Abstract: The treatment of many ocular disorders is hampered because of poor penetration of systemically administered drugs into the eye. The tight junctional complexes (zonulae occludens) of the retinal pigment epithelium and retinal capillaries are the site of the blood-ocular barrier. This barrier inhibits penetration of substances, including antibiotics, into the vitreous. Over the last 18 years we have evaluated the nontoxic doses of various drugs. These include antibiotics and antifungals for treatment of bacterial and fungal endophthalmitis, antivirals for treatment of viral retinitis (specifically, when medication with these drugs poses the threat of toxicity to other organs). Intravitreal antineoplastic drugs have been studied to prevent cell proliferation in the vitreous cavity after retinal attachment surgery, which can lead to proliferative vitreoretinopathy (PVR).

Abstract: The present invention provides compositions comprising PAMAM dendrimers conjugated with one or more biologically active agents, and their use systemically to target activated microglia/macrophages in retina/choroid and generally, inflammatory and/or angiogenic diseases of the eye.