title: Decrease in corneal damage due to benzalkonium chloride by the addition of sericin into timolol maleate eye drops.
abstract: We investigated the protective effects of sericin on corneal damage due to benzalkonium chloride (BAC) used as a preservative in commercially available timolol maleate eye drops using rat debrided corneal epithelium and a human cornea epithelial cell line (HCE-T). Corneal wounds were monitored using a fundus camera TRC-50X equipped with a digital camera; eye drops were instilled into the rat eyes five times a day after corneal epithelial abrasion. The viability of HCE-T cells was calculated by TetraColor One; and Escherichia coli (ATCC 8739) were used to measure antimicrobial activity. The reducing effects on transcorneal penetration and intraocular pressure (IOP) of the eye drops were determined using rabbits. The corneal wound healing rate and rate constants (kH) as well as cell viability were higher following treatment with 0.005% BAC solution containing 0.1% sericin than in the case of treatment with BAC solution alone; the antimicrobial activity was approximately the same for BAC solutions with and without sericin. In addition, the kH for rat eyes instilled with commercially available timolol maleate eye drops containing 0.1% sericin was significantly higher than that of eyes instilled with timolol maleate eye drops without sericin, and the addition of sericin did not affect the corneal penetration or IOP reducing effect of commercially available timolol maleate eye drops. A preservative system comprising BAC and sericin may provide effective therapy for glaucoma patients requiring long-term anti-glaucoma agents.
authors.affiliation: School of Pharmacy, Kinki University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan.
authors.forename: Noriaki
authors.initials: N
authors.lastname: Nagai
authors.forename: Yoshimasa
authors.initials: Y
authors.lastname: Ito
authors.forename: Norio
authors.initials: N
authors.lastname: Okamoto
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Shimomura
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D001548:Benzalkonium Compounds / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D003315:Cornea / Q000166:cytology / Q000187:drug effects*; D004847:Epithelial Cells / Q000166:cytology / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D009883:Ophthalmic Solutions / Q000737:chemistry*; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D047030:Sericins / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013999:Timolol / Q000737:chemistry*; D014945:Wound Healing / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D001548:Benzalkonium Compounds; D009883:Ophthalmic Solutions; D047030:Sericins; D013999:Timolol