Pharmacokinetics and local safety profile of propranolol eye drops in rabbits.

Abstract:

BACKGROUND:Oral propranolol, a nonselective β-blocker, is able to reduce the progression of retinopathy of prematurity in newborns, but it appeared unsafe. This study aimed to find, in rabbits, a propranolol eye drop concentration able to induce lower plasma but higher retinal concentrations than those obtained after oral administration. METHODS:Male New Zealand white rabbits were treated with oral propranolol (0.25 mg/kg/6 h) for 5 d, and propranolol concentrations were measured after 1, 2, 3, and 6 h in plasma, aqueous humor, vitreous humor, and retina. These concentrations were compared with those obtained after the administration of one drop of 25 μl of propranolol 0.1% prepared in saline, applied every 6 h to both eyes for 5 d. A Draize eye test and histological analyses were performed to assess eye drop tolerability. RESULTS:The administration of eye drops produced retinal concentrations similar to, but plasma concentrations significantly lower than, those measured after oral administration. The local tolerability profile was excellent. CONCLUSION:Propranolol eye drops are able to ensure high retinal and low plasma concentrations of propranolol, and this finding opens the perspective of possible topical treatment with propranolol in newborns with retinopathy of prematurity.

journal_name

Pediatr Res

journal_title

Pediatric research

authors

Padrini L,Isacchi B,Bilia AR,Pini A,Lanzi C,Masini E,Della Bona ML,Calvani AM,Ceccantini R,la Marca G,Filippi L

doi

10.1038/pr.2014.108

subject

Has Abstract

pub_date

2014-10-01 00:00:00

pages

378-85

issue

4

eissn

0031-3998

issn

1530-0447

pii

pr2014108

journal_volume

76

pub_type

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