Vanillyl Butyl Ether to Topically Induce Blood Cell Flux, Warming Sensation

Dec 1, 2010 | Contact Author | By: Ling-Chiao Chen, Shih-Jung Wu and Christina Huang, Corum Inc.
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Title: Vanillyl Butyl Ether to Topically Induce Blood Cell Flux, Warming Sensation
vanillyl butyl etherx warming agentx vasodilationx laser speckle contrast imagingx
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Keywords: vanillyl butyl ether | warming agent | vasodilation | laser speckle contrast imaging

Abstract: It has been hypothesized that vanillyl butyl ether (VBE) has the same warming and vasodilation mechanisms as capsicum. Thus, VBE was formulated at various levels into cream formulations and applied topically to the forearms of 21 individuals. Following application, changes in blood cell flux (BCF) were investigated using a laser speckle contrast imager.

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L-C Chen, S-J Wu and C Huang, Vanillyl butyl ether to topically induce blood cell flux, warming sensation, Cosm & Toil 125(12) 34-39 (Dec 2010)

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Substances known to impart a sensation of warmth upon application are called warming agents and include capsicum (red pepper), ginger extract and vanillyl alcohol alkyl ether derivatives. Capsicum is the material used most as a warming agent in personal care; however, its side effects may include skin irritation, burning, itching and possible carcinogenicity. In relation, vanillyl alcohol alkyl ether derivatives, specifically vanillyl butyl ether (VBE), was investigated as an alternative, milder warming agent for personal care applications.

Vanilloids contain vanillyl groups that bind to the transient receptor potential type V1 channel (Vanilloid receptor-1, TRPV1), a nonselective cation channel that naturally responds to noxious stimuli such as high temperatures and acidic pH. This binding of the vanilloid to TRPV1 opens the channel pore, which leads to an influx of predominantly calcium cations. In turn, this action causes membrane depolarization that, once reaching a threshold level, generates an action potential that is propagated along the axon to the synapse. Activated neurons will release glutamate, adenosine triphosphate (ATP) and a variety of neuropeptides as transmitters from the synapse. These neurotransmitters launch a cascade and eventually reach the central nervous system.

Lab Practical: Using VBE

  • The solubility of VBE with other ingredients affects the releasing level of VBE from the formulation to impart a warming sensation.
  • VBE is oil-soluble and more stable in emulsions than water solutions.
  • It is recommended that the PIT method be used to add VBE to formulations.
  • VBE should be added as the temperature approaches PIT and not after the phase inversion.

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Table 1. Summary data

Table 1. Summary data

Summary data of measurable response and average BCF increase following the topical application of VBE cream in 21 individuals

Figure 1. BCF curve of volunteer 14

Figure 1. BCF curve of volunteer 14

BCF curve of volunteer 14; x = time in minutes; y = perfusion unit (PU); flux 1 is the untreated BCF curve; flux 2 to 5 indicate the BCF curve of 0%, 0.1%, 0.3% and 0.5% VBE cream, respectively. T5 represents application at 5 min; PMax represents maximum peak of flux 5.

Figure 2. BCF image of volunteer 14

Figure 2. BCF image of volunteer 14

BCF image of volunteer 14 a) before application, and b) 22 min after application

Figure 3. BCF percent increase

Figure 3. BCF percent increase

BCF percent increase; data are mean ± SD by error bar; untreated = no cream applied; ***p < 0.001

Footnotes [Chen 125(12)]

a The moor FLPI laser speckle contrast imager is manufactured by Moor Instruments, Axminster, United Kingdom.

b The statistical and power analysis software used for this study is produced by NCSS, Kaysville, UT USA.

Formula 1. Test o/w warming cream

A. Cetyl Alcohol (and) Glyceryl Stearate (and) PEG-75 Stearate (and) Steareth-20

3.00% w/w
Hydrogenated Polydecene 3.00
Isododecane 4.20
Octyldodecyl Stearoyl Stearate 3.00
Dimethicone 2.00

B. Water (aqua)

qs to 100.00
Glycerin 2.50


C. Sodium Hydroxide 0.30
D. Vanilly Butyl Ether 0.0–0.50
E. Water (aqua) 30.00
F. Sodium Hydroxide 0.40
Methylisothiazolinone 0.10
Fragrance (parfum) 0.10
Procedure: Heat A and B separately to 80˚C. Slowly add B to A with slow stirring. After B is completely incorporated, cool and increase stirring speed. Adjust pH value with a small amount of C. After cooled to 60˚C, add D then E, with high stirring speed. After cooling to 43˚C, add F and remaining water; mix well.






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