Liposomally-entrapped ganciclovir for the treatment of cytomegalovirus retinitis in AIDS patients. Eperimental toxicity and pharmacokinetics, and clinical trial.

Important note: Information in this article was accurate in 1993. The state of the art may have changed since the publication date.

Liposomally-entrapped ganciclovir for the treatment of cytomegalovirus retinitis in AIDS patients. Eperimental toxicity and pharmacokinetics, and clinical trial.

Doc Ophthalmol. 1992;82(4):297-305. Unique Identifier : AIDSLINE MED/93314554
Diaz-Llopis M; Martos MJ; Espana E; Cervera M; Vila AO; Navea A; Molina FJ; Romero FJ; Department of Surgery, School of Medicine and Dentistry,; University of Valencia, Spain.

Abstract: Treatment of retinitis by cytomegalovirus (CMV) in AIDS patients requires frequent repetitive injections of intravitreal ganciclovir (GCV). This study was undertaken to establish experimentally whether the intravitreal application of liposomally-entrapped GCV could prolong intraocular therapeutic levels when compared with the intravitreal injection of free GCV, and the clinical effectiveness of this approach in AIDS patients. Intraocular concentration of GCV was determined by means of an ELISA test in rabbit vitreous 2, 3, 7, and 14 days after a single intravitreal injection of either different doses of the free drug (0.2-20 mg) or 1 mg of liposomally-entrapped GCV. After 72 h, only the vitreous of rabbits injected with doses of free GCV greater than or equal to 5 mg showed therapeutic levels of the drug; no GCV was detected after 72 h with any of the doses applied. Moreover, the microscopic study revealed GCV-induced damage in retinal structures in the animals injected with a free GCV dose greater than or equal to 15 mg. Intravitreal injection to rabbits of 1 mg of liposomally-encapsulated GCV showed no retinal toxicity at any of the time points studied, and therapeutic levels were detected up to 14 days after injection (4.67 +/- 0.39 microgram/ml). Five AIDS patients suffering CMV retinitis were injected with 0.5 mg of liposomally-entrapped GCV (2 mg of lecithin). Complete remission of the CMV retinitis was observed already at the third injection of 0.5 mg GCV (one per week) and relapse did not occur during the 2-4 month follow-up of the patients. In view of the results presented, it can be concluded that intravitreal injection of liposomally-encapsulated GCV increases the time period required for reinjections in the treatment of CMV retinitis.

Keywords: Animal AIDS-Related Opportunistic Infections/*DRUG THERAPY Cytomegalovirus Infections/*DRUG THERAPY Drug Carriers Eye Infections, Viral/*DRUG THERAPY Follow-Up Studies Ganciclovir/*ADMINISTRATION & DOSAGE/PHARMACOKINETICS/*TOXICITY Human Liposomes Rabbits Retina/*DRUG EFFECTS Retinitis/*DRUG THERAPY/MICROBIOLOGY Support, Non-U.S. Gov't Treatment Outcome CLINICAL TRIAL JOURNAL ARTICLE
931030
M93A0753

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