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Sustained Delivery of Timolol Maleate for Over 90 Days by Subconjunctival Injection.

  • Academic Journal
  • Lavik E; 1 Department of Chemical, Biochemical, and Environmental Engineering, University of Maryland-Baltimore County , Baltimore, Maryland.
    Kuehn MH; 2 Department of Ophthalmology and Visual Sciences, The University of Iowa , Iowa City, Iowa.; 3 Iowa City Veterans Affairs Center for the Prevention and Treatment of Visual Loss , Iowa City, Iowa.
    Shoffstall AJ; 4 Department of Biomedical Engineering, Case Western Reserve University , Cleveland, Ohio.
    Atkins K; 4 Department of Biomedical Engineering, Case Western Reserve University , Cleveland, Ohio.
    Dumitrescu AV; 2 Department of Ophthalmology and Visual Sciences, The University of Iowa , Iowa City, Iowa.
    Kwon YH; 2 Department of Ophthalmology and Visual Sciences, The University of Iowa , Iowa City, Iowa.
  • Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics [J Ocul Pharmacol Ther] 2016 Dec; Vol. 32 (10), pp. 642-649. Date of Electronic Publication: 2016 Nov 11.
  • English
  • Purpose: Medical treatment of glaucoma relies on intraocular pressure (IOP)-lowering medications, typically administered daily by the patient. While these medications are effective when applied correctly, patient adherence is a major obstacle in glaucoma treatment. We have developed a sustained-release formulation of timolol maleate that can be injected subconjunctivally to avoid patient noncompliance.
    Methods: A biodegradable microsphere formulation for timolol maleate was injected subconjunctivally in normal rabbits. We measured timolol levels in tears, aqueous humor, vitreous humor, and serum of study rabbits. Furthermore, IOP profiles were recorded longitudinally. Tissue compatibility and side effects were evaluated using histochemistry.
    Results: The microsphere formulation led to measureable amounts of timolol in the aqueous humor and the tear film for up to 90 days. Timolol was not detectable in the serum at any time. A significant reduction of IOP was observed in treated eyes. Clinically, the subconjunctival administration of the microspheres was well tolerated with no signs of inflammation or infection. The absence of local inflammation was confirmed by histology.
    Conclusions: A single subconjunctival administration of timolol microspheres achieved delivery and IOP reduction in rabbits for up to 90 days without local or systemic inflammation or toxicity. This approach has the potential to improve the management of glaucoma in patient populations, who are challenged to adhere to a regimen of daily eye drops.
    Competing Interests: Author Disclosure Statement No competing financial interests exist.
Additional Information
Publisher: Association For Ocular Pharmacology And Therapeutics Country of Publication: United States NLM ID: 9511091 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1557-7732 (Electronic) Linking ISSN: 10807683 NLM ISO Abbreviation: J Ocul Pharmacol Ther Subsets: MEDLINE
Publication: New York, NY : Association For Ocular Pharmacology And Therapeutics
Original Publication: New York, NY : The Association, c1995-
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DP2 OD007338 United States OD NIH HHS
Keywords: glaucoma pharmacology; rabbit; sustained delivery; timolol maleate
0 (Delayed-Action Preparations)
817W3C6175 (Timolol)
Date Created: 20161112 Date Completed: 20171106 Latest Revision: 20181113