Abstract
Changes in the barrier mechanisms in the eye should determine the rational route for the administration and dosage of each drug in the treatment of traumatic injuries and other pathologies. The aim of this study was to examine the efficacy of intra-arterial delivery of 14C-riboflavin (as an “indicator”) and compare it with intravenous and intramuscular administration in an animal model of chemical eye burn. 14C-riboflavin (14C-I) was administered by intra-arterial (carotid artery), intravenous (femoral vein) and intramuscular (femoral muscle) routes. The total radioactivity was determined over 2 h in the plasma and structures of the rabbit’s eyes using a scintillation counter. The results of the study show that intravascular administration of 14C-I gives significantly higher concentrations of total radioactivity in the blood and is accompanied by a significant increase in the permeability of the blood-barrier and barrier in eyes suffering from burns. The highest concentration in the plasma and aqueous humour of the anterior chamber of the eye was observed during the first hour with the intra-arterial route of administration of 14C-I in either burnt and unburnt eyes. The distribution of total radioactivity in the structures of the eye over the 2 h of the experiment showed a higher level of the drug under intra-arterial administered in the uveal regions, namely: the iris, ciliary body, choroid, retina and also the sclera and cornea. This experimental model shows that intra-arterial administration can increase the bioavailability of a drug to the structures of the eye within a short period of time.
Highlights
Changes in the barrier mechanisms in the eye should determine the rational route for the administration and dosage of each drug in the treatment of traumatic injuries and other pathologies
The highest total radioactivity in plasma was observed with intra-arterial administration of riboflavin in the initial study period (10–60 min)
The process of plasma distribution in the intra-arterial administration is characterized by a two-phase process: α-phase was observed within 10 to 60 min of the experiment, β-phase was from 60 to 120 min
Summary
Changes in the barrier mechanisms in the eye should determine the rational route for the administration and dosage of each drug in the treatment of traumatic injuries and other pathologies. The distribution of total radioactivity in the structures of the eye over the 2 h of the experiment showed a higher level of the drug under intra-arterial administered in the uveal regions, namely: the iris, ciliary body, choroid, retina and the sclera and cornea. Chemical damage to the eye, especially alkali burns that quickly penetrate the structures of the eye, is a real problem and requires immediate evaluation and treatment In this regard, the assessment of the most effective route for drug delivery in the shortest possible time is very important. Low molecular weight and lipophilic drugs can penetrate the barriers, achieving significant concentrations in the retina and vitreous tissue after systemic administration[16, 17] This effect is levelled by a large blood volume of distribution. This creates the need for large doses of drugs when they are administered systemically, rather than by local injection in order to obtain a sufficient concentration gradient in the choroid and retina
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