Intraocular pharmacokinetics of a crystalline lipid prodrug, octadecyloxyethyl-cyclic-cidofovir, for cytomegalovirus retinitis.

Purpose: To evaluate the intraocular pharmacokinetics of octadecyloxyethyl-cyclic-cidofovir (ODE-cCDV) after intravitreal injection into rabbit eyes.

Methods: Twenty-seven New Zealand red rabbits (27 eyes) received intravitreal injections of (14)C-labeled ODE-cCDV (100 μg drug suspended in 5% dextrose), and ocular tissues were collected from 3 rabbits at each predetermined time point (1 h, 1 day, 3 days, 1 week, 2 weeks, 3 weeks, 5 weeks, and 9 weeks) after the injection. The eye globes were enucleated, and the vitreous, retina, and choroids were separated and harvested into pre-weighed scintillation vials.

Intraocular properties of a repository urokinase receptor antagonist a36 Peptide in rabbits.

Purpose: To evaluate the intraocular properties of A36, a peptide that directly antagonizes the cell surface urokinase receptor and so prevents pericellular urokinase plasminogen activator activity.

Methods: A total of 41 rabbits were used. The toxicity study tested three doses of A36: 1 mg/ eye, 0.

Intravitreal crystalline drug delivery for intraocular proliferation diseases.

Purpose: A long-lasting, slow-release, crystalline antiviral drug delivery system was initially reported using ganciclovir and cyclic cidofovir as the prototype compounds. The present study was undertaken to investigate the feasibility of applying this system to antiproliferative small molecules.

Methods: The crystalline lipid prodrugs of hexadecyloxypropyl-arabinofuranosylguanine 5'-monophosphate (HDP-P-AraG), hexadecyloxypropyl 5-fluoro-2'-deoxyuridine cyclic 3',5'-monophosphate (HDP-cP-5-F-2dUrd), and hexadecyloxypropyl 5-fluoro-2'-deoxyuridine 5'-monophosphate (HDP-P-5-F-2dUrd) were synthesized from their parent compounds arabinofuranosylguanine (AraG) and 5-fluoro-2'-deoxyuridine (5-F-2dUrd).

Toxicity and intraocular properties of a novel long-acting anti-proliferative and anti-angiogenic compound IMS2186.

Purpose: To investigate the intraocular properties and toxicity of IMS2186, a small molecule developed as an anti-choroidal neovascularization (anti-CNV) drug.

Materials And Methods: Cellular toxicity and mechanism of action was tested on cell lines in vitro. Intraocular studies used rabbits for drug dissolution as well as toxicity and rats for the treatment study as well as the toxicity confirmation study.

Discrepancy between fluorescein angiography and optical coherence tomography in detection of macular disease.

Purpose: To compare high-resolution optical coherence tomography (OCT) and fluorescein angiography (FA) in detection of macular edema (ME) of various etiologies.

Methods: In a retrospective study over a 12-month period at one retina center, data for consecutive eyes that had undergone simultaneous conventional FA (HRA; Heidelberg Engineering, Vista, CA) and StratusOCT (Carl Zeiss Meditec, Dublin, CA) to rule out ME were reviewed. A subset of patients underwent additional examination with extremely high-resolution (6-microm)/ultrahigh-speed spectral OCT/scanning laser ophthalmoscopy (OTI, Inc.

Intraocular properties of an alkoxyalkyl derivative of cyclic 9-(S)-(3-hydroxyl-2-phosphonomehoxypropyl) adenine, an intravitreally injectable anti-HCMV drug in rabbit and guinea pig.

Purpose: The aim of this study was to investigate intraocular properties and determine the highest nontoxic dose of hexadecyloxypropyl-cyclic-HPMPA (HDP-cHPMPA), a novel, potent, intravitreally injectable, slow-releasing crystalline drug for long-acting treatment of cytomegalovirus (CMV) retinitis.

Methods: Various concentrations of HDP-cHPMPA were first studied in vitro in a human foreskin fibroblast (HFF) cell line infected with human cytomegalovirus (HCMV) to determine the EC50. In vivo, 9 pigmented rabbits and 3 doses (55, 100, and 550 microg/eye) were tested in triplicate in 1 eye of each animal.

Comparison of visual acuity in macular degeneration patients measured with snellen and early treatment diabetic retinopathy study charts.

Purpose: To compare the measurements of visual acuity (VA) results measured with Snellen and Early Treatment Diabetic Retinopathy Study (ETDRS) charts in eyes with and without age-related macular degeneration (AMD).

Design: Cross-sectional study.

Participants: One hundred four participants (190 eyes) selected from a university retina practice; 80 participants (142 eyes) had some degree of AMD.

Standardized visual acuity results associated with primary versus secondary bevacizumab (avastin) treatment for choroidal neovascularization in age-related macular degeneration.

Purpose: To compare standardized visual outcomes and macular thickness changes associated with primary and secondary bevacizumab (Avastin; Genentech, Inc., South San Francisco, CA) therapy for choroidal neovascularization (CNV) in age-related macular degeneration (AMD).

Methods: Eighteen eyes received primary bevacizumab treatment; 20 eyes received pegaptanib (Macugen; Eyetech/OSI Pharmaceuticals, New York, NY) as initial treatment followed by bevacizumab therapy.

Evaluation of subretinal triamcinolone acetonide in patients with exudative age-related macular degeneration.

Purpose: The aim of this paper was to present the results of subretinal delivery of triamcinolone acetonide (TCA) in humans with choroidal neovascularization (CNV) caused by age-related macular degeneration (AMD).

Methods: Twenty two (22) eyes of 22 patients underwent pars plana vitrectomy with subretinal TCA administration. Two milligrams (2 mg) of preservative-free TCA were delivered through a 32-gauge automatic subretinal injector in 20 microL of volume.