Pharmacokinetics of the antineoplastic agent 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) in the aqueous and vitreous of rabbit.

1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU), an anticancer drug, was assayed in the aqueous and vitreous of rabbits after intravenous injection, subconjunctival injection, and topical application. Pharmacokinetic parameters were calculated from the time-course curves. The penetration into aqueous and vitreous across the blood-aqueous barrier and the blood-retinal barrier after intravenous injection was related to the anatomic dimensions of the eye (the volume of tissue involved and the surface area through which BCNU diffuses). To evaluate the three routes of administration, the area under the time-course curve was calculated from the simulated time-course curve. The results suggest that topical application of BCNU is the best and subconjunctival injection the second best route for treating an iris tumor, and that intravenous injection is the best route for choroidal and retinal tumors.