Introduction: Atropine is an old-known drug which is gaining increasing attention due to the myriad of therapeutic effects it may trigger on eye structures. Nevertheless, novel applications may require more adequate topical formulations.
Areas covered: This review aims to gather the existing knowledge about atropine and its clinical applications in the ophthalmological field when administered topically. Atropine ocular pharmacokinetics is paid a special attention, including recent evidences of the capability of the drug to access to the posterior segment. Ocular bioavailability and systemic bioavailability are counterbalanced. Finally, limitations of traditional dosage forms and potential advantages of under investigation delivery systems are analyzed.
Expert opinion: Mydriasis and cyclopegia have been widely exploited for eye examination, management of anterior segment diseases, and more recently as antidotes of chemical weapons. Improved knowledge on drug receptors and related pathways explains atropine repositioning as an outstanding tool to prevent myopia. The ease with which atropine penetrates ocular tissues is a double edged sword, that is, while it ensures therapeutic levels in the posterior segment, the unspecific distribution causes a wide variety of untoward effects. The design of formulations that can selectively deliver atropine to the target tissue for each specific application is an urgent unmet need.
Keywords: Amblyopia; atropine; contact lenses; cyclopegia; mydriasis; myopia; ocular bioavailability; ocular pharmacokinetics; systemic bioavailability; uveitis.