Abstract: Administration of therapeutic, prophylactic, or diagnostic agents that bind to a receptor or ligand in the eye or to the skin in microcrystalline form leads to increased delivery and long-lasting activity within the eye as compared with administration of the agent in non-crystalline form. Compositions and methods for delivery of active agents in microcrystalline form to the eye for the treatment, prevention and diagnosis of eye diseases and disorders are provided. In preferred embodiments, microcrystals include sunitinib malate in complex with pamoic acid. Administration of microcrystals of sunitinib malate/pamoic acid to the eye provides protection from glaucoma for up to 6 months or longer without retinal toxicity, following a single injection into the eye.