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Related Concept Videos

Bioavailability: Influencing Factors01:22

Bioavailability: Influencing Factors

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...
Bioavailability: Overview01:13

Bioavailability: Overview

Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...
Bioavailability: Overview01:17

Bioavailability: Overview

Bioavailability refers to the proportion of an administered drug that reaches the systemic circulation in its active, unaltered form. It is a crucial pharmacokinetic parameter that determines the effectiveness of a drug in achieving its intended therapeutic outcomes. The route of administration significantly influences bioavailability, with intravenous administration achieving 100% bioavailability as the drug directly enters the bloodstream. In contrast, oral administration often results in...
Cancer Prevention02:59

Cancer Prevention

Several factors can increase the risk of cancer in an individual. About 50% of cancer cases can be prevented by adopting a healthy lifestyle, regular exercise, eating healthy, and following a modest cancer prevention diet. Epidemiological studies have consistently shown that populations with vegetable and fruit-rich diets have reduced the incidence of cancer. On the other hand, populations who have a diet rich in animal fat, red meat, junk food, or high calories are predisposed to cancer.
Some...
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

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...
Factors Influencing Bioavailability: First-Pass Elimination01:23

Factors Influencing Bioavailability: First-Pass Elimination

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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Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay
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Isoflavones: estrogenic activity, biological effect and bioavailability.

Daniela Cristina Vitale1, Cateno Piazza, Barbara Melilli

  • 1Pharmacokinetic Unit, Unifarm Research Center, Catania, Italy.

European Journal of Drug Metabolism and Pharmacokinetics
|November 20, 2012
PubMed
Summary

Isoflavones from soy beans, like genistein and daidzein, offer health benefits but their effectiveness depends on how the body absorbs them. Improving isoflavone bioavailability through formulations is key to maximizing their therapeutic potential.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Nutritional Science

Background:

  • Isoflavones (genistein, daidzein, glycitein) are soy phytoestrogens with estrogenic activity, structurally similar to 17-β-estradiol.
  • They are linked to health benefits including cancer chemoprevention, cardiovascular health, osteoporosis management, and relief of menopausal symptoms.
  • Isoflavone efficacy is significantly influenced by their pharmacokinetic properties, particularly absorption and distribution.

Purpose of the Study:

  • To review and discuss pharmacokinetic factors influencing the biological activity of isoflavones.
  • To highlight the importance of isoflavone chemical form and bioavailability for their health effects.
  • To explore formulation strategies for enhancing isoflavone absorption and distribution.

Main Methods:

  • Review of existing clinical studies and scientific literature on isoflavone pharmacokinetics.
  • Analysis of the impact of isoflavone chemical forms (conjugated vs. aglycone) on bioavailability.
  • Discussion of advanced formulation techniques (lipid-based, cyclodextrin complexation) to improve absorption.

Main Results:

  • Glucose-conjugated isoflavones exhibit poor intestinal absorption and lower biological activity compared to aglycones.
  • Colonic microbes can convert glycosylated isoflavones into more absorbable aglycones.
  • Differences in absorption and metabolism exist between aglycone and conjugated forms of key isoflavones like genistein and daidzein.

Conclusions:

  • Understanding isoflavone metabolism and bioavailability is critical for elucidating their biological effects.
  • The chemical form of isoflavones profoundly impacts their therapeutic potential.
  • Advanced formulations are necessary to enhance isoflavone bioavailability and optimize health benefits.