The applicability of a drug delivery system to an ophthalmic preparation was examined using lipid microspheres containing hydrocortisone 17-butyrate 21-propionate (HBP). A 3H-labelled HBP ophthalmic suspension and 3H-labelled HBP lipid microspheres were applied to rabbit eyes, which were then enucleated at fixed intervals to determine the level of 3H-labelled HBP in ocular tissues. The lipid microspheres were shown to deliver the drug to the anterior ocular tissues more effectively than the ophthalmic suspension. It is suggested that a lipid microsphere ophthalmic preparation of various lipophilic drugs including steroids may be useful as a drug delivery system for ophthalmic therapy.