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
Terry Earl Brady, The Valley (AI); Anthony Lee Dellinger, Burlington, NC (US); Lowell Hughes, The Valley (AI); Melinda K. M. Goddard, The Valley (AI); Christopher E. Starr, New York, NY (US); and Abed Alqader Ibrahim, Greensboro, NC (US)
Filed by Terry Earl Brady, The Valley (AI); Anthony Lee Dellinger, Burlington, NC (US); Lowell Hughes, The Valley (AI); Melinda K. M. Goddard, The Valley (AI); Christopher E. Starr, New York, NY (US); and Abed Alqader Ibrahim, Greensboro, NC (US)
Filed on Sep. 28, 2023, as Appl. No. 18/374,342.
Int. Cl. A61K 33/44 (2006.01); A61K 33/38 (2006.01); A61K 45/06 (2006.01); A61K 47/36 (2006.01)
CPC A61K 33/44 (2013.01) [A61K 33/38 (2013.01); A61K 45/06 (2013.01); A61K 47/36 (2013.01)] 18 Claims
 
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.