WO2022243843A1 - Lotion antivirale - Google Patents

Lotion antivirale Download PDF

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Publication number
WO2022243843A1
WO2022243843A1 PCT/IB2022/054540 IB2022054540W WO2022243843A1 WO 2022243843 A1 WO2022243843 A1 WO 2022243843A1 IB 2022054540 W IB2022054540 W IB 2022054540W WO 2022243843 A1 WO2022243843 A1 WO 2022243843A1
Authority
WO
WIPO (PCT)
Prior art keywords
antiviral
lotion
face
optionally
parts
Prior art date
Application number
PCT/IB2022/054540
Other languages
English (en)
Inventor
Kabamba ALEXANDRE
Original Assignee
Council For Scientific And Industrial Research
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Council For Scientific And Industrial Research filed Critical Council For Scientific And Industrial Research
Publication of WO2022243843A1 publication Critical patent/WO2022243843A1/fr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/005Antimicrobial preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/02Algae
    • A61K36/04Rhodophycota or rhodophyta (red algae), e.g. Porphyra
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/645Proteins of vegetable origin; Derivatives or degradation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9706Algae
    • A61K8/9717Rhodophycota or Rhodophyta [red algae], e.g. Porphyra
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions

Definitions

  • the current invention relates to an antiviral lotion comprising birithsin (GRFT).
  • the current invention further relates to a process for producing said antiviral lotion, and to use of the antiviral lotion as an antiviral agent.
  • GRFT griffithsin
  • COVID-19 2019 coronavirus disease
  • SARS-CoV-2 the etiological agent
  • COVID-19 Even asymptomatic infected people are able to effectively spread SARS-CoV-2 and the vast majority (around 80%) of COVID-19 cases are either asymptomatic or have only mild symptoms. However, 20% of all those infected will develop severe illness, with the mortality rate standing at about 2% across the globe.
  • COVID-19 has affected millions of people and caused millions of deaths in the world, both in developed and developing countries; as well as taking many economies into recessions or to the brink of collapse.
  • Griffithsin is a lectin protein that has been isolated from the red algae Griffithsia Sp., although it has also been successfully produced recombinantly in plants. It is known to be a highly effective human immunodeficiency virus (HIV) entry inhibitor and has been investigated as a potential microbicide against HIV-1 . In addition, it has been studied as an anti-viral agent against other enveloped viruses including SARS and Ebolavirus.
  • HIV human immunodeficiency virus
  • an antiviral face and optionally body lotion comprising birithsin (GRFT).
  • the antiviral lotion may be effective against enveloped viruses including coronaviruses, in particular SARS-CoV-2 and/or MERS-CoV. More particularly, the antiviral lotion is safe and non-irritating and can be used on sensitive areas of the body, such as the face.
  • the antiviral lotion may further comprise or consist of the following ingredients:
  • one or more emollients including coconut oil
  • one or more preservatives including Euxyl PE9010;
  • buffers including sodium hydroxide (NaOH);
  • (ix) optionally one or more fragrances and/or colourants.
  • the antiviral lotion consists of the following ingredients:
  • the antiviral lotion has a pH of between about pH 5.0-5.8.
  • a process for manufacturing the antiviral lotion of the invention comprising or consisting of the steps of: a) in a first vessel mixing one or more stabilisers including disodium EDTA, one or more thickeners including xantham gum and optionally a diluent including de-ionised water to form a part A and heating part A to 75°C; b) in a second vessel mixing one or more emulsifiers including a wax, and one or more emollients including coconut oil to form a part B, and heating part B to 75°C; c) mixing part A to part B until uniformly mixed at 75°C, and then removing the mixed parts A and B from heat; d) homogenising the mixed parts A and B and cooling to 40°C; e) in a third vessel mixing one or more humectants including glycerine, and one or more preservatives including Euxyl PE9010 to form a part C, followed by
  • the process for manufacturing the antiviral lotion of the invention may consist of the steps of: a) in a first vessel mixing disodium EDTA, xantham gum and de-ionised water to form a part A and heating the part A to 75°C; b) in a second vessel mixing a wax and coconut oil to form a part B, and heating the part B to 75°C; c) mixing part A to part B at 75°C until uniformly mixed, and then removing the mixed parts A and B from heat; d) homogenising the mixed parts A and B and cooling to 40°C; e) in a third vessel mixing glycerine and Euxyl PE9010 to form a part C, followed by adding part C to the homogenised and cooled parts A and B of step d) and mixing until uniformly mixed; f) checking the pH of the uniformly mixed parts A, B and C of step e) and adjusting to between about pH 5.0 and 5.8 by addition of NaOH to form a buffered lotion solution;
  • a method for sanitising parts of the body, in particular, sensitive areas such as the face with the use of the antiviral lotion according to the invention comprising application of the antiviral lotion to the face and optionally the body.
  • a method for inhibition of viruses including enveloped viruses, in particular coronaviruses such as SARS-CoV-2 and/or MERS-CoV with the use of the antiviral lotion according to the invention comprising application of the antiviral lotion to the face and optionally the body.
  • an antiviral lotion according to the invention for use in a method of sanitising parts of the body and/or inhibition of viruses, including enveloped viruses, in particular coronaviruses such as SARS-CoV-2 and/or MERS-CoV, in particular, sensitive areas such as the face, comprising application of the antiviral lotion to the face and optionally the body.
  • viruses including enveloped viruses, in particular coronaviruses such as SARS-CoV-2 and/or MERS-CoV, in particular, sensitive areas such as the face, comprising application of the antiviral lotion to the face and optionally the body.
  • Figure 1 shows GRFT containing lotion inhibition of coronavirus infection of Vero cells.
  • SARS-CoV-2 was incubated with the GRFT containing lotion prior to the infection of Vero cells. After 72 hours of tissue culture the viral infection of cells was measured by luminescence detection. Bars represent mean ⁇ standard deviation of 2 independent experiments.
  • B The experiment above was repeated using MERS-CoV virus. Note that CL means the cell control i.e. the background reading.
  • the current invention relates to an antiviral lotion comprising birithsin (GRFT).
  • the current invention further relates to a process for producing said antiviral lotion, and to use of the antiviral lotion as an antiviral agent.
  • GRFT griffithsin
  • the applicant has developed an antiviral lotion that is safe and non-irritating, and effective against enveloped viruses, including coronaviruses such as SARS-CoV-2 or MERS-CoV that can be used on sensitive areas of the body, including the face.
  • coronaviruses such as SARS-CoV-2 or MERS-CoV that can be used on sensitive areas of the body, including the face.
  • the antiviral lotion comprises or consists of the following ingredients:
  • one or more emollients including coconut oil
  • one or more preservatives including Euxyl PE9010;
  • buffers including sodium hydroxide (NaOH);
  • diluents including water, such as de-ionised water;
  • (ix) optionally one or more fragrances and/or colourants.
  • the antiviral lotion having 0.1 mg/ml GRFT was tested for stability under different conditions compared with a reference standard lotion, including performance of mechanical tests (Table 2), and an accelerated and visual stability test (Table 3). All mechanical tests were passed, with the antiviral lotion conforming to the stability of the reference standard lotion.
  • the lotion skin irritation test was done at the Sefako Makgatho Health Science University (SMU) comparing the antiviral lotion having 0.1 mg/ml GRFT, with de ionised water as a negative control and a positive control lotion (1% sodium lauryl sulphate or SLS).
  • SMU Sefako Makgatho Health Science University
  • Controls and products were applied to the inner forearm of each volunteer in a randomized, blinded pattern at zero hours and repeated on the same position at 24 hours.
  • a measured volume of control or product was placed in the respective chamber and the chamber attached to the forearm. Products were tested using specially designed aluminium Finn Chambers on Scanpore ® tape for occluded sites or modified Hilltop chambers for unoccluded sites as set out in Table 4 below. The patches were observed at 0, 24, 48, 72 and 96 hours after application. Patch areas were covered with the chambers for the first 2 x 23 hours, thereafter the chambers were removed.
  • the antiviral lotion was formulated according to Table 1 above to contain the lectin griffithsin (GRFT) at concentrations of 0.1 , 0.03, 0.01 , 0.003, and 0.001 mg/ml (w/v). These lotions formulations were used in a viral inhibition assay by incubating them with either SARS-CoV-2 or MERS-CoV before the infection of cells.
  • GRFT lectin griffithsin
  • the antiviral lotion containing GRFT ICso for the inhibition of SARS-CoV-2 was calculated to be 0.033 mg/ml.
  • the antiviral lotion was potently inhibitory to MERS-CoV ( Figure 1 B) with an ICso value of 0.023 mg/ml.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Mycology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medical Informatics (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une lotion antivirale efficace contre les virus enveloppés, notamment les coronavirus, comprenant de la griffithsine (GRFT). L'invention concerne en outre un procédé de production de ladite lotion antivirale, et l'utilisation de ladite lotion antivirale en tant qu'agent antiviral contre les virus enveloppés, notamment les coronavirus.
PCT/IB2022/054540 2021-05-20 2022-05-16 Lotion antivirale WO2022243843A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ZA2021/03412 2021-05-20
ZA202103412 2021-05-20

Publications (1)

Publication Number Publication Date
WO2022243843A1 true WO2022243843A1 (fr) 2022-11-24

Family

ID=82019255

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2022/054540 WO2022243843A1 (fr) 2021-05-20 2022-05-16 Lotion antivirale

Country Status (1)

Country Link
WO (1) WO2022243843A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160339076A1 (en) * 2014-01-28 2016-11-24 The Population Council, Inc. Combination product for the prevention of sexually transmitted infections
WO2021222965A1 (fr) * 2020-05-07 2021-11-11 Ess Holding Gmbh Lectine se liant au mannose pour le traitement ou la prophylaxie de maladies inflammatoires
WO2021236672A2 (fr) * 2020-05-18 2021-11-25 University Of Louisville Research Foundation, Inc. Compositions et méthodes de prévention d'infection à coronavirus
WO2022029604A1 (fr) * 2020-08-07 2022-02-10 Council For Scientific And Industrial Research Système d'administration de médicament de type microémulsion pour le traitement du syndrome de détresse respiratoire aiguë

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160339076A1 (en) * 2014-01-28 2016-11-24 The Population Council, Inc. Combination product for the prevention of sexually transmitted infections
WO2021222965A1 (fr) * 2020-05-07 2021-11-11 Ess Holding Gmbh Lectine se liant au mannose pour le traitement ou la prophylaxie de maladies inflammatoires
WO2021236672A2 (fr) * 2020-05-18 2021-11-25 University Of Louisville Research Foundation, Inc. Compositions et méthodes de prévention d'infection à coronavirus
WO2022029604A1 (fr) * 2020-08-07 2022-02-10 Council For Scientific And Industrial Research Système d'administration de médicament de type microémulsion pour le traitement du syndrome de détresse respiratoire aiguë

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KRAMZER LINDSAY F ET AL: "Preformulation Characterization of Griffithsin, a Biopharmaceutical Candidate for HIV Prevention", AAPS PHARMSCITECH, SPRINGER INTERNATIONAL PUBLISHING, CHAM, vol. 22, no. 3, 24 February 2021 (2021-02-24), XP037445282, DOI: 10.1208/S12249-021-01931-0 *
MORI T ET AL: "ISOLATION AND CHARACTERIZATION OF GRIFFITHSIN, A NOVEL HIV-INACTIVATING PROTEIN, FROM THE RED ALGA GRIFFITHSIA SP", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY FOR BIOCHEMISTRY AND MOLECULAR BIOLOGY, US, vol. 280, no. 10, 11 March 2005 (2005-03-11), pages 9345 - 9353, XP009061538, ISSN: 0021-9258, DOI: 10.1074/JBC.M411122200 *

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