Improving the safety of topically applied timolol in the pigmented rabbit through manipulation of formulation composition

Ability of Poly-<small>L</small>-arginine to Enhance Drug Absorption into Aqueous Humor and Vitreous Body after Instillation in Rabbits

“…1), as well as the AUC 0-60 28-fold for pyridoxamine and 18-fold for FD-4 compared with controls (Table 1). Podder et al 20) reported that the timolol concentration in the aqueous humor achieved in the presence of 0.025% benzalkonium chloride and 0.05% EDTA after instillation of 0.65% timolol solution was 1.8-and 1.6-times higher than in the controls. It has also been reported that 0.025-1% laurocapram (Azone ® ) enhanced the area of under the aqueous humor concentration-time curve (AUC aqueous humor ) of cimetidine 3.9-to 2.6-fold using eye drops containing 1% cimetidine, and 0.025-1% hexamethylene lauramide increased the AUC aqueous humor by 4.4-to 19-fold.…”

Pharmacological Evaluation of a New Timolol/Pilocarpine Formulation

“…Camber et al [12] reported that hyaluronic acid, used as a vehicle, increased the bioavailability of pilocarpine compared with a commercial preparation. It has also been shown [11] that hyaluronic acid used as a vehicle increased the ocular absorption of timolol. These data are attributed to the rheologic and mucoadhesive characteristics of hyaluronic acid.…”

“…It has also been shown that hyaluronic acid is a good vehicle for drugs administered topically to the eye [11,12]. Hyaluronic acid is a naturally occurring mucopolysaccharide consisting of residues of D-glucuronic acid and Nacetyl-D-glucosamine and is present in skin, synovial fluid as well as in the vitreous and aqueous humor.…”

Role of benzalkonium chloride in DNA strand breaks in human corneal epithelial cells

“…The mechanism of the microbiocidal action of BAC is thought to be due to disruption of the cell membranes of microorganisms. BAC has also been reported to enhance drug penetration and improve topical bioavailability of ophthalmic drugs [1][2][3].…”