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Related Concept Videos

Mechanically-gated Ion Channels01:12

Mechanically-gated Ion Channels

Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
Mechanically-gated Ion Channels01:12

Mechanically-gated Ion Channels

Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
Modified-Release Drug Delivery Systems: Stimuli-Activated01:30

Modified-Release Drug Delivery Systems: Stimuli-Activated

Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also called...
Cycloaddition Reactions: MO Requirements for Thermal Activation01:16

Cycloaddition Reactions: MO Requirements for Thermal Activation

Thermal cycloadditions are reactions where the source of activation energy needed to initiate the reaction is provided in the form of heat. A typical example of a thermally-allowed cycloaddition is the Diels–Alder reaction, which is a [4 + 2] cycloaddition. In contrast, a [2 + 2] cycloaddition is thermally forbidden.
Activation Energy01:26

Activation Energy

Activation energy is the minimum amount of energy necessary for a chemical reaction to move forward. The higher the activation energy, the slower the rate of the reaction. However, adding heat to the reaction will increase the rate, since it causes molecules to move faster and increase the likelihood that molecules will collide. The collision and breaking of bonds represents the uphill phase of a reaction and generates the transition state. The transition state is an unstable high-energy state...
Cycloaddition Reactions: MO Requirements for Photochemical Activation01:12

Cycloaddition Reactions: MO Requirements for Photochemical Activation

Some cycloaddition reactions are activated by heat, while others are initiated by light. For example, a [2 + 2] cycloaddition between two ethylene molecules occurs only in the presence of light. It is photochemically allowed but thermally forbidden.

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Mechanostimulation of Multicellular Organisms Through a High-Throughput Microfluidic Compression System
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Published on: December 23, 2022

Drug mechanochemical activation.

I Colombo1, G Grassi, M Grassi

  • 1Eurand S.p.A., Physical Pharmacy Laboratory, via Martin Luther King, 13-20060 Pessano con, Bornago, Milano, Italy.

Journal of Pharmaceutical Sciences
|April 2, 2009
PubMed
Summary
This summary is machine-generated.

Mechanochemical activation, a solvent-free mechanical treatment, enhances drug solubility and bioavailability, particularly for poorly water-soluble drugs. This process optimizes drug delivery systems through controlled milling conditions.

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Area of Science:

  • Materials Science
  • Pharmaceutical Technology
  • Physical Chemistry

Background:

  • Solid drug mechanochemical activation via cogrinding is a promising technique.
  • This method aims to enhance drug solubility and bioavailability.
  • It offers a solvent-free alternative to traditional drug formulation methods.

Purpose of the Study:

  • To review the theoretical background of solid drug mechanochemical activation.
  • To discuss the advantages, drawbacks, and mechanisms of this activation process.
  • To explore experimental tools and mathematical modeling for optimizing mechanochemical activation.

Main Methods:

  • Review of theoretical principles and existing literature on mechanochemical activation.
  • Discussion of experimental techniques for evaluating drug activation.
  • Analysis of mill types and mathematical modeling of mill dynamics.

Main Results:

  • Mechanochemical activation significantly improves drug solubility and bioavailability.
  • The process is solvent-free, simplifying purification and reducing costs.
  • Optimization of milling parameters (time, speed, ratio) is crucial for system properties.

Conclusions:

  • Mechanochemical activation is an effective strategy for enhancing the bioavailability of poorly water-soluble drugs.
  • This technique avoids solvent use, offering environmental and economic benefits.
  • The approach is most suitable for drugs with low solubility but good permeability.