Title Image

SLOW RELEASE ESSENTIAL OILS

A NEW GENERATION OF NUTRITIONAL + COSMETIC PROGRAMS CONTAINING LONG ACTING – SLOW RELEASE ESSENTIAL OILS

 

Note: These programs are based on thorough scientific research, their efficacy is pharmacologically & scientifically proved, the key discoveries are patented, published, and this research work received the European PAEXA award & French Academy of Science award.

DISCOVERY OF LONG ACTING – SLOW RELEASE EOs

 

Use of ESSENTIAL OILS (EOs) in Ayurveda

Introduction: Aromatherapy is now becoming one of the major complementary therapies which use essential oils, internally & externally as major therapeutic agents to treat several diseases. The global essential oils market size was valued at US$ 6.63 billion in 2016, growing at a CAGR of 9.7%. A market research study by Grand View Research estimates that the global essential oils market is expected to reach $11.67 billion by 2022.

The use of EOs was very common since Ayurvedic period and remains common today.

Ayurveda considered Eos as “Agni” or “Fire” (as they are highly concentrated pure fire elements of a plant) and suggested using only in very small quantities as aromatherapy, perfumes or massage but never “internally”.  Modern medicine is using EOs internally & externally, usually in high concentrations without any proofs of their safety. Only since last few years, the concern over the safety of EOs is becoming a major concern in all the developed countries.

These aromatic molecules are very potent organic volatile chemicals that make even the surroundings free from parasites, bacteria, viruses and fungi. Their efficacy as antibacterial, antiviral, anti-inflammatory; force, muscle, mood, memory, circulation, & immunity-booster, is documented scientifically.

Regulatory concerns over the use of Essential Oils!

EU is now concerned with EO vapour toxicity & side effects! It started with the allergens, in 2002, which was the reason for the foundation of EFEO – the European Federation of Essential Oils. Because of this regulation, several end users decided to change their formulas and minimized using substances containing allergens. Then came the REACH Cosmetic Regulation EC N° 1223/2009, with many more restrictions for marketing EOs in cosmetics.

Even if EOs are diluted before use, they are applied on live skin. Skin is keratinized and doesn’t allow substances to enter easily into the body. EOs contain high concentrations of 100s of chemicals such as a-pinene, canfene, β-pinene, Sabinene, β-myrcene, a-felandrene, limonene, β-felandrene, g-terpinene, β-ocimene, a-ocimene, linalool, caryophyllene, terpinen-4-ol, azulene derivative, a-humelene, a-terpineol, germacrene D, bicyclogermacrene, isoledene, g-cadinene, d-cadinene, copaene, elemene, caryophilene oxide, spathulenol, eudol, germacrone, unidentified sesquiterpene alcohol, epi-bicyclosesquiphelandrene, Α-cadinol, elemol, neril hexanoate, g-eudesmol, g-cadinol, unidentified sesquiterpenes, …

Traditional use suggests that they are probably not harmful to the health but their toxicity, mutagenicity, and carcinogenicity were never studied.

They are highly volatile and 50% oil evaporates within a few minutes, as shown below (see: https://link.springer.com/article/10.1007/BF02324825).

50% evaporation rate in minutes: Sandalwood: 46 min; Jasmin absolute: 46 min; Patchouli: 28.5 min; Cloves: 29 min; Anise: 24.5 min; Rose: 23.5 min; Geranium: 22.5 min; Ylang-Ylang: 22 min; Citronella: 19.5 min; Fennel seed: 19.5 min; Clary sage: 17 min; Coriander: 15.5 min; Peppermint: 15.5 min; Lavender: 13 min; Dillweed: 10.5 min; Bergamot: 9 min; Orange: 8.5 min; Mandarin: 6 min.

The key problems with the use of current diluted EOs are:

  1. Poor absorption / poor efficacy,
  2. Limited duration of activity but flash absorption (max within 10-50 min after skin application) instead of slow release to minimize side effects and to maximize efficacy,
  3. More oil (nearly 90%) is volatilized and enters the body through the lungs than is acting topically where it was applied,
  4. Nearly instant release of 100’s of chemicals in the air with unknown toxicity / side effects,
  5. High chances of toxicity due to sudden high blood/air concentration, if inhaled.
  6. Not being fatty, aromatic oils do not spread well on a large skin surface. Mixed with a carrier, they are poorly absorbed.

What the September 2018 EU guidelines may change?

Not known yet, but surely those guidelines shall:

  • further reduce the concentration limits for use, in order to minimize air evaporation and sudden peak of unknown chemicals absorbed from the air (using low concentrations, however, may lead to more frequent/multiple applications),
  • call for stopping the use in children & pregnant women altogether

(we will update this section in September 2018).

Development of specific low-concentration, slow release, long-acting, filmogen Essential Oil (EO) formulations

Not only due to the absence of novelty in this field, but also due to changing regulations and the probability of withdrawal of many currently best-selling EO formulations at the end of the year, we launched a R&D program with the objective to find new EO formulations which:

  • could be used in low concentrations, as per the legislation/regulations,
  • could remain over the biological surface (skin, mucosa) over a period of at least 4-6h, so as to deploy their therapeutic potential;
  • could be released slowly into the biological tissue;
  • are not volatilized within an hour;
  • are not irritant & have very few/slight side effects, due to the low concentrations used / absorbed.

R&D PROGRAM

  • Phase 1: Searching for an EO-storing, non-irritant film for topical application

The initial R&D phase was concentrated mainly on searching for an ingredient with hydrating and slow-fading filmogen properties, capable to trap EOs for slow release.

To achieve these objectives, it was not possible to use any ingredient which is a chemical, which does not trap but absorbs essential oils, which has a density lower than the density of EOs (ex: normal or salted water, saline, since EOs float in water), which may interact with EOs, and which may have any pharmacological, metabolic, receptor, immunological or biological interaction with the underlying live tissue.

The secondary objective was to render the film adherent & resistant to mechanical pressures.

After testing different filmogen substances for their cellular interaction and cellular toxicity using in vitro cell culture models, we identified some natural, cell-friendly, filmogen ingredients:

  • plant-based
  • sugar-based (ex. sucrose, glucose, fructose, saccharose)
  • sugar–alcohol-based solutions

Finally, we conceived as a viscous, colorless, odorless, solution with humectant properties. It had no interactions with any EOs and the film was capable of trapping EOs. This solution was patented worldwide.

Disadvantages of VD-binder film:

  1. The product was poorly filmogen as it disintegrated within 90-120 minutes because of its humectant properties.
  2. The EO release was prolonged up to 1.5-2h, but it was not satisfactory enough.

 

  • Phase 2: Improving the duration of retention of the film

 

To improve the duration of film retention, so as to avoid frequent EO applications and to allow slow EO release, multiple experiments were conducted, adding different substances into the standard VD-binder solution.

We observed that some natural and synthetic polymers, which are very big, branched and inert molecules, have the properties to bind specifically with VD-binder macromolecules without interacting with EOs.

This binding improved the film resistance and flexibility to mechanical pressures. The duration of retention over a live biological surface was improved up to 4-6h.  The EO-incorporating film was designated “F-VD-binder” film.

The desired quantities of selected Ayurvedic EOs were incorporated in the F-VD-binder film to conceive a new, slow-release device for EOs.

This research was conducted in collaboration with Inflamlab, University of Toulouse, France.

Phase 3: Verifying speed of EO release from F-VD-binder film

These experiments were conducted at LEXVA Laboratoire Analytique, St Beauzire in France.

Example:

Aim: To compare the release of Eucalyptus EO, the EO was mixed in water or in F-VD-binder solution at a concentration of 0.20% and kept overnight. The concentration of volatile compounds (Alpha-Pinene, Limonene, and Eucalyptol) was quantified through aqueous phase GC / FID chromatography on a semi-polar column after 20h storage. The concentrations were determined by measuring the area covered compared to water control.

The following mean results were obtained:

Blue curve: Saline solution + EO; Orange curve: F-VD-binder  + EO

Component Alpha pinene Limonene Eucalyptol
Mean area M1 (EO mixed in water) 1032.288       298.375  1.209 e4
Mean area M2 (EO mixed in F-VD-binder)   242.527         69.077    160 e4
% decrease in EO release vs water solution –          76.55% –          76.84% –          86.76%

These results show that when incorporated in a filmogen F-VD-binder solution, the EO volatility decreases 4-5 times, compared to the same concentration of EO in another non-filmogen solution.

The filmogenicity of F-VD-binder was also determined in vitro by applying the film over live skin tissue (n=6 each) and washing the film with the culture medium (isotonic liquid) at 6h intervals. Depending upon the concentration of VD-binder in F-VD-binder film, the mechanical resistance of the film could be increased 5 to 6-fold (maximum effects between 40-50% VD-binder concentration in water).

Slow-release & long-acting essential oil formulations

Based on these findings, we conceived a range of topical EO preparations, containing 1 or more EOs for each specific pathology to be treated.

Precautions: In the absence of scientific data to demonstrate safety, the use of essential oils is not recommended in pregnant women & children below 8 of age.

Conclusion: To take full advantage of the beneficial properties of EO by topical application, the EOs were incorporated in a filmogen liquid. The EO evaporation and in consequence their concentration was reduced 4-5 times. The efficacy was improved due to long term adherence, environmental & pulmonary contamination was highly minimized. Long acting & slow release EO formulations should represent the 1st and one of the major improvement in EO therapy

NUTRITIONAL & EO PROGRAMS BASED ON THESE DISCOVERIES

Why a program containing a nutritional supplement & a cosmetic?

Because Ayurveda suggests acting:

  • Internally & Externally (to prepare a healthy ground 1st)
  • On the cause & the symptoms

These preparations usually contain a synergistic association of “Earth elements”, Plant Extracts and Essential Oils, which cannot be mixed easily. Therefore, the solids are presented as nutritional supplements & the Essential Oils as cosmetic preparations.

PRESENTATION:

Each program containing 2 packs:

  1. Slow-release Essential Oil spray (2-3 sprays twice /d)
  2. A container or strips with 60 or 90 vegetal capsules (2-4 caps/d)

Note: These programs are manufactured in France under GMP or ISO13485 norms.

Complete program is presented in a box which may contain capsules (variable presentation) & an essential oil spray for each pathology. Examples: