration increased. With sodium cholate hydrate, only slight difference in binding efficiency was observed for all types and concentrations of pectin. The results indicate that the ability to bind bile salts of pectin might be responsible for its hypocholesterolemic action observed in experimental animals and humans.

scholarly journals Spectrophotometric determination of the critical micellar concentration of bile salts using bilirubin monoglucuronide as a micellar probe. Utility of derivative spectroscopy

1988 ◽  
Vol 252 (1) ◽  
pp. 275-281 ◽  
Author(s):  
W Spivak ◽  
C Morrison ◽  
D Devinuto ◽  
W Yuey
Keyword(s):  
Bile Salt ◽  
Bile Salts ◽  
Sodium Taurocholate ◽  
Critical Micellar Concentration ◽  
Relative Energy ◽  
Bile Pigment ◽  
Sharp Change ◽  
Derivative Spectroscopy ◽  
Invasive Method ◽  
Sudden Decrease

We have developed a simple biologically non-invasive method for determining the critical micellar concentration (CMC) of bile salts using pure naturally occurring bilirubin IX alpha monoglucuronide (BMG), an important bile pigment present in virtually all mammalian biles. This methodology employs visible absorbance spectroscopy of BMG in bile salts over a range of bile salt concentrations that include the reported CMC. Using 100 microM-BMG in 0.4 M-imidazole buffer at pH 7.8, we calculated that the CMC for sodium taurochenodeoxycholate is between 2.5 and 3.0 mM based on: (1) an abrupt change in lambda max. in this concentration range, (2) a precipitous decrease in the amplitude of the absorbance shoulder at 450 nm, (3) a sudden decrease in the second derivative absorbance of BMG at 400 nm and an increase in absorbance at 470 nm, (4) a sharp change in the 4th derivative absorbance at 375 and 395 nm. In contrast, sodium taurocholate, a bile salt that reportedly does not have a CMC but continuously self-associates over a wide concentration range, exhibited none of these changes. The use of derivative spectroscopy enhances the ability to detect the CMC changes and also indicates the number of BMG species in solution and their relative energy states.

scholarly journals Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

2017 ◽  
Vol 20 ◽  
pp. 305 ◽  
Author(s):  
Mosab Arafat ◽  
Cathrin Kirchhoefer ◽  
Momir Mikov ◽  
Muhammad Sarfraz ◽  
Raimar Löbenberg
Keyword(s):  
Bile Salt ◽  
Oral Bioavailability ◽  
Bile Salts ◽  
Structural Integrity ◽  
Sodium Deoxycholate ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Class Iii ◽  
Simulated Intestinal Fluid ◽  
Fed State

PURPOSE: Liposomes have been studied as a colloidal carrier in drug delivery systems, especially for oral administration. However, their low structural integrity in the gut is still a major shortcoming. Membrane disruptive effects of physiological bile salts in the small intestine result in premature drug release prior to intestinal absorption. Thus, we analyzed the stabilizing effect of sodium deoxycholate when incorporated into nano-sized liposomes. METHOD: Cefotaxime-loaded liposomes were prepared with different sodium deoxycholate concentrations (3.75- 30 mM) by rotary film evaporation followed by nano-size reduction. The physical integrity of liposomes was evaluated by monitoring cefotaxime leakage, particle sizes in different simulated physiological media. The oral bioavailability and pharmacokinetics of cefotaxime was assessed in rats (n = 6 per group) after single dose of drug-encapsulated in liposomes containing bile salt, drug in conventional liposomes, and cefotaxime solution (oral and intravenous). RESULTS: Simulated gastric fluid with low pH showed less effect on the stability of liposomes in comparison to media containing physiological bile salts.  Liposomes containing 15 mM sodium deoxycholate were most stable in size and retained the majority of encapsulated cefotaxime even in fed state of simulated intestinal fluid being the most destructive media. Pharmacokinetics data showed an increase in Cmax and AUC0-inf in the following order: cefotaxime solution < conventional liposomes < liposomes made with bile salts. The total oral bioavailability of cefotaxime in liposomes containing bile salt was found to be 5-times higher compared to cefotaxime solution and twice as much as in conventional liposomes. CONCLUSION: Incorporation of bile salts, initially used as membrane permeation enhancer, also acted as a stabilizer against physiological bile salts. The nano-sized liposomes containing sodium deoxycholate were able to reduce the leakage of encapsulated cefotaxime in the gut due to the improved vesicle stability and to enhance the oral bioavailability of acid-labile drugs up to 5-fold. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Ileal transposition into the upper jejunum affects lipid and bile salt absorption in rats

1996 ◽  
Vol 271 (4) ◽  
pp. G681-G691 ◽  
Author(s):  
T. Tsuchiya ◽  
T. J. Kalogeris ◽  
P. Tso
Keyword(s):  
Bile Salt ◽  
Bile Salts ◽  
Sodium Taurocholate ◽  
Cholesterol Absorption ◽  
Lymphatic Transport ◽  
Proximal Jejunum ◽  
Ileal Transposition ◽  
Sham Surgery ◽  
Salt Absorption ◽  
Lymph Duct

To determine whether ileal transposition affects absorption and transport of lipids and bile salts, we studied the absorption and lymphatic transport of triglyceride, cholesterol, and sodium taurocholate in rats with the distal quarter of their small bowel transposed to the proximal jejunum and in control rats whose intestines were transected and reanastomosed without transposition. Three weeks after transposition or sham surgery, rats were equipped with duodenal or jejunal and intestinal lymph duct cannulas and then given continuous duodenal or jejunal infusions of lipid emulsion containing triolein (40 mumol/h + [3H]triolein) and cholesterol (7.8 mumol/h + [14C]cholesterol) for 8 h. Lymph lipid output was measured; after 8 h of lipid infusion, luminal and mucosal radioactive lipid distribution was also quantified. Transposition had no effect on triglyceride absorption and transport, but cholesterol absorption and transport were both significantly attenuated in the transposed rats. In a separate study we examined whether ileal transposition would alter the kinetics of bile salt absorption. Six weeks after either transposition or sham surgery, rats were given a duodenal bolus injection of 14C-labeled sodium taurocholate mixed in rat bile, and the output of radiolabeled bile salt through a bile fistula was measured. Appearance of radiolabeled taurocholate was gradual in the control rats, peaking at approximately 90 min after administration. Appearance of labeled bile salt was rapid in the transposed rats, peaking within 60 min after administration. In conclusion, ileal transposition has no effect on triglyceride absorption but attenuates cholesterol absorption and transport, possibly by promoting premature absorption of bile salts.

scholarly journals The inhibitory effect of blood serum on hæmolysis

1923 ◽  
Vol 95 (665) ◽  
pp. 42-61 ◽  
Keyword(s):  
Blood Serum ◽  
Bile Salt ◽  
Bile Salts ◽  
Quantitative Methods ◽  
Sodium Taurocholate ◽  
Marked Change ◽  
Inhibitory Effect ◽  
Haemolytic Activity ◽  
Serum Globulin

It has been recognised for many years that blood serum has an inhibitory effect on the hæmolysis produced by many substances, notably saponin and bile salts. Ransom (1), in 1901, observing that cholesterol inhibits the action of saponin, attributed the inhibitory effect of serum to the contained cholesterol. The quantities of cholesterol used in his experiments are far greater than those which occur in serum, and the experiments are inconclusive for that reason. Bayer (2), in 1907, investigated the inhibitory effect produced by serum on the action of the bile salts. He found that cholesterol has no inhibitory effect, that lecithin produces inhibition, but not in the quantities that occur in blood, and that the proteins of the serum are responsible for the inhibition. He calls attention to the results of von Eisler (3), who states that serum globulin inhibits the action of staphalolysin and of tetanolysin, and also those of von Liebermann, who finds that hæmolysis by soaps is prevented by serum albumin (4). Bayer’s researches are, in the main, confirmed by Sellards (5). The investigations of Ludke (6) and of Scandaliato (7), who found that the inhibitory effect of serum is slightly increased after the injection of bile salts, may be mentioned. The conclusions of these authors are unreliable, since inadequate methods of measuring the amount of inhibition were used. References to various points in connection with the inhibition produced by serum in vivo and in vitro are to be found in the writer’s earlier papers (8, 9, 10). The Nature of the Inhibitory Substances . Before proceeding to the quantitative estimations, it is necessary to know which constituents of serum are responsible for the inhibition of saponin and bile salt hæmolysis respectively. Bayer’s results might be taken as conclusive were it not for two considerations: (1) Bayer filtered most of the solutions of bile salts, and lecithin-bile-salt mixtures, whose hæmolytic power he wished to determine, through a Berkefeld filter, and thereafter tested their hæmolytic activity. He states that this procedure has no effect on the time taken for these solutions to produce hæmolysis. This is a fallacy, for a solution of sodium taurocholate will not pass through a filter paper without losing some of its hæmolytic activity, while passage through a Berkefeld filter causes a very marked change indeed (10). It is therefore not permissible to regard the hæmolytic activity of a solution filtered in this way as identical with, or even corresponding to, the activity of an unfiltered solution; (2) Bayer used very rough quantitative methods—he refers to “slight hæmolysis,” “considerable hæmolysis,” etc., and, accordingly, would be able to detect only very marked degrees of inhibition. The same remark applies to the experiments of Sellards.

scholarly journals Enzymic hydrolysis of sphingomyelin in the presence of bile salts

1980 ◽  
Vol 185 (3) ◽  
pp. 749-754 ◽  
Author(s):  
S Yedgar ◽  
S Gatt
Keyword(s):  
Bile Salt ◽  
Bile Salts ◽  
Sodium Taurocholate ◽  
Absolute Concentration ◽  
Mixed Aggregates ◽  
Sodium Taurodeoxycholate ◽  
Rate Of Hydrolysis ◽  
The Absolute ◽  
Hydrolysis Of ◽  
Low Activity

Sphingomyelin in mixed dispersion with bile salts was hydrolysed by the solubilized sphingomyelinase of rat brain lysosomes. In parallel studies, physical properties of these dispersions were determined. The kinetic curves that described the rate of hydrolysis as a function of increasing concentrations of bile salt were multiphasic. A region of very low activity was followed by an ascending portion, a peak, a descending portion, a trough and a second ascending portion. The positions of the initiation points, peaks and troughs were found to be a function of the respective ratios of the bile salt to sphingomyelin for the detergent sodium taurodeoxycholate, but of the absolute concentration of the detergent for sodium taurocholate. Turbidity studies suggested that hydrolysis of sphingomyelin begins at a bile salt concentration that solubilizes the lipid and incorporates it into a mixed micelle with the detergent. Ultracentrifugation studies suggested that the sizes of the mixed aggregates of detergent and lipid were a function of the ratio of taurodeoxycholate to sphingomyelin, but of the absolute concentration of the bile salt, for sodium taurocholate.

Bile salt related secretion of acid phosphatase in rat bile

1986 ◽  
Vol 64 (11) ◽  
pp. 1347-1352 ◽  
Author(s):  
Raul A. Marinelli ◽  
Marcelo G. Luquita ◽  
Emilio A. Rodríguez Garay
Keyword(s):  
Acid Phosphatase ◽  
Bile Salt ◽  
Bile Salts ◽  
Sodium Taurocholate ◽  
Experimental Models ◽  
Experimental Conditions ◽  
Bile Fistula ◽  
Salt Depletion ◽  
Protein Output ◽  
Rat Bile

The biliary excretion of bile salts, lysosomal acid phosphatase, and total proteins were studied in rats under different experimental conditions: (i) during bile salt loss through a bile fistula and (ii) after loading with exogenous sodium taurocholate. The experimental models were suitable to demonstrate that variations in the excretion of bile salts were associated with those of acid phosphatase output. During bile salt depletion, acid phosphatase output showed a decrease parallel to that of bile salts. Following a single i.v. injection of sodium taurocholate and during its i.v. infusion, a rapid increase of acid phosphatase excretion in bile was seen. The patterns of enzyme outputs observed after administration of sodium taurocholate suggested a bulk discharge in bile of lysosomal contents. The profiles of protein output were similar to those of acid phosphatase suggesting an association between the secretory mechanism of these bile constituents. In contrast to sodium taurocholate, 4-methylumbelliferone, which also increases canalicular bile flow, did not produce changes in the excretory patterns of the bile components studied. Therefore, the results suggested a bile salt related secretion of acid phosphatase in the rat, which may involve protein secretion in bile.

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