# US 12,005,077 B1 · Broad-spectrum antimicrobial, biocompatible and preservative-free functionalized fullerenes ophthalmic solution with reactive oxygen species scavenging and advanced targeting, penetration, and hydration > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,005,077 B1 - Document ID: US12005077B1 - Status: Granted - Kind: B1 - Application number: 18/374,342 - Filed: 2023-09-28 - Granted: 2024-06-11 - Earliest claimed: 2023-09-28 - Applicants: Terry Earl Brady; Anthony Lee Dellinger; Lowell Hughes; Melinda K. M. Goddard; Christopher E. Starr; Abed Alqader Ibrahim - Inventors: Terry Earl Brady; Anthony Lee Dellinger; Lowell Hughes; Melinda K. M. Goddard; Christopher E. Starr; Abed Alqader Ibrahim - Web page: https://patentgrep.com/patent/US12005077B1 ## CPC - A61K 33/44: Elemental carbon, e.g. charcoal, carbon black - A61K 9/0048: {Eye, e.g. artificial tears} - A61K 31/728: Hyaluronic acid - A61K 33/38: Silver; Compounds thereof - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids - A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin - A61K 47/61: the organic macromolecular compound being a polysaccharide or a derivative thereof - A61K 47/6911: {the form being a liposome} - A61P 27/02: Ophthalmic agents - 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 introduces an ophthalmic solution containing halo-fullerenes. When the spherical fullerene carbon cages are functionalized with halogens, the resulting halo-fullerenes demonstrate sustained antimicrobial activity. Fullerenes are also characterized by unique electron properties that impart antioxidant capabilities as free radical scavengers. Nonetheless, far smaller than ocular tissue cells, halo-fullerenes are biocompatible—and capable of penetrating intricate barriers, like the cornea and conjunctiva, with potential to achieve greater efficacy and symptom relief in chronic dry eye than conventional treatments. With remarkable surface area, halo-fullerenes also allow customization and possess a unique molecular architecture for broader applications. This multifunctional solution thus imparts antimicrobial activity, antioxidative protection, molecular lubrication, and shielding from external irritants while penetrating dense ocular structures. Without the need for antibiotic additives or preservatives, the invention can offer an effective, safe option for dry eye treatment, prophylaxis in contact lens solutions, and post-surgical care. ## Claims ### Claim 1 An ophthalmic solution composition for prevention and treatment of chronic dry eye and other ocular maladies comprising: a. thiolated hyaluronic acid functionalized endohedral halo-fullerenes of C2nX, wherein n ranges from 10 to 360, and the halo-fullerenes have multiple side-chains of halogens attached to a carbon cage, and wherein said halo-fullerenes possess functionalization patterns selected from the group consisting of C60X6, C60X8, and C60X24, wherein X is a halogen molecule selected from the group consisting of iodine, bromine, chlorine, and fluorine; b. an aqueous delivery vehicle; c. a penetration enhancer; d. optionally a pharmacologically active ingredient; wherein said thiolated hyaluronic acid functionalized endohedral halo-fullerenes are modified via thiol-ene click chemistry and provide antimicrobial activity, antioxidative protection, molecular lubrication, and shielding from external irritants, facilitating penetration through ocular barriers without the need for antibiotic additives or preservatives. ### Claim 2 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes are enriched with silver nanoparticles. ### Claim 3 (depends on 1) The ophthalmic solution composition of claim 1, wherein the thiolated hyaluronic acid functionalized endohedral halo-fullerenes provide enhanced moisture-retention properties and serve as an eye lubricant. ### Claim 4 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes further comprise antimicrobial nanoparticles on the exterior of the carbon cage. ### Claim 5 (depends on 4) The ophthalmic solution composition of claim 4, wherein the antimicrobial nanoparticles are silver nanoparticles. ### Claim 6 (depends on 5) The ophthalmic solution composition of claim 5, wherein said halo-fullerenes and silver nanoparticles are encapsulated liposomal hyaluronic acid. ### Claim 7 (depends on 1) The ophthalmic solution composition of claim 1, further comprising pharmaceutically acceptable buffering agents that maintain a pH within a range of 6.0 to 8.0. ### Claim 8 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes disrupt the hydrogen-bonding network of water molecules at the surface, reducing surface tension and enhancing the spread and penetration of the composition on applied surfaces. ### Claim 9 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes maintain tear functions, improve tear film uniformity, and stabilize tear osmolarity. ### Claim 10 (depends on 1) The ophthalmic solution composition of claim 1, wherein the penetration enhancer facilitates increased absorption of the halo-fullerenes and the optional pharmacologically active ingredient(s) through the cornea and conjunctiva. ### Claim 11 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes provide sustained activity against pathogens and oxidative stress, consistent with extended cellular turnover cycles. ### Claim 12 (depends on 1) The ophthalmic solution composition of claim 1, wherein the composition is free from preservatives. ### Claim 13 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes act as a free-radical scavenger to minimize oxidative damage to ocular tissues. ### Claim 14 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes demonstrate consistent antimicrobial properties to maintain sterility, without the addition of caustic preservatives or secondary biocidal agents. ### Claim 15 (depends on 1) The ophthalmic solution composition of claim 1, wherein the halo-fullerenes can enhance the bioavailability of ophthalmic compounds when incorporated into the composition. ### Claim 16 (depends on 1) The ophthalmic solution composition of claim 1, wherein the penetration enhancer is selected from the group consisting of cyclodextrins, surfactants, and polymeric micelles. ### Claim 17 (depends on 1) The ophthalmic solution composition of claim 1, wherein said composition is compatible with contact lens use, ensuring lens clarity free of protein deposits. ### Claim 18 (depends on 1) The ophthalmic solution composition of claim 1, wherein said composition aids in the repair of epithelial defects and promotes healing of an ocular surface post-injury.