Optimizing Ingredients

The Case for Sustained-Release Caffeine

Numerous studies have shown that caffeine is the most cost efficient method of delivering energy. Caffeine, as an energy source, has been well studied. Caffeine has been used for centuries and is an old compound.

How does Caffeine work?

Caffeine, once absorbed, readily crosses the blood–brain barrier that separates the bloodstream from the interior section of the brain. Once inside the brain, the principal mode of action for Caffeine is as a nonselective antagonist of adenosine receptors. Adenosine is a key endogenous molecule that regulates tissue function. The caffeine molecule is structurally similar to adenosine, and binds to adenosine receptors on the surface of cells without activating them. In this case, it is classified as an antagonist. Therefore, caffeine acts as a competitive inhibitor.

Caffeine is known to boost the effects of the neurotransmitters serotonin, dopamine and acetylcholine. Dopamine is known to affect levels of concentration. Dopamine blocks adenosine receptors in the brain, which when not interfered with these receptors, are what typically signal the brain when it’s time to go to bed. Caffeine also increases the release of catecholamines through the sympathetic nervous system, which among other things can increase heart rate, send more blood to the muscles and signal to the liver to release sugar into the bloodstream for energy.

Caffeine impacts thermogenesis.

Research studies have documented favorable biological changes when Caffeine is administered. These changes, such as, increased metabolic rate, increased fat oxidation and a perception of increased physical and mental energy, even while recognizing that excess caffeine leads to jitteriness and sleeplessness. Studies have shown that Caffeine at commonly consumed doses can have a significant influence on energy balance and may promote thermogenesis in the treatment of obesity. Hence the interest in Caffeine in weight management!

Sustained release delivery of Caffeine without the crash.

Recently, there have been calls from different entities to ban Caffeine or to prevent its use in different applications. Again, Caffeine is an old bioactive ingredient. The calls for more regulation of Caffeine have been exacerbated because of its ability to cause jitteriness and the traditional Caffeine crash. Use of sustained release or timed release Caffeine can be used to avoid jitteriness and the typical Caffeine crash. The dissolution curve below clearly shows sustained release of Caffeine when microencapsulation is used to coat each particle of Caffeine with a thin food grade film.


Microencapsulation, as a technology, is being used to deliver timed released tasteless bitter-free Caffeine over periods of 2, 4, 6, 8 and 12 hours. Microencapsulation is therefore an effective tool for delivery of sustained or timed released energy from Caffeine. This tool is also used to mask the bitter undesirable taste of Caffeine.

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