WO2025155269A1

WO2025155269A1 - Serum containing encapsulated niaouli essential oil

Info

Publication number: WO2025155269A1
Application number: PCT/TR2024/051822
Authority: WO
Inventors: Evrim AKYIL; Sinan OZER; Nilay DOGAN
Original assignee: Anadolu Universitesi; Istanbul Medipol Universitesi
Current assignee: Anadolu Universitesi; Istanbul Medipol Universitesi
Priority date: 2024-01-16
Filing date: 2024-12-27
Publication date: 2025-07-24
Anticipated expiration: 2026-07-16
Also published as: TR2024000493A2

Abstract

The invention relates to serum containing encapsulated niaouli essential oil. In the preparation of said serum, firstly niaouli essential oil is encapsulated and then the obtained micro/nanoparticles are loaded into the serum carrier system. The serum containing encapsulated niaouli essential oil, which is the subject of the invention, contains olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate and encapsulated niaoulii essential oil. The serum containing encapsulated niaouli essential oil is used as a new alternative treatment method for eczema treatment.

Description

SERUM CONTAINING ENCAPSULATED NIAOULI ESSENTIAL OIL

Technical Field

The invention relates to serum containing encapsulated niaouli essential oil. In the preparation of the serum, firstly niaouli essential oil is encapsulated and then the obtained micro/nanoparticles are loaded into the serum carrier system.

State of the Art

In the medical world, in addition to modern medical practices, studies on the development of alternative and complementary traditional treatment methods are increasing. Aromatherapy is one of the therapies that use essential oils to prevent and treat various diseases among complementary medical practices. Essential oils are natural, volatile and complex compounds found in aromatic plants, known for their strong odours, and are components obtained from plants by steam or water distillation [1 ]. In aromatherapy, treatment is performed using essential oils or herbal drugs that carry essential oils as the main active ingredient [2], In the field of dermatology, the use of aromatherapy and essential oils is used as antimicrobial, antitumour, antiinflammatory agents in acne vulgaris, bacterial infections, fungal infections, burns, wound healing, alopecia areata, eczematous, atomic eczema and some other diseases. Atopic dermatitis (atopic eczema) is a chronic, recurrent, itchy and inflammatory skin disease. It is possible to use essential oils in drug delivery systems in the treatment of these dermatological diseases with encapsulation. Encapsulation is a technology that allows solid, liquid and gas materials to be kept in capsules by coating them, protecting a very small substance or the entire component, and allowing them to be released under specific conditions and at specific speeds. Niaouli essential oil (Melaleuca Viridiflora) is an essential oil obtained by steam distillation from fresh leaves of Melaleuca Vi rich flora from the Myrtaceae family. Niaouli essential oil contains high levels of monoterpenes and sesquiterpenes [3]. Niaouli essential oil is a volatile oil source rich in 1 ,8-cineole and is used in pharmaceutical preparations and in different areas of aromatherapy for the treatment of cough and cold, rheumatism and neuralgia [4]- In the state of the art, corticosteroids are used in the treatment of eczema, which is a chronic and inflammatory skin disease. However, in patients who initially improve with topical corticosteroid use, symptoms may worsen after a certain period of time and changes in the clinical disease pattern may occur. Therefore, in patients receiving eczema treatment, the risk of recurrence and worsening of symptoms after treatment cannot be prevented.

In another state of the art practice, essential oils are used in dermatological treatments and diseases that occur on the skin, such as eczema. In this method, a cream/gel product containing formulations of essential oils is applied to the skin. However, in this application method, there may be interactions between the essential oils in the formulation content and environmental factors such as pH, oxygen, humidity, light and heat. In this case, the risk of interactions with environmental factors that limit the use of essential oils in dermatological treatment cannot be prevented.

In another state of the art, essential oils are used by applying them directly to the skin surface where eczema occurs. However, this application has disadvantages such as direct contact of essential oils with the skin, causing the skin problem to progress worse. For this reason, the risk of skin irritation and worsening of skin problems cannot be prevented when using essential oils in dermatological treatment.

The limitations and inadequacies of the solutions in the state of the art, the risk of recurrence and worsening of symptoms after treatment with the use of corticosteroids in eczema treatment, the risk of interactions with environmental factors that limit the use of essential oils in dermatological treatment, the problem of skin irritation due to direct contact of essential oils with the skin in eczema treatment, and the disadvantages such as causing the skin problem to progress worse, have necessitated making a development in this area.

Brief Description and Aims of the Invention

The invention relates to serum containing encapsulated niaouli essential oil. In the preparation of the serum of the invention, firstly niaouli essential oil is encapsulated and then the obtained micro/nanoparticles containing niaouli essential oil are loaded into the serum carrier system. The serum containing encapsulated niaouli essential oil of the invention contains olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate, ethyl acetate copolymer and encapsulated niaouli essential oil.

One of the aims of the invention is to increase the stability and effectiveness of essential oils in formulations used in the treatment of eczema. By loading the encapsulated niaouli essential oil of the invention into modern drug carrier systems, the stability and effectiveness of the formulation developed for use in dermatological treatments are increased.

Another aim of the invention is to provide a solution to the problem of skin irritation caused by direct contact of essential oils with the skin in dermatological treatments. Since the serum containing the encapsulated niaouli essential oil is encapsulated and the micro/nanoparticles are loaded into the serum carrier system, direct contact of the essential oil in its content to the skin is prevented and no irritation problem occurs on the skin.

Another aim of the invention is to prevent the restriction of the use of essential oils used in dermatological treatments due to their interaction with environmental factors and stability problems. The serum containing the encapsulated niaouli essential that is the subject of the invention does not interact with environmental factors such as pH, oxygen, humidity, light and heat by loading the micro/nanoparticles into the serum carrier system. In addition, niaouli essential oil is encapsulated in order to eliminate the stability problems that arise due to the fact that niaouli essential oil is a volatile oil and the irritating properties of essential oils.

Another aim of the invention is to provide prolong effectiveness of essential oils used in dermatological treatment content. The fact that the serum system containing encapsulated niaouli essential oil, which is the subject of the invention, can remain on the skin for a long time without forming an oily texture increases the absorption period and thus the effectiveness period of the essential oil is increased. The use of this encapsulated niaouli essential oil serum as a new alternative treatment method for eczema treatment minimises the factors that restrict its use by increasing the effectiveness and stability of the active ingredient niaouli essential oil.

Description of Drawings

Figure 1. Preparation method of serum containing encapsulated niaouli essential oil

Description of Reference Numbers:

1 . Niaouli essential oil, ethyl acetate copolymer, acetone

2. Micro/nanoparticle

3. Spray solution

4. Collection container

5. Inlet air

6. Heater

7. Pump

8. Spray solution

9. Drying area

10. Spray

1 1 . Outlet air

12. Cyclone collector

13. Collection container

Detailed Description of the Invention

The invention relates to serum containing encapsulated niaouli essential oil for use in dermatological treatments. The serum containing encapsulated niaouli essential oil, which is the subject of the invention, contains olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate, ethyl acetate copolymer and encapsulated niaouli essential oil.

In the preparation of the serum containing encapsulated niaouli essential oil, which is the subject of the invention, firstly niaouli essential oil is encapsulated and then the obtained micro/nanoparticles containing niaouli essential oil are loaded into the serum carrier system. The serum containing encapsulated niaouli essential oil, which is the subject of the invention, can be used as a new alternative treatment method for eczema treatment. By encapsulating the serum containing encapsulated niaouli essential oil, which is the subject of the invention, and loading the micro/nanoparticles into the serum carrier system, it does not interact with environmental factors such as pH, oxygen, humidity, light and heat and does not come into direct contact with the skin. Thus, irritations resulting from direct contact of the essential oil on the skin are also prevented. The ability of the serum system to remain on the skin for a long time without creating an oily texture increases the absorption time and in this case, niaouli essential oil shows its effectiveness for a longer time.

Production method of the serum containing encapsulated niaouli essential oil which is the subject of the invention comprises the process steps of: i) preparing spray solution containing ethyl acetate copolymer, niaouli essential oil and acetone, ii) obtaining encapsulated niaouli essential oil in the form of micro/nanoparticles containing niaouli essential oil by spray drying the spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil, iii) preparing a mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate to which micro/nanoparticles containing niaouli essential oil will be added, iv) adding micro/nanoparticles containing niaouli essential oil to the mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate, v) dispersing micro/nanoparticles containing niaouli essential oil in the mixture homogeneously by simple mixing method, and vi) preparing serum formulation containing olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate, and encapsulated niaouli essential oil.

In one embodiment of the invention, the production method of the serum containing encapsulated niaouli essential oil comprises the process steps of: i) preparing spray solution containing ethyl acetate copolymer, niaouli essential oil and acetone, ii) obtaining encapsulated niaouli essential oil in the form of micro/nanoparticles containing niaouli essential oil by spray drying the spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil, iii) preparing a mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate to which micro/nanoparticles containing niaouli essential oil will be added, iv) weighing micro/nanoparticles containing niaouli essential oil at a rate of 0.88% (w/w) of the total amount of the mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate, and adding them to the mixture, v) dispersing micro/nanoparticles containing niaouli essential oil in the mixture homogeneously by simple mixing method, and vi) preparing serum formulation containing olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate, and encapsulated niaouli essential oil.

Preparation method of spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil used in the production of serum containing encapsulated niaouli essential oil, which is the subject of the invention, comprises the process steps of: i) dissolving ethyl acetate copolymer in acetone using a magnetic stirrer, ii) adding niaouli essential oil to the solution after preparing the solution containing ethyl acetate copolymer and acetone, and iii) mixing the solution containing ethyl acetate copolymer, acetone and niaouli essential oil. in one embodiment of the invention, the preparation method of spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil used in the production of serum containing encapsulated niaouli essential oil comprises the process steps of: i) dissolving 0.1 -6 g of ethyl acetate copolymer in 50-200 mL of acetone at 20-1500 rpm on a magnetic stirrer at room temperature, ii) adding 0.1 -10 mL of niaouli essential oil after preparing the solution containing ethyl acetate copolymer and acetone, and iii) mixing the solution containing ethyl acetate copolymer, acetone and niaouli essential oil at a speed of 20-1500 rpm for another 2-60 minutes.

The content of the spray solution used in the spray drying stage of the micro/nanoparticles containing the niaouli essential oil of the invention is explained in Table 1 . The contents of the serum mixture without the addition of micro/nanoparticles containing said niaouli essential oil are explained in Table 2.

Table 1 : Spray solution content

Table 2: Serum mixture without micro/nanoparticles containing Niaouli essential oil

The spray solution used in the preparation of the serum containing encapsulated niaouli essential oil, which is the subject of the invention, contains ethyl acetate copolymer, niaouli essential oil and acetone.

In one embodiment of the invention, the spray solution used in the preparation of the serum containing niaouli essential oil of the invention contains 0.1 -3% ethyl acetate copolymer, 0.1 -6% niaouli essential oil and 100 mL acetone.

In another embodiment of the invention, the spray solution used in the preparation of the serum containing niaouli essential oil of the invention contains 0.1 -5 g ethyl acetate copolymer (g), 50-200 mL acetone, and 0.1 -10 mL niaouli essential oil. The content of the serum formulation containing encapsulated niaouli essential oil of the invention is explained in Table 3.

Table 3: Serum formulation content

In the production method of the serum containing encapsulated niaouli essential oil, which is the subject of the invention, the spray drying method is used in the encapsulation of niaouli essential oil. Spray drying is carried out at 40-120°C temperature, 1 -4 pump levels, 60-100% spray percentage, and 30-58 bar pressure.

The oil amount determination analysis of the micro/nanoparticles containing encapsulated niaouli essential oil, which is the subject of the invention, has been performed. The micro/nanoparticles containing encapsulated niaouli essential oil, which is the subject of the invention, contain 0.2-10% niaouli essential oil by weight.

The serum containing encapsulated niaouli essential oil, which is the subject of the invention, for use in dermatological treatments, contains olive oil, caprylic/capric triglyceride, ethyl acetate copolymer, cyclopentasiloxane, isopropyl myristate, and encapsulated niaouli essential oil.

In one embodiment of the invention, the serum containing encapsulated niaouli essential oil, which is the subject of the invention, contains 44.06% olive oil, 26.45% caprylic/capric triglyceride, 10.97% ethyl acetate copolymer, 8.82% cyclopentasiloxane, 8.82% isopropyl myristate, and 0.88% encapsulated niaouli essential oil.

In order to investigate the stability of micro/nanoparticles containing niaouli essential oil in the formulation, two equal mixtures were prepared. A amount of micro/nanoparticles containing niaouli essential oil was added to one of the mixtures, and an equal amount of pure (uncoated) niaouli essential oil was added to the other as the amount encapsulated by A amount of micro/nanoparticles. Both formulations obtained were mixed using a simple mixing method until they showed a homogeneous dispersion. Both formulations were weighed at time 0 and left in 4°C, 25°C and 40°C stability cabinets with their caps open and weighed again at certain intervals. Since niaouli is a volatile component, the mass differences resulting from its evaporation were evaluated and it was observed that micro/nanoparticles containing niaouli essential oil could store niaouli essential oil in the formulation for a longer time compared to niaouli essential oil added purely.

REFERENCES

[1] Bakkali F, Averbeck S, Averbeck D, Idaomar M. Biological effects of essential oils - a review. Food Chem Toxicol 2008; 46: 46-475.

[2] Tatli I. Dogal Aromaterapbtik Yaglar ile Cilt Terapisi. Turkiye Klinikleri J Cosm Dermatol-Special Topics 2012; 5(4): 46-53.

[3] Bombarda, L, Raharivelomananal , P., Ramanoelina, P., Faure R., Bianchini, J. P., Gaydou, E. M., (2001 ). Spectrometric identifications of sesquiterpene alcohols from niaouli (Melaleuca quinquenervia) essential oil, Analytica Chimica Acta 447 113-123.

[4] Elliot, W.R., Jones, D.L., (1993). Encyclopaedia of Australian Plants Suitable for Cultivation, vol. 6. Lothian, Melbourne, pp. 315-317, 359.

Claims

1. The serum containing encapsulated niaouli essential oil for use in dermatological treatments, comprising olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate, ethyl acetate copolymer and encapsulated niaouli essential oil.

2. The serum containing encapsulated niaouli essential oil according to Claim 1 , wherein it is use in the treatment of eczema.

3. The serum containing encapsulated niaouli essential oil according to Claim 1 , comprising 44.06% olive oil, 26.45% caprylic/capric triglyceride, 8.82% cyclopentasiloxane, 8.82% isopropyl Myristate, and 0.88% encapsulated niaouli essential oil.

4. The preparation method of the serum containing encapsulated niaouli essential oil according to any of the previous claims, comprising the process steps of: i. preparing spray solution containing ethyl acetate copolymer, niaouli essential oil and acetone, ii. obtaining encapsulated niaouli essential oil in the form of micro/nanoparticles containing niaouli essential oil by spray drying the spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil, iii. preparing a mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate to which micro/nanoparticles containing niaouli essential oil will be added, iv. adding micro/nanoparticles containing niaouli essential oil to the mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate, v. dispersing micro/nanoparticles containing niaouli essential oil in the mixture homogeneously by simple mixing method, and vi. preparing serum formulation containing olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate, and encapsulated niaouli essential oil.

5. A method according to claim 4, comprising the process steps of: i. preparing spray solution containing ethyl acetate copolymer, niaouli essential oil and acetone, ii. obtaining encapsulated niaouli essential oil in the form of micro/nanoparticles containing niaouli essential oil by spray drying the spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil, iii. preparing a mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate to which micro/nanoparticles containing niaouli essential oil will be added, iv. weighing micro/nanoparticles containing niaouli essential oil at a rate of 0.88% (w/w) of the total amount of the mixture of olive oil, caprylic/capric triglyceride, cyclopentasiloxane, and isopropyl myristate, and adding them to the mixture, v. dispersing micro/nanoparticles containing niaouli essential oil in the mixture homogeneously by simple mixing method, and vi. preparing serum formulation containing olive oil, caprylic/capric triglyceride, cyclopentasiloxane, isopropyl myristate, and encapsulated niaouli essential oil.

6. The preparation method of the serum containing encapsulated niaouli essential oil according to Claim 4, comprising, in the preparation of spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil, the process steps of: i. dissolving ethyl acetate copolymer in acetone using a magnetic stirrer, ii. adding niaouli essential oil to the solution after preparing the solution containing ethyl acetate copolymer and acetone, and iii. mixing the solution containing ethyl acetate copolymer, acetone and niaouli essential oil.

7. The preparation method of the serum containing encapsulated niaouli essential oil according to Claim 4, comprising, in the preparation of spray solution containing ethyl acetate copolymer, acetone and niaouli essential oil, the process steps of: i. dissolving 0.1 -6 g of ethyl acetate copolymer in 50-200 mL of acetone at 20-1500 rpm on a magnetic stirrer at room temperature, ii. adding 0.1 -10 mL of niaouli essential oil after preparing the solution containing ethyl acetate copolymer and acetone, and iii. mixing the solution containing ethyl acetate copolymer, acetone and niaouli essential oil at a speed of 20-1500 rpm for another 2-60 minutes.

8. The preparation method of the serum containing encapsulated niaouli essential oil according to Claim 4, wherein the spraying solution in process step (i) contains 0.1 -3% ethyl acetate copolymer, 0.1 -6% niaouli essential oil and 100 mL acetone.

9. The preparation method of the serum containing encapsulated niaouli essential oil according to Claim 4, wherein the spraying solution in process step (i) contains ethyl acetate copolymer, acetone, and niaouli essential oil.

10. The preparation method of the serum containing encapsulated niaouli essential oil according to Claim 4, wherein the spraying solution in process step (i) contains 0.1 -5 g of Ethyl acetate copolymer (g), 50-200 mL of acetone, 0.1 -10 mL of niaouli essential oil.

11. The preparation method of the serum containing encapsulated niaouli essential oil according to Claim 4, wherein the micro/nanoparticles in process step (ii) contain 0.2-10% by weight of niaouli essential oil.

12. The preparation method of the serum containing encapsulated niaouli essential oil according to Claim 4, wherein the spray drying in process step (ii) is done at 40-120°C temperature, 1 -4 pump level, 60-100% spray percentage, and 30-58 bar pressure.

13. Micro/nanoparticle in which the niaouli essential oil obtained in process step (ii) of a method according to claim 4 is encapsulated into the ethyl acetate copolymer.

14. A micro/nanoparticle according to claim 12, comprising 0.2-10% niaouli essential oil by weight.

15. Serum comprising a micro/nanoparticle according to claim 12.