INSECT REPELLING COMPOSITION

Abstract

A composition and method for insect repellent is provided. The composition in one form has on a weight percentage basis 10-20% 2,6-dimethyl-7-octen-2-ol; 0.1-5% 2,6-octadienal, 3,7-dimethyl-; 1-10% benzyl benzoate; 0.01-2% citral; 1-10% hexamethylindanopyran; 10-40% lavender oil; 20-50% Lemon Oil Argentina; 5-15% Lime Oil Distilled Mexican; 0.01-3% limonene; 5-15% rosemary oil; and optionally 0.1-10% an insect repellent active ingredient selected from the group consisting of N,N-Diethyl-meta-toluamide (DEET), ethyl butylacetylaminopropionate and picaridin. The composition has insect repellent properties.

Claims

1. A composition comprising, on a weight percent basis: 10-20% 2,6-dimethyl-7-octen-2-ol; 0.1-5% 2,6-octadienal, 3,7-dimethyl-; 1-10% benzyl benzoate; 0.01-2% citral; 1-10% hexamethylindanopyran; 10-40% lavender oil; 20-50% Lemon Oil Argentina; 5-15% Lime Oil Distilled Mexican; 0.01-3% limonene; and 5-15% rosemary oil.

2. The composition of claim 1, further comprising 0.1-10% an insect repellent active ingredient selected from the group consisting of N,N-Diethyl-meta-toluamide (DEET), ethyl butylacetylaminopropionate and picaridin.

3. The composition of claim 1, further comprising on a weight basis 0.1-10% alcohol selected from the group consisting of isopropyl, ethyl, and methyl.

4. The composition of claim 1, comprises: 12-18% 2,6-dimethyl-7-octen-2-ol; 0.1-1% 2,6-octadienal, 3,7-dimethyl-; 2-5%—benzyl benzoate; 0.01-1% citral; 2-5%—hexamethylindanopyran; 25-30% lavender oil; 30-40% Lemon Oil Argentina; 5-10% Lime Oil Distilled Mexican; 0.01-0.1% limonene; and 5-10% rosemary oil.

5. The composition of claim 4, further comprising 1-10% an insect repellent active ingredient selected from the group consisting of N,N-Diethyl-meta-toluamide (DEET), ethyl butylacetylaminopropionate and picaridin.

6. The composition of claim 4, further comprising on a weight basis 0.1-1% alcohol selected from the group consisting of isopropanol, ethanol and methanol.

7. The composition of claim 1 further comprises an inactive carrier, which in combination thereby forms a topical location.

8. The composition of claim 1, wherein the composition is formulated as a solution for application as a spray or mist.

9. A method for repelling insects comprising deploying a composition comprising, on a weight percent basis: 10-20% 2,6-dimethyl-7-octen-2-ol; 0.1-5% 2,6-octadienal, 3,7-dimethyl-; 1-10% benzyl benzoate; 0.01-2% citral; 1-10% hexamethylindanopyran; 10-40% lavender oil; 20-50% Lemon Oil Argentina; 5-15% Lime Oil Distilled Mexican; 0.01-3% limonene; and 5-15% rosemary oil.

10. The method of claim 9, wherein the composition further comprises 0.1-10% an insect repellent active ingredient selected from the group consisting of N,N-Diethyl-meta-toluamide (DEET), ethyl butylacetylaminopropionate and picaridin.

11. The method of claim 9, wherein deploying the composition comprises applying the composition to an individual to thereby repel insects from the individual.

12. The method of claim 9, wherein deploying the composition comprises spraying the composition in an area where one wishes to repel insects.

13. The method of claim 9, wherein deploying the composition comprises placing the composition in an area where one wishes to repel insects.

14. The method of claim 9, wherein deploying the composition comprises burning the composition to thereby release its constituents into the surrounding environment to thereby repel insects in the surrounding environment.

15. The method of claim 9, wherein deploying the composition comprises spraying or misting the composition formulated as a solution for application as a liquid.

16. The method of claim 9, wherein the composition comprises: 12-18% 2,6-dimethyl-7-octen-2-ol; 0.1-1% 2,6-octadienal, 3,7-dimethyl-; 2-5%—benzyl benzoate; 0.01-1% citral; 2-5%—hexamethylindanopyran; 25-30% lavender oil; 30-40% Lemon Oil Argentina; 5-10% Lime Oil Distilled Mexican; 0.01-0.1% limonene; and 5-10% rosemary oil.

17. The method of claim 16, wherein the composition further comprises 0.1-10% an insect repellent active ingredient selected from the group consisting of N,N-Diethyl-meta-toluamide (DEET), ethyl butylacetylaminopropionate and picaridin.

18. The composition of claim 5, further comprising on a weight basis 0.1-10% alcohol selected from the group consisting of isopropyl, methanol and ethanol.

19. The composition of claim 2, further comprises an inactive carrier, which in combination thereby forms a topical location.

20. The composition of claim 2, wherein the composition is formulated as a solution for application as a spray or mist.

21. The method of claim 10, wherein deploying the composition comprises applying the composition to an individual to thereby repel insects from the individual.

22. The method of claim 10, wherein deploying the composition comprises spraying the composition in an area where one wishes to repel insects.

23. The method of claim 10, wherein deploying the composition comprises placing the composition in an area where one wishes to repel insects.

Description

DETAILED DESCRIPTION

[0083] The present composition functions as a repellent of insects including mosquitoes. The mechanism by which the present invention operates varies depending on the specific constituents in the composition. The composition includes constituents such as fragrances that act on an insect's olfactory sensory neurons. Other constituents in the present composition affect an insect's other senses.

[0084] In one preferable formulation, the present composition achieves a superior insect repellent that focuses on repellent factors while avoiding limitations of toxicity to humans, animals or other living things including plants to which one wishes to repel insects.

[0085] Referring specifically to how various formulations of the present composition affect insects and in particular mosquitoes, each mosquito olfactory sensory neuron expresses one odorant receptor which recognizes specific structural features or epitopes in odorant molecules. Axons of neurons expressing the same receptor converge onto a single glomerus. Therefore a given odorant may have structural features that are recognized by odorant receptors Or83b, Or47a, Or4, Or103, and cpA that activate the corresponding glomeruli. Another odorant may have different epitopes and may activate alternate receptors. A third type of odorants may have completely different epitopes and activate several receptors simultaneously. Therefore, an odorant receptor and its corresponding glomerulus can be activated by several different odorants, but each odorant is likely to elicit a unique pattern of glomeruli activation. This pattern constitutes an odorant specific neural pattern that the mosquito utilizes to find prey.

[0086] One aspect of the present composition focuses on specific components or constituents that inhibit these olfactory receptors either specifically or universally to effectively “blind” the insect (e.g., mosquito) to human prey. This strategy allows one to select specific constituents and respective concentrations for inclusion in formulations of the present composition sufficient to produce an insect repellent that has synergistic, superior insect repellent properties as compared with that of DEET, IR3535, or picaridin alone which only affect singular receptors.

[0087] In accordance with another aspect of the present composition, the composition can be formulated to make an individual to which the composition is applied “blind” to insects such as but not limited to mosquitos or other biting insects, by inhibiting the protein receptors that detect body odors in humans or animals. These specialized receptors detect specific proteins of body odors emitted by humans. These odors are sulcatone and lactic acid. The mosquito antennae have specialized receptors (AaegOr4, AaegOr65, and AaegOr103) that detect human body odors sulcatone and lactic acid that are specific in locating human prey. All of these receptors require the function of P450 isozymes for the receptors to detect these human specific odorants. It would be a unique strategy to incorporate key chemicals into a repellent that sufficiently inhibits the function of the AaegOr4, AaegOr65, and AaegOr103 receptors. Successful deactivation of these key receptors via P450 isozyme inhibition would blind the mosquito to the presence of a human host. Accordingly, several formulations of the present composition include constituents for the purpose of blinding mosquito sulcatone and lactic acid receptors by inactivation of native receptor P450 isozymes.

EXAMPLES

[0088] The following are examples of formulations and uses of the present composition.

Example 1

[0089] Formula 1—The composition of Formula 1 has, on a weight percentage basis the following:

TABLE-US-00001 1. 2,6-dimethyl-7-octen-2-ol 14.20% 2. 2,6-octadienal, 3,7-dimethyl- 0.44% 3. ethyl alcohol 0.15% 4. benzyl benzoate 3.55% 5. citral 0.06% 6. hexamethylindanopyran 3.55% 7. lavender oil 28.80% 8. Lemon Oil Argentina 35.00% 9. Lime Oil Distilled Mexican 7.10% 10. limonene 0.06% 11. rosemary oil 7.10%

Experiments

[0090] Table 1 (below) demonstrates insect repellency of Formula 1 to inhibit both landing and probing (feeding behavior) of mosquitoes.

TABLE-US-00002 TABLE 1 ‘Neat’ pure Formula 1 - 100% concentration Time Landings Probes 1 hour after application 100% repellency 100% repellency 2 hours after application 100% repellency 100% repellency

[0091] Collagen membranes were used as a skin analog for testing the liquid test substances. The collagen membranes were moistened with water and the surface was dried prior to the applications to provide a texture and consistency that was similar to human skin. The applications were conducted with the collagen membranes by shaking the test substances well, then applying the test substance onto the membranes until wet and then gently rubbing the test substance into the membranes.

[0092] The membranes were placed on top of water moistened paper towels (lightly moistened) to maintain a “skin like” consistency by preventing complete moisture loss from the membranes while aging. The membranes were placed on the paper towels with the untreated side in contact with the paper towels and water was added to the paper towels as needed to maintain moisture during the aging process. Each test substance was evaluated at 1 and 2 hours after the applications. Each evaluation consisted of two (2) replicates per age.

[0093] Twenty-five (25) female mosquitoes were released inside a 1′×1′ cage and the mosquitoes were held without food for at least 2 hours prior to testing. The cage had a 1′×1′ wooden cover on the top of the cage with an approximate 2.5″×6″ removable section in its center. The section was removable to provide an opening in the top of the cage for the test surface and for the mosquitoes to try to feed on the test subject's arm above the test surface. Mesh was placed on the top side of the test surface to prevent direct contact of the test surface with the test subject's arm and disposable wood spacers were placed on top of the top cover to elevate the test subject's arm from the test substance and to prevent the mosquitoes from being able to feed on the test subject.

[0094] An untreated pre-treatment evaluation was conducted prior to testing the treated test surface by counting the number of mosquitoes that landed and probed on an untreated test surface during a 5-minute time period. The treated surface was evaluated in the same manner as the untreated surface and the repellency was calculated by comparing the number of landing and probes during the pre-treatment evaluation to the number of landing and probes during the treatment evaluation. The study was conducted using two different test subjects for each test substance and aged evaluation.

TABLE-US-00003 TABLE 2 As active ingredient of Formula 1 in a lotion* % Active ingredient Time Landings Probes 0.25% 6 hours after 83% repellency 95% repellency application 0.25% 8 hours after 42% repellency 50% repellency application 1% 6 hours after 63% repellency 83% repellency application 1% 8 hours after 73% repellency 78% repellency application 5% 6 hours after 78% repellency 91% repellency application 5% 8 hours after 75% repellency 83% repellency application (*The lotion formulation consists of 0.25%, 1% and 5% Formula 1 and the following inactive ingredients by weight: 81-85.8% water 5.6% cetearyl alcohol 2.4% ceteareth-20 2% isopropyl myristate 2% soybean oil 0.995% glycerin 0.900% phenoxy ethanol 0.10% ethylhexylglycerin

[0095] Collagen membranes were used as a skin analog for testing the liquid test substances. The collagen membranes were moistened with water and the surface was dried prior to the applications to provide a texture and consistency that was similar to human skin. The applications were conducted to the collagen membranes by shaking the test substances well, then applying the test substance onto the membranes using a 1 gram/600 cm2 application rate and then gently rubbing the test substance into the membranes.

[0096] The membranes selected for the untreated controls were moistened with water but did not receive any other application. The membranes were placed on top of water moistened paper towels (lightly moistened) to maintain a “skin like” consistency by preventing complete moisture loss from the membranes while aging. The membranes were placed on the paper towels with the untreated side in contact with the paper towels and water was added to the paper towels as needed to maintain moisture during the aging process. Test substances were evaluated at 6 and 8 hours after the applications. Each evaluation consisted of 4 replicates for the controls and 4 replicates for each test substance per age.

[0097] Twenty-five (25) female mosquitoes were released inside a 1′×1′ cage and the mosquitoes were held without food for at least 2 hours prior to testing. The cage had a 1′×1′ wooden cover on the top of the cage with an approximate 2.5″×6″ removable section in its center. The section was removable to provide an opening in the top of the cage for the test surface and for the mosquitoes to try to feed on the test subject's arm above the test surface. Mesh was placed on the top side of the test surface to prevent direct contact of the test surface with the test subject's arm and disposable wood spacers were placed on top of the top cover to elevate the test subject's arm from the test substance and to prevent the mosquitoes from being able to feed on the test subject. An untreated pre-treatment evaluation was conducted prior to testing the treated test surface by counting the number of mosquitoes that landed and probed on an untreated test surface during a 5-minute time period. The treated surface was evaluated in the same manner as the untreated surface and the repellency was calculated by comparing the number of landing and probes during the pre-treatment evaluation to the number of landing and probes during the treatment evaluation. The study was conducted using two different test subjects for each test substance and aged evaluation.

[0098] It will now be clear that the present composition in its various formulations provides features and advantages not found in prior insect repellents. The present composition can be formulated to have strong insect repellent properties while being safe for humans and animals.

[0099] Further, the composition can be formulated to have superior mosquito repelling properties based on its constituents including fragrances which are created by selection of active extracts that effect multiple repellent strategies of predator insects such as, but not limited to, mosquitos, lice, ticks, fleas, flies, bed bugs and mites.

[0100] Further, the present composition can be optimized by selecting the specific constituents in desired amounts to achieve a desired insect repellent property based on the desired insect to repel and based on a selected desire to protect mammals including humans and animals from insects including biting insects.

[0101] Selection of desirable constituents for inclusion of formulations of the presented composition are based on inhibition of key insect receptors which include mosquito receptors for repelling mosquitos. This may be accomplished synergistically by inhibition of carbon dioxide receptors, body odor receptors, DEET-like receptors or Dopamine Receptors. Progressive inhibition of synaptic firing of potentials in these key receptors lead result in the insect finding the human target undesirable and causes aversion to feeding.

[0102] Further, the composition can be modified such that when applied to humans, the human is “invisible” or unappealing to insects such as mosquitos by specially selecting particular isolates comprising the fragrance linked to ultra-stimulate key receptors utilized by mosquitos or other insects to select prey.

[0103] In various forms of the present composition, the constituents work synergistically to effect known DEET receptors of an insect such as a mosquito. For example there are two specific DEET receptors Or83B and Or47a. The contemplated formula contains linalool that is known to affect these specific receptors respectively.

[0104] In addition, the present composition can be formulated to inhibit key chemical signatures that modulate mosquito feeding behavior. Doing so would result in reducing or controlling the infection rate of malaria carried by mosquitos. It is known that the malaria parasite will cause infected individuals to “outgas” chemical attractants that attract mosquitoes (pinene and limonene). It is the object of the invention to utilize a-pinene or limonene or both as chemical “blinding agents” by over stimulating mosquito sensory receptors that detect these chemicals. Over stimulation of these key receptors will elicit an avoidance behavior of predatorial mosquitoes.

[0105] In addition, the composition can be formulated with specific chemical constituents that render an insect “blind” for sensing carbon dioxide discharge from animals and human hosts. The receptors in particular are the gr1, gr2, and gr3 “gustatory” receptors containing the cpA receptor sensory cluster. It would be contemplated that the formulations would contain ethyl pyruvate, 7-a-beta-nepatalactone, methyl salicylate either independently or in combination as gustatory inhibitors.

[0106] The composition can also be formulated to contain specific chemical isolates that “blind” insect receptors AaegOr4, AaegOr65, and AaegOr103 by deactivation or inhibition of P450 isozymes found in the receptor. Deactivation of protein specific receptors would blind the mosquito to the presence of sulcatone and lactic acid odors produced by human targets. These contemplated isolates are myrcene, borneol, and pinene that actively deactivate the sulcatone and lactic acid specific protein receptors of the mosquito by direct and passive inhibition of the receptors native neuronal P450 isozymes.

[0107] Alternatively, the present composition can be formulated to prevent malaria infection by creating a topical formulation of botanical abstracts that are toxic to malaria (P. falciparum) sporozoites. It is contemplated that certain chemical components of botanical extracts are toxic to malarial sporozoites and plasmodium. It is further contemplated that direct reduction of malaria infection may be accomplished as the mosquito proboscis comes into contact with these botanical extracts at the initiation of penetration of the host.

[0108] In yet another alternative, the present composition can be formulated to contain chemicals that inhibit mosquitoes from developing learned behavior to avoid the aversion causing properties of DEET. It has been proven that mosquitoes can learn behavior that bypasses and reduces the effectiveness of DEET. This learned behavior has been well identified as one of the key factors that reduce the effectiveness of DEET. It is the object of the invention that the mosquito repelling formula contain monoterpenes as a means of inhibiting loss of DEET effectiveness by tolerance learning. This would include limonene.

[0109] Further, modifying the constituents in the present composition will have an effect to alter the overcall fragrant signature of the resulting composition which through routine experimentation and optimization will result in an insect repellent to perform as a repellent of a desired insect or for a particular application or use.