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Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug absorption...
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Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...
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When a drug is taken orally, it undergoes a journey starting from the gastrointestinal (GI) tract, passing through the portal vein, reaching the liver, and finally entering the systemic circulation. This process involves the absorption of the drug across the GI tract. The liver is the primary site for metabolizing the drug, with some metabolism also occurring in the gut wall. This journey significantly reduces the quantity of the drug that reaches the systemic circulation, a phenomenon known as...
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After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...

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Curcumin bioavailability from enriched bread: the effect of microencapsulated ingredients.

Paola Vitaglione1, Roberta Barone Lumaga, Rosalia Ferracane

  • 1Department of Food Science, University of Naples, Portici (NA), Italy. paola.vitaglione@unina.it

Journal of Agricultural and Food Chemistry
|March 10, 2012
PubMed
Summary

Curcumin bioavailability from bread is enhanced by encapsulation, which increases absorption and prevents breakdown. Phenolic acids are the main metabolites and may contribute to curcumin

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Published on: November 9, 2016

Area of Science:

  • Nutritional Science
  • Pharmacokinetics
  • Food Science

Background:

  • Curcumin, a polyphenol, exhibits limited bioavailability due to rapid metabolism and poor absorption.
  • Dietary intake of curcumin is often achieved through fortified foods like bread.
  • Encapsulation technologies aim to improve the stability and absorption of bioactive compounds.

Purpose of the Study:

  • To evaluate the human bioavailability of curcumin from bread formulations.
  • To compare the effects of free curcumin, encapsulated curcumin, and encapsulated curcumin with other polyphenols on curcuminoid and phenolic acid absorption.
  • To investigate the role of encapsulation and co-administered polyphenols in modulating curcumin bioavailability and metabolism.

Main Methods:

  • Human study involving consumption of bread enriched with free curcumin (FCB), encapsulated curcumin (ECB), or encapsulated curcumin plus other polyphenols (ECBB).
  • Quantification of serum, urinary, and fecal curcuminoids and phenolic acids using High-Performance Liquid Chromatography coupled with tandem Mass Spectrometry (HPLC/MS/MS) over 24 hours.
  • Analysis of absorption, excretion, and metabolic profiles of curcumin and its derivatives.

Main Results:

  • Serum curcuminoid concentrations were low (<4 nmol/L), with glucuronides being 10-fold lower.
  • Encapsulation significantly increased and delayed curcuminoid absorption compared to free curcumin.
  • Ferulic and vanillic acids (phenolic acids) were found in much higher concentrations than curcuminoids, with ECBB yielding the highest amounts; phenolic acids are major metabolites of curcuminoids.

Conclusions:

  • Curcuminoid encapsulation enhances bioavailability from enriched bread, likely by preventing premature biotransformation.
  • Co-administration with other polyphenols had a minor impact on this effect.
  • Phenolic acids represent the primary metabolites of curcuminoids and may play a role in their observed biological activities.