Liposomes for intravitreal drug delivery: A state of the art

Intravitreal administration of drugs has raised a large interest during the last two decades improving the treatment of infectious diseases of the posterior segment of the eye or edematous maculopathies. This route of administration allows achieving high drug concentrations in the vitreous and avoiding adverse effects resulting from systemic administration. However, many drugs are rapidly cleared from the vitreous humor; therefore, to reach and to maintain effective therapy, repeated administrations are necessary. Unfortunately, frequent intravitreal injections increase the risk of endophthalmitis, damage to lens, retinal detachment. Moreover, some drugs provoke a local toxicity at their effective dose inducing side-effects and possible retinal lesions. This is the reason why new drug delivery systems, among which liposomes, have been developed to improve the intravitreal administration of drugs. Liposomes can reduce the toxicity and increase the residence time of several active molecules in the eye. In vivo, they can protect poorly-stable drugs such as peptides and nucleic acids from degradation. Successful reports have shown their potential for improving the treatment of retinitis induced by cytomegalovirus in human and more recently for the treatment of uveitis in rats. Moreover, recent preliminary studies about the trafficking of liposomes in ocular tissues and fluids following intravitreal injection attempted to elucidate their fate. All the data discussed in this review support the large interest raised by these colloidal carriers for intravitreal drug delivery. (c) 2012 Elsevier B.V. All rights reserved.