COMPOSITION FOR THE TREATMENT OF COVID-19 AND TREATMENT METHOD

Abstract

New formulation to be used in the treatment and prevention of infections caused by COVID-19 and other coronaviruses, consisting of a food supplement the main active ingredient of which is liposome-encapsulated lactoferrin. As secondary active ingredients, it includes zinc salt and vitamin C, also encapsulted in liposomes. This composition is intended to be used as a treatment for mild or acute cases of COVID-19, and to prevention infection by those who are not infected.

Claims

1. A composition to be used for treatment and prevention of infections caused by COVID-19 and other coronavirus, characterized by containing liposomal 5 lactoferrin as the main active ingredient.

2. A composition to be used for treatment and prevention of infections caused by COVID-19 and other coronavirus, according to claim 1, characterized by the fact that the concentration of liposomal lactoferrin in the formulation is between 2.9 mg/ml and 10 3.5 mg/ml, and preferably 3.2 mg/ml.

3. A composition to be used for treatment and prevention of infections caused by COVID-19 and other coronavirus, according to claim 1, characterized by the fact that the diameter of the particle of lactoferrin liposome is 124±6 nm.

4. A composition to be used for treatment and prevention of infections caused by COVID-19 and other coronavirus, according to claims 3, characterized by the fact that the phospholipid used to produce the lactoferrin liposomes is phosphatidylcholine.

5. Composition to be used for treatment and prevention of infections caused by COVID-19 and other coronavirus, according to claim 1, characterized by the fact that, besides the main active ingredients (lactoferrin), it contains liposome-encapsulated zinc salt in a concentration of between 1.0 mg/ml and 1.2 mg/ml, preferably 1.1 mg/ml.

6. A composition to be used for treatment and prevention of infections caused by COVID-19 and other coronavirus, according to claim 5, characterized by the fact that zinc salt is preferably zinc sulphate.

7. Composition to be used for treatment and prevention of infections caused by COVID-19 and other coronavirus, according to claim 6, characterized by the fact that, besides the main active ingredients (lactoferrin) and a secondary active ingredient (zinc salt liposomes), it contains vitamin C liposomes in a concentration of between 1.1 mg/ml and 1.3 mg/ml, preferably 1.2 mg/ml.

8. Use of the composition of previous claims for the treatment and prevention of infections caused by COVID-19 and other coronavirus using the following doses of liposomal lactoferrin: curative dose: 64-96 mg (20-30 ml composition) every 6 h every day to cure the infection caused by COVID-19 (256-384 mg liposomal lactoferrin/day) preventive dose: 64 mg (20 ml composition) 2 or 3 times a day (128-192 mg liposomal lactoferrin/day).

9. Use of the composition of previous claims for the treatment and prevention of infections caused by COVID-19 and other coronavirus using a dose of liposomal lactoferrin that can be increased to 960 mg/day.

10. Use of the composition of previous claims for the treatment and prevention of infections caused by COVID-19 and other coronavirus on pregnant women and babies under 2 years of age suing the following dose of liposomal lactoferrin: mothers: 20 mg (6.25 ml) 3 or 4 times a day (72-80 mg/day).—babies: 20 mg (6.25 ml) 2 times a day.

11. A therapeutic method for treating infection of Corona Virus-19, comprising the steps of: A) assessing and documenting predetermined symptoms for Corona Virus-19 infections; and B) administering orally an effective amount of lactoferrin with a liposome carrier, over a predetermined period of time, to reduce said symptoms.

12. The method set forth in claim 11 further including an effective amount of vitamin C liposomes.

13. The method set forth in claim 12 further including an effective amount of zinc salt liposomes.

14. The method set forth in claim 13 wherein said effective amounts of lactoferrin, vitamin C and zinc salt liposomes are administered daily.

15. The method set forth in claim 14 wherein said effective amounts of lactoferrin is kept between 256 mg and 384 mg per day.

16. The method set forth in claim 15 wherein said effective amount of lactoferrin between 64 mg and 96 mg every 6 hours.

17. The method set forth in claim 16 wherein said symptoms are in the group that consists of tiredness or weakness, loss of smell, loss of taste, cough, muscular pain, headache and diarrhea.

18. A therapeutic method for preventing Corona Virus-19 infection, comprising the steps of: A) assessing and documenting predetermined symptoms of a patient; and B) administering orally an effective amount of lactoferrin in a liposome, over a predetermined period of time to prevent infection.

19. The method set forth in claim 18 further including an effective amount of vitamin C liposomes.

20. The method set forth in claim 19 further including an effective amount of zinc salt liposomes.

21. The method set forth in claim 20 wherein said effective amounts are administered daily.

22. The method set forth in claim 21 wherein said effective amounts of lactoferrin is kept between 128 mg and 192 mg per day.

23. The method set forth in claim 22 wherein said effective amount of lactoferrin is 64 mg between two and three times per day.

24. A therapeutic method for treating infection of Corona Virus-19, comprising the steps of: A) assessing and documenting the symptoms of a patient; and B) administering via nebulizer an effective amount of lactoferrin, over a predetermined period of time, to reduce said symptoms.

25. The method set forth in claim 24 wherein said effective amount is administered daily.

26. The method set forth in claim 25 wherein said effective amount of lactoferrin is not less than 64 mg and no more than 96 mg every six hours.

27. A therapeutic method for preventing Corona Virus-19 infection, comprising the steps of: A) assessing and documenting that a patient lacks any symptoms; and B) administering via nebulizer an effective amount of lactoferrin, over a predetermined period of time.

28. The method set forth in claim 27 wherein said effective amounts are administered daily.

29. The method set forth in claim 28 wherein said effective amount of lactoferrin between 128 mg and 192 mg per day.

30. The method set forth in claim 29 wherein said effective amount of lactoferrin is 64 mg given between two and three times per day.

Description

[0075] To complement the description and facilitate the understanding of the characteristics of the invention, for illustrative purposes this descriptive memory includes a set of images which represent the following:

[0076] FIG. 1:—These two images show how the formulation prevents the entry of coronavirus in the cell, and when there is infection.

[0077] FIG. 2—Distribution of particle size per number of particles (%) obtained through DLS studies for A) lactoferrin liposomes, B) sodium ascorbate liposomes, and C) zinc sulphate liposomes.

[0078] FIG. 3: Absence or presence of dry cough from patients before treatment (day 0) and after the treatment (48 hours and 5 days).

[0079] FIG. 4—Absence or presence of muscular pain from patients before treatment (day 0) and after the treatment (48 hours and 5 days).

[0080] FIG. 5—Absence or presence of tiredness from patients before treatment (day 0) and after the treatment (48 hours and 5 days).

[0081] FIG. 6—Absence or presence of headache from patients before treatment (day 0) and after the treatment (48 hours and 5 days).

[0082] FIG. 7—Absence or presence of taste from patients before treatment (day 0) and after the treatment (48 hours and 5 days).

[0083] FIG. 8—Absence or presence of smell from patients before treatment (day 0) and after the treatment (48 hours and 5 days).

[0084] FIG. 9—Diagram representing the mediation by lactoferrin of inflammation induced by the infection caused by COVID-19, which leads to the activation of macrophages and dendritic cells.

EXPLANATION OF EXECUTION MODE

[0085] Below is the description of the implementation method of the invention. On the one hand, it alludes to this invention, and on the other hand, to the use of said invention.

[0086] Soy lecithin for food purposes was purchased from Lipoid (Ludwigshafen, Germany); tween 20, from Comercial Quimica Massó (Barcelona, Spain); ethanol 96° from Panreac (Barcelona, Spain); lactoferrin from Ferrer Health (Barcelona, Spain); sodium ascorbate from Fagron Ibérica (Barcelona, Spain); and zinc sulphate heptahydrate from Nutrifoods (Barcelona, Spain).

[0087] The different liposomal solutions were prepared according to the procedure developed by the Sesderma laboratories (Valencia, Spain).(Serrano et al., 2015) Specifically, phospholipids (Phosphatidylcholine) were dissolved in ethanol 96° at room temperature, and then tween 20 was added to the ethanol solution. Simultaneously, the different active ingredients were dissolved in double-distilled water at a 5.2, 150 and 14 mg/ml concentration for lactoferrin, sodium ascorbate and zinc sulphate, respectively. Later, the lipidic mixture and the aqueous solution containing the corresponding active ingredient (lactoferrin, sodium ascorbate or zin sulphate) were combined and vigorously shaken for 5 minutes.

[0088] Finally, the resulting liposomal suspensions were filtered using a cellulose acetate syringe filter without surfactant, with a pore size of 0.2 μm.

[0089] The final concentration of the active ingredients in the different liposomal suspensions is detailed in the table below:

[0090] Active Ingredient Concentrations in the Different Liposomic Suspensions Prepared

TABLE-US-00007 Active Concentration ingredient (mg/ml) lactoferrin 4 Sodiom 100 ascorbate Zinc 10 sulphate

[0091] The characterisation of the liposome in terms of particle size was evaluated through dynamic light dispersion (DLS). All measurements were carried out using a Delsa Nano C particle analyser (Beckman Coulter, Madrid, Spain), and performed three times in diluted liposome suspensions with filtered de-ionised water. Polydispersity index (PDI) was used as a measure to define homogeneity in size distribution. A sample presenting a PDI value equal to or lower than 0.2 is considered as a homogeneous population.

[0092] With the purpose of administering the encapsulated active ingredients to volunteers in the study, the prepared liposomal solutions were included in two liquid formulations of food supplement. The formulations of food supplements that consisted in a mixture of components with a nutritional a mixture of components with a nutritional physiological effect are shown in the table below:

Composition of Food Supplements

[0093]

TABLE-US-00008 Food supplement 1 Food supplement 2 Citric acid Citric acid Potassium sorbate Potassium sorbate Sucralose Sucralose Aroma Aroma Sodium benzoate Sodium benzoate Xanthan gum Xanthan gum Glycerine Glycerine Sodium ascorbate liposomes Zinc sulphate liposomes Lactoferrin liposomes

[0094] The concentration of active ingredients in the different food supplement formulations is specified in the table below:

Active Ingredient Concentration in the Prepared Formulation of the Food supplement (SA)

[0095]

TABLE-US-00009 Active Concentration (mg/ml) ingredient SA1 SA2 Lactoferrin 3, 2 — Sodium 1, 2 — ascorbate Zinc sulphate — 1, 1

[0096] Studies on particle size revealed that all the liposome formulations used in this study present a particle diameter in the interval of approximately 100-130 nm, with a PDI under 0.15. Results are shown in FIG. 2 and are summarised in the table below:

Particle Diameter Measured by DLS and Polydispersity Index (PDI) of Lactoferrin Liposomes, Sodium Ascorbate and Zinc Sulphate

[0097]

TABLE-US-00010 Active ingredient encapsulated in Particle liposomes diameter (nm) PDI Lactoferrin 124 ± 6 0.14 ± 0.03 Sodium 128 ± 8 0.06 ± 0.02 ascorbate Zinc sulphate 130 ± 4 0.11 ± 0.03

[0098] Regarding the use of this composition, it must be done with the following doses of liposomal lactoferrin or amount:

[0099] Curative dose: 64-96 mg (20-30 ml) every 6h daily to cure the infection caused by COVID-19 (256-384 mg/day). Doses can be increased to 640-960 mg/day.

[0100] Preventive dose: one 64 mg dose, 2 or 3 times a day prevents the infection caused by COVID-19 (128-192 mg/day).

[0101] Pregnancy and babies (glycerosome encapsulation, alcohol free): [0102] Pregnant women and babies under 2 years of age. [0103] Mothers: 20 mg (6.25 ml) 3 or 4 times a day (72-80 mg/day). [0104] Babies: 20 mg (6.25 ml) twice a day. [0105] Zinc Defense syrup: 10-30 mg/day (10-30 ml)

[0106] In addition, regarding nasal administration of lactoferrin nasal drops (Lactyferrin™): these nasal drops contain nano-lactoferrin to quickly relieve acute sinusitis and smell and taste alterations experienced by many patients, while contributing to handling dry cough. In severe cases, we recommend applying 2 drops on each nostril every 2-3 hours for 12 hours, and then every 4-6 hours. Lactyferrin nasal drops are a very important factor for the relief of respiratory symptoms.

[0107] Once the nature of the invention has been adequately described, as well as an example of preferential implementation, it is clarified that the materials, shape, size and arrangements of the elements described can be modified, provided this does not entail an alteration of the essential characteristics of the invention, described below.