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Related Concept Videos

Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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...
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...
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: Overview01:17

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...
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...

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Bioavailability of curcumin: problems and promises.

Preetha Anand1, Ajaikumar B Kunnumakkara, Robert A Newman

  • 1Cytokine Research Laboratory and Pharmaceutical Development Center, Department of Experimental Therapeutics, The University of Texas M. D. Anderson Cancer Center, Houston, Texas 77030, USA.

Molecular Pharmaceutics
|November 15, 2007
PubMed
Summary

Curcumin, a compound from turmeric, shows anti-inflammatory and antioxidant benefits but has poor bioavailability. Researchers are developing methods like nanoparticles and analogues to enhance its absorption for treating various diseases.

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Area of Science:

  • Pharmacology
  • Natural Products Chemistry
  • Medicinal Chemistry

Background:

  • Curcumin, derived from turmeric, exhibits significant anti-inflammatory, antioxidant, antiproliferative, and antiangiogenic properties.
  • Clinical trials confirm curcumin's safety in humans, even at high doses (12 g/day).
  • Poor bioavailability, attributed to low absorption, rapid metabolism, and systemic elimination, limits curcumin's therapeutic potential.

Purpose of the Study:

  • To review strategies for enhancing curcumin bioavailability.
  • To highlight the therapeutic efficacy of curcumin across various diseases.
  • To discuss the future prospects of curcumin as a therapeutic agent.

Main Methods:

  • Review of literature on curcumin bioavailability enhancement techniques.
  • Analysis of studies investigating curcumin's therapeutic applications.
  • Examination of clinical trial data regarding curcumin safety and efficacy.

Main Results:

  • Several approaches to improve curcumin bioavailability have been explored, including adjuvants (e.g., piperine), liposomal formulations, nanoparticles, phospholipid complexes, and structural analogues (e.g., EF-24).
  • Structural analogues like EF-24 demonstrate rapid absorption and a favorable plasma half-life.
  • Despite bioavailability challenges, curcumin has demonstrated therapeutic benefits in cancer, cardiovascular diseases, diabetes, arthritis, neurological disorders, and Crohn's disease.

Conclusions:

  • Enhancing curcumin's bioavailability is crucial for maximizing its therapeutic impact.
  • Ongoing research into novel delivery systems and analogues promises to overcome current limitations.
  • Improved bioavailability is expected to position curcumin as a leading therapeutic agent for numerous human diseases.