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Related Concept Videos

Facilitated Diffusion01:16

Facilitated Diffusion

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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...
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Passive Diffusion: Overview and Kinetics01:17

Passive Diffusion: Overview and Kinetics

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Passive diffusion is a critical process that allows small lipophilic drugs to cross the cell membrane along a concentration gradient. This mechanism's efficiency depends on four primary factors: the membrane's surface area, the drug's lipid-water partition coefficient, the concentration gradient, and the membrane's thickness.
When administered orally, drugs establish a substantial concentration gradient between the gastrointestinal (GI) lumen and the bloodstream, expediting...
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Cellular Membranes and Drug Transport01:24

Cellular Membranes and Drug Transport

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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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Pore Transport and Ion-Pair Transport01:17

Pore Transport and Ion-Pair Transport

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Pore transport and ion-pair formation are critical mechanisms for the absorption and distribution of drugs in the body.
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited  but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
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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.
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Drug Absorption Mechanism: Passive Membrane Transport01:23

Drug Absorption Mechanism: Passive Membrane Transport

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Passive transport is a method of drug absorption where small, lipid-soluble drugs can move across the cell membrane. This movement happens along the concentration gradient, which is a natural flow from higher to lower concentration areas. The speed at which the drug moves is directly related to its lipid–water partition coefficient. This means that the more a drug dissolves in lipids, the faster it diffuses or spreads throughout the body. It is important to note that most drugs are either...
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Evidence that desferrioxamine cannot enter cells by passive diffusion.

J B Lloyd1, H Cable, C Rice-Evans

  • 1Department of Biological Sciences, Keele University, Staffordshire, U.K.

Biochemical Pharmacology
|May 1, 1991
PubMed
Summary
This summary is machine-generated.

Desferrioxamine enters cells solely through pinocytosis, not other mechanisms. This finding necessitates a re-evaluation of how this iron chelator works in the body.

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Area of Science:

  • Cell biology
  • Pharmacokinetics
  • Biochemistry

Background:

  • Desferrioxamine is an iron chelator used clinically.
  • Its cellular uptake mechanism is traditionally assumed to be passive diffusion or carrier-mediated transport.
  • Understanding desferrioxamine's cellular entry is crucial for its therapeutic application.

Purpose of the Study:

  • To investigate the cellular uptake mechanism of desferrioxamine.
  • To compare desferrioxamine uptake with a known fluid-phase pinocytosis marker.
  • To determine the intracellular fate of desferrioxamine.

Main Methods:

  • In vitro study using rat visceral yolk sac.
  • Comparison of [14C]desferrioxamine and [14C]sucrose accumulation kinetics.
  • Assessment of inhibitor effects on substrate uptake.

Main Results:

  • Kinetic parameters for desferrioxamine and sucrose were similar.
  • Inhibitor effects on both substrates were comparable.
  • Desferrioxamine uptake was consistent with fluid-phase pinocytosis.
  • Internalized desferrioxamine was localized in lysosomes.

Conclusions:

  • Desferrioxamine enters cells exclusively via pinocytosis.
  • Desferrioxamine is retained within lysosomes after cellular uptake.
  • Current pharmacokinetic models for desferrioxamine's iron depletion require re-evaluation.