# US 11,298,375 B2 · Halogenated fullerene functionalized as a biocidal and chemotactic spermicide to vaginally harbor and neutralize spermatozoa for use as a safe and effective contraceptive

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- Number: US 11,298,375 B2
- Document ID: US11298375B2
- Status: Granted
- Kind: B2
- Application number: 17/499,223
- Filed: 2021-10-12
- Published: 2022-02-17
- Granted: 2022-04-12
- Earliest claimed: 2021-10-12
- Applicants: Terry Earl Brady; Anthony Lee Dellinger; Melinda K. M. Goddard; Kristen Dellinger
- Inventors: Terry Earl Brady; Anthony Lee Dellinger; Melinda K. M. Goddard; Kristen Dellinger
- Web page: https://patentgrep.com/patent/US11298375B2

## CPC

- A61K 33/44: Elemental carbon, e.g. charcoal, carbon black
- A61K 9/0034: {Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants}
- A61K 9/0036: {Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms}
- A61K 9/02: Suppositories; Bougies; Bases therefor; {Ovules}(apparatus for making A61J3/08; devices for introducing into the body A61M31/00)
- A61K 31/015: carbocyclic
- A61K 31/11: Aldehydes
- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 38/17: from animals; from humans {(enzyme inhibitors A61K38/005)}
- A61K 38/1703: {from vertebrates}
- A61P 15/18: Feminine contraceptives
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides the methods and composition useful as a contraceptive by preventing motile sperm from reaching a mature ovum, thereby blocking fertilization and preventing pregnancy. The contraceptive is comprised of halogen functionalized fullerene nanoparticles (halo fullerenes) and chemotactic stimulants that act synergistically to divert, incapacitate and ultimately rupture spermatozoa to avert fertilization. When applied vaginally prior to coitus, the suspension is activated by exposure to spermatozoa upon insemination. Notably, non-spermatozoa cells are unaffected by the pH-neutral suspension; however, closer to the same scale, microbes are susceptible to its inherent biocidal properties. Following application and coitus, the contraceptive evacuates naturally, along with seminal and vaginal fluids thereafter.

## Claims

### Claim 1

A contraceptive composition that chemically stimulates, diverts targeting, impedes mobility, ruptures and incapacitates spermatozoa comprising:
a. one or more halo fullerenes with the chemical formula of C60X6, C60X8, or C60X24, wherein X is a halogen selected from the group consisting of fluorine, chlorine, bromine, and iodine;
b. bourgeonal;
c. protamine;
d. optionally one or more pharmaceutical-grade additives.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the concentration of halo fullerenes is between 0.01% and 5.0%, based on the total weight of the composition.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the concentration of bourgeonal is between 0.0001% and 2.0%, based on the total weight of the composition.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the concentration of protamine is between 0.0001% and 1.0%, based on the total weight of the composition.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the halo fullerenes structurally damage and rupture the distal flagellum of spermatozoa.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the composition stimulates hyperactivation of spermatozoa.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the composition stimulates competitive behavior between spermatozoa from the same or multiple sources.

### Claim 8 (depends on 1)

The composition of claim 1, wherein the composition induces motility impediments, chemotactic stimulation, cellular membrane rupture, and subsequent neutralization of spermatozoa.

### Claim 9 (depends on 1)

The composition of claim 1, wherein the composition provides incapacitation of spermatozoa.

### Claim 10 (depends on 1)

The composition of claim 1, wherein the composition provides for topical contraception that is sperm stimulating, attracting, and spermicidal.

### Claim 11 (depends on 1)

The composition of claim 1, wherein the composition caustically and physically ruptures the cellular membrane of spermatozoa and irreversibly incapacitates the sperm.

### Claim 12 (depends on 1)

The composition of claim 1, wherein the composition causes irreversible damage for incapacitation and immobility of the spermatozoa in the presence of seminal and/or vaginal fluids.

### Claim 13 (depends on 1)

The composition of claim 1, which further comprises one or more of Helional and an aliphatic ester.

### Claim 14 (depends on 1)

The composition of claim 1, which further comprises one or more pharmaceutical grade, steroidal hormones at a concentration consistent with spermatozoa stimulation.

### Claim 15 (depends on 1)

The composition of claim 1, further comprising a natural homopolymer.

### Claim 16 (depends on 1)

The composition of claim 1, wherein the halo fullerenes are biocidal and neutralize bacterial, fungal and viral pathogens present in vaginal or seminal fluids.

### Claim 17 (depends on 1)

The composition of claim 1, wherein the composition is a liquid suspension, or wherein the composition is contained inside of a soluble capsule.

### Claim 18 (depends on 1)

The composition of claim 1, wherein the composition and post-coital exudates of incapacitated spermatozoa, cellular and molecular particulates, halo fullerene aggregates, and stimulant analytes remain neutral with respect to vaginal tissues to allow gravitational evacuation and normal vaginal secretions clearance.

### Claim 19 (depends on 17)

The composition of claim 17, wherein the composition is a buffered suspension that prolongs retention of the contraceptive for continuous efficacy.
