June 2022
Volume 63, Issue 7
Open Access
ARVO Annual Meeting Abstract  |   June 2022
Contact lenses that deliver statins
Author Affiliations & Notes
  • Ana Filipa Pereira-da-Mota
    Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Facultad de Farmacia, Instituto de Materiales (iMATUS) and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, Santiago de Compostela, Spain
  • María Vivero-López
    Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Facultad de Farmacia, Instituto de Materiales (iMATUS) and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, Santiago de Compostela, Spain
  • María Serramito
    Ocupharm Research Group, Facultad de Óptica y Optometría, Universidad Complutense de Madrid, Madrid, Spain
  • Fernando Huete-Toral
    Ocupharm Research Group, Facultad de Óptica y Optometría, Universidad Complutense de Madrid, Madrid, Spain
  • Gonzalo Carracedo
    Ocupharm Research Group, Facultad de Óptica y Optometría, Universidad Complutense de Madrid, Madrid, Spain
  • Angel Concheiro
    Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Facultad de Farmacia, Instituto de Materiales (iMATUS) and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, Santiago de Compostela, Spain
  • Carmen Alvarez-Lorenzo
    Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Facultad de Farmacia, Instituto de Materiales (iMATUS) and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, Santiago de Compostela, Spain
  • Footnotes
    Commercial Relationships   Ana Filipa Pereira-da-Mota None; María Vivero-López None; María Serramito None; Fernando Huete-Toral None; Gonzalo Carracedo None; Angel Concheiro None; Carmen Alvarez-Lorenzo None
  • Footnotes
    Support  This project is funded by the European Union’s Horizon 2020 research and innovation programme under the Marie Skłodowska-Curie Actions grant agreement N° 813440 (ORBITAL–Ocular Research by Integrated Training And Learning).
Investigative Ophthalmology & Visual Science June 2022, Vol.63, 1854. doi:
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    • Get Citation

      Ana Filipa Pereira-da-Mota, María Vivero-López, María Serramito, Fernando Huete-Toral, Gonzalo Carracedo, Angel Concheiro, Carmen Alvarez-Lorenzo; Contact lenses that deliver statins. Invest. Ophthalmol. Vis. Sci. 2022;63(7):1854.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Purpose : The oral administration of statins, 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitors, has been associated with beneficial effects on eye conditions due to their pleiotropic effects. The efficacy of its use could be improved if efficient ocular formulations are developed reducing the side effects related with the systemic absorption. The objective of the work was to design contact lenses (CLs) as platforms for the prolonged release of statins (pravastatin sodium). A bioinspired strategy was used to mimic the active site of HMG-CoA.

Methods : Bioinspired hydrogels were prepared from mixtures of 2-hydroxyethyl methacrylate (HEMA), ethylene glycol phenyl ether methacrylate (EGPEM), and 2-aminoethyl methacrylamide hydrochloride (APMA). A physicochemical characterization of the hydrogels was carried out. The hydrogels were loaded by soaking in a pravastatin solution during 48h. Drug release was monitored in simulated lacrimal fluid. Ex vivo porcine cornea and sclera permeability was assessed using vertical diffusion cells. Pravastatin was administered as eye drops and as CLs to male New Zealand white rabbits. The levels of pravastatin in tear fluid were collected using Schirmer test strips. The drug accumulated in cornea, sclera, crystalline, aqueous and vitreous humour, and retina was also quantified.

Results : The incorporation of APMA monomer (E200A40 and E0A40 hydrogels) remarkably increased the amount of pravastatin loaded (7.26±0.6 and 6.70±0.2 mg/g, respectively, Figure 1), without altering the swelling, transmittance, mechanical properties and ocular compatibility typical of soft CLs. The CLs sustained the in vitro release for 1 day. In ex vivo permeability tests, pravastatin was detected in the receptor chamber through transscleral permeation. In in vivo tests, the eye drops resulted in measurable pravastatin levels for 1h. The permanence of the drug in tear fluid was prolonged for more than 8h when it was administered as CLs. Among the ocular tissues evaluated, pravastatin was detected in the cornea (158.5±31.8 ng/g), sclera (1.53±0.6 ng/g), aqueous (108.7±47.5 ng/g) and vitreous humour (2.00±0.6 ng/g).

Conclusions : The design of CLs applying a bioinspired strategy allows the incorporation of pravastatin without altering the properties required as a medical device. Pravastatin-loaded CLs have a great potential to serve as a novel delivery system for the treatment of disorders affecting the anterior and posterior segment of the eye.

This abstract was presented at the 2022 ARVO Annual Meeting, held in Denver, CO, May 1-4, 2022, and virtually.

 

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