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Steatorrhea
Published in Charles Theisler, Adjuvant Medical Care, 2023
Bile salt therapy was effective in a case study where a patient underwent a colectomy, partial ileectomy, and ileostomy for Crohn's disease. There was concern that bile salt therapy would cause or exacerbate severe diarrhea, but this did not happen.3 Oral bile acid supplementation reduced fat excretion markedly, but did not aggravate diarrhea in this case and in another study.5,6
An Overview of Molecular Nutrition
Published in Nicole M. Farmer, Andres Victor Ardisson Korat, Cooking for Health and Disease Prevention, 2022
Vincent W. Li, Catherine Ward, Delaney K. Schurr
Once in the stomach, gastric lipase, amongst other digestive enzymes, is released. However, gastric lipase is responsible for only the initial and minimal breakdown of ingested fats. The large majority of fat digestion does not occur in the stomach, but later on in the small intestine. Once released from the food matrix, fat is now bound to bile salts to undergo its main form of digestion in the small intestine. Pancreatic lipase works to break down triglyceride fats into monoglycerides and fatty acids. The efficient activity of the lipase is dependent on the presence of bile salts on fat droplets. Multiple bile salts with the complexed triglyceride components spontaneously form micelles. Micelles then enter enterocytes where the bile is broken down and chylomicrons are packaged and extruded from the basolateral enterocyte wall to enter the lymphatics. This is the mechanism for absorption of triglycerides which represent 90% of dietary fat. Dietary cholesterol undergoes a similar process except it requires a transport protein in order to enter the enterocyte. Lastly, MCTs, such as coconut oil, when extruded from the enterocyte go directly into the blood stream, by passing the lymphatic system. Therefore, MCTs are suspected of having a favorable metabolic profile.
Functions of the Liver
Published in Peter Kam, Ian Power, Michael J. Cousins, Philip J. Siddal, Principles of Physiology for the Anaesthetist, 2020
Peter Kam, Ian Power, Michael J. Cousins, Philip J. Siddal
The liver produces about 1 L of bile per day, and this passes into the gall bladder where it is concentrated to about one-fifth of its volume. Bile consists of electrolytes, protein, bilirubin, bile salts and lipids. Bile acids (cholic acid and chenodeoxycholic acid) are produced in the liver from cholesterol. In the gut, bacterial action on cholic and chenodeoxycholic acids produces secondary bile acids such as deoxycholic acid and lithocholic acid. The bile acids conjugate with glycine or taurine to form bile salts (Figure 37.5). Bile salts are more water soluble and less lipid soluble, which limits the passive absorption in the small intestine so that the bile salts remain within the gut. The main function of bile salts is the emulsification of dietary fat, which is essential for fat absorption. In addition, bile salts are also important for the absorption of fat-soluble vitamins, especially vitamins A, D, E and K. At the terminal ileum, bile salts are reabsorbed by the apical sodium-dependent bile transporter. The reabsorbed bile salts are carried to the liver in the portal circulation, mostly bound to plasma proteins. The recirculation of bile salts is referred to as enterohepatic circulation.
Promising strategies for improving oral bioavailability of poor water-soluble drugs
Published in Expert Opinion on Drug Discovery, 2023
Bruna Rocha, Letícia Aparecida de Morais, Mateus Costa Viana, Guilherme Carneiro
Moreover, bile salts (e.g. taurocholate, glycocholate, etc.) are surfactants that emulsify lipids and lipophilic molecules, favoring solubilization in the GIT. However, this can facilitate the action of pancreatic lipases and degradation [10]. Bile salts can also enhance the intestinal permeability of macromolecules by transcellular disturbance [11]. The mucus is a viscoelastic hydrogel-like protective barrier in the stomach and large intestine; it is intermittent in the small intestine and composed of water, mucin (a negatively charged glycoprotein), carbohydrates, lipids, nucleic acids, antibodies, and salts. As it can interact with various drugs by electrostatic (e.g. between cationic drugs and mucin fibers) and other forces, the mucus can be considered selectively permeable to external drugs and a barrier for absorption [12].
Hyaluronic acid-enriched bilosomes: an approach to enhance ocular delivery of agomelatine via D-optimal design: formulation, in vitro characterization, and in vivo pharmacodynamic evaluation in rabbits
Published in Drug Delivery, 2022
Asmaa Ashraf Nemr, Galal Mohamed El-Mahrouk, Hany Abdo Badie
The ability of bilosomes to deliver vaccine orally was studied and proved due to their ability to shield the drug from the bile salts and enzymes of the gastrointestinal tract due to the presence of bile salts in their composition (Aburahma, 2014; Jain et al., 2014; Al-Mahallawi et al., 2015). Bile salts are solubilizing and permeation-enhancing agents. They are widely used because of their biological compatibility and have no toxicity (Zafar et al., 2021). Also, the capability and the safety of the transdermal delivery of bilosomes were investigated and confirmed due to its nanosized vesicle and the elasticity that is required for transdermal delivery (Al-Mahallawi et al., 2015). Bilosomes have been also utilized for ocular delivery. The nanosized vesicles of bilosomes together with the presence of surfactants and bile salts in their compositions provide a promising attempt to assess them for ocular delivery (Mohsen et al., 2020).
Development and optimization of curcumin analog nano-bilosomes using 21.31 full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma: in-vitro evaluation, in-vivo safety assay
Published in Drug Delivery, 2022
Haidy Abbas, Yasmin A. El-Feky, Majid Mohammad Al-Sawahli, Nehal M. EL-Deeb, Hala Bakr El-Nassan, Mariam Zewail
The aim of the current study was to formulate and evaluate the synthesized PIP having an improved anticancer potential compared to CU against hepatocellular carcinoma cells, in BLs adopting 21.31 full factorial design. The obtained BLs are expected to have assimilation-enhancing ability that can increase the drug water solubility and hence, can increase the drug absorption and protect it from the expected enzymatic degradation into GIT. In addition, bile salts can act as solubilizing and permeation enhancing agents which can also improve the drug oral absorption. The prepared formulations were evaluated and optimized to obtain the formula giving the highest desirability according to different chosen dependent variables. This work can be considered the first report of encapsulating curcumin analog (PIP) with enhanced anticancer activity in BLs to combine the advantages of the superior pharmacological activity of CU analog along with the numerous advantages of BLs in terms of BLs' ability to increase the encapsulated drug solubility, stability, permeation across biological barriers and consequently drug bioavailability and pharmacological effects are further improved.