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Related Concept Videos

Carrier-Mediated Transport01:06

Carrier-Mediated Transport

572
Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
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Cellular Membranes and Drug Transport01:24

Cellular Membranes and Drug Transport

1.0K
Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
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Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport01:23

Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport

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Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
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Drug Absorption Mechanism: Carrier-Mediated Membrane Transport01:19

Drug Absorption Mechanism: Carrier-Mediated Membrane Transport

4.7K
Certain large, lipid-insoluble drug molecules that resemble amino acids, peptides, or glucose, require specialized carrier proteins to facilitate their diffusion across cell membranes. This transport can occur through either facilitated diffusion, which does not require energy input, or active transport, which does require energy input.
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
4.7K
Facilitated Diffusion01:16

Facilitated Diffusion

680
The plasma membrane, a critical structure in cellular biology, houses an array of transporters, or carrier proteins, interspersed within its lipid bilayer. These proteins play a crucial role in solute transport through facilitated diffusion, a form of passive diffusion that uses transporters to move the molecules across the membrane.
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
680
Membrane Transporters01:31

Membrane Transporters

13.4K
Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
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Updated: Sep 28, 2025

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

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Cell Surface Transporters and Novel Drug Developments.

Natasha Carmichael1, Philip J R Day2,3

  • 1Faculty of Biology, Medicine and Health, The University of Manchester, Manchester, United Kingdom.

Frontiers in Pharmacology
|March 30, 2022
PubMed
Summary

Drug development faces high attrition rates. Emerging evidence suggests carrier-mediated transport, not diffusion, is key for cell entry, potentially revolutionizing drug discovery with targeted transporters and beyond Lipinski

Keywords:
aptamerschemical fragmentsdiffusiontherapeutic indextransporters

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Author Spotlight: Expression and Purification of Human Solute Carrier Transporters Using Codon-Optimized Genes
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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Computational Biology

Background:

  • High attrition rates (95%) persist in drug discovery, especially for anticancer drugs.
  • Lipinski's Rule of 5 (Ro5) guides development, but many drugs don't comply.
  • The COVID-19 pandemic accelerated drug development, prompting a re-evaluation of existing processes.

Purpose of the Study:

  • To explore novel drug development strategies beyond traditional methods.
  • To investigate the role of carrier-mediated transport in cellular drug uptake.
  • To highlight the potential of targeting cell surface transporters for improved drug efficacy and reduced toxicity.

Main Methods:

  • Review of emerging evidence on drug permeation mechanisms.
  • Analysis of computational biology's role in optimizing ADMET properties.
  • Exploration of novel drug development approaches like beyond the Rule of 5 (bRo5) and fragment-based design.

Main Results:

  • Carrier-mediated transport may be the primary mechanism for drug entry into cells, challenging the long-held belief in phospholipid bilayer diffusion.
  • Targeting cell surface transporters offers a promising route to enhance drug specificity and reduce dosage.
  • Beyond the Rule of 5 (bRo5) molecules and pulsatile drug delivery systems represent expanding frontiers in drug development.

Conclusions:

  • Exploiting cell surface transporters can significantly improve the therapeutic index of drugs.
  • A shift towards transporter-mediated drug uptake and bRo5 molecules could revolutionize drug discovery, leading to more efficient and successful outcomes.
  • Optimizing intracellular drug entry via transporters is a critical step toward reducing attrition rates in drug development.