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Related Concept Videos

Tight Junctions01:29

Tight Junctions

6.8K
Tight junctions are molecular seals between cells that prevent the leaking of fluids, ions, and other small solutes across cavities and compartments in multicellular organisms. They are mainly composed of claudin and occludin transmembrane proteins, and other proteins such as tricellulin and JAM (junctional adhesion molecule). All these proteins are 4-pass transmembrane proteins, except JAM, which is a single-pass transmembrane protein belonging to the immunoglobulin superfamily. The...
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Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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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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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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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...
332
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

358
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...
358
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

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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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Overview of Cell-Cell Junctions01:14

Overview of Cell-Cell Junctions

19.1K
The complex three-dimensional arrangement of cells in any multicellular organism is defined and maintained by interactions of cells with each other and the extracellular matrix. Cell-cell junctions are specialized structures where the multi-protein complexes on one cell interact with the multi-protein complexes on another  cell. These cell junctions are classified  into three main types based on their function — occluding, anchoring, and gap junctions.
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Related Experiment Video

Updated: May 2, 2026

Functional Assessment of Intestinal Tight Junction Barrier and Ion Permeability in Native Tissue by Ussing Chamber Technique
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Recent progress in tight junction modulation for improving bioavailability.

Daniel Saaber1, Sabrina Wollenhaupt, Knut Baumann

  • 1Technische Universität Braunschweig, Institut für Pharmazeutische Technologie , Mendelssohnstr. 1, Braunschweig 38106 , Germany s.reichl@tu-bs.de.

Expert Opinion on Drug Discovery
|February 25, 2014
PubMed
Summary
This summary is machine-generated.

Novel drugs often have low bioavailability, but tight junction (TJ) modulation offers a solution. This approach enhances drug absorption and has potential applications in diseases with impaired barrier function, paving the way for new therapies.

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Area of Science:

  • Pharmacology
  • Biotechnology
  • Drug Delivery

Background:

  • Many novel drugs (Biopharmaceutics Classification System Class III/IV) exhibit poor bioavailability.
  • Tight junction (TJ) modulation presents a viable strategy to enhance the absorption of such pharmaceutical compounds.
  • Dysfunctional barrier integrity and TJ dysregulation in certain diseases create a therapeutic opportunity for TJ modulators.

Purpose of the Study:

  • To review current TJ modulators (AT1002, PN159, labradimil).
  • To summarize their effects on TJs, adverse events, and clinical trial outcomes.
  • To explore the current understanding of TJ regulation and future development opportunities for novel TJ modulators.

Main Methods:

  • Literature review of existing TJ modulators.
  • Analysis of clinical trial data for AT1002, PN159, and labradimil.
  • Synthesis of current knowledge on TJ regulation pathways.

Main Results:

  • AT1002, PN159, and labradimil demonstrate varying effects on TJs and clinical efficacy.
  • Adverse effects and successes in clinical trials are documented for each modulator.
  • The review highlights challenges and opportunities in developing new TJ modulators.

Conclusions:

  • Mechanism-based (MB) TJ modulators represent a promising area for pharmaceutical research.
  • MB approaches are anticipated to yield the most significant future advancements.
  • Further research into TJ signaling pathways and regulation is crucial for advancing MB TJ modulator development.