RT Journal Article
T1 Contact lenses for pravastatin delivery to eye segments: design and in vitro-in vivo correlations
A1 Mota, Ana F. Pereira da
A1 Vivero López, María
A1 Serramito, Maria
A1 Díaz Gómez, Luis
A1 Serro, Ana Paula
A1 Carracedo, Gonzalo
A1 Huete Toral, Fernando
A1 Concheiro Nine, Ángel Joaquín
A1 Álvarez Lorenzo, Carmen
K1 Drug-eluting contact lenses
K1 Ex vivo permeation studies
K1 In vitro ocular release tests
K1 Ocular biodistribution
K1 In vitro-in vivo correlations
AB Oral administration of cholesterol-lowering statins, HMG-CoA reductase inhibitors, is associated with beneficial effects on eye conditions. This work aims to design contact lenses (CLs) that can sustainedly deliver pravastatin and thus improve the ocular efficacy while avoiding systemic side effects of statins. Bioinspired hydrogels were prepared with monomers that resemble hydrophobic (ethylene glycol phenyl ether methacrylate) and amino (2-aminoethyl methacrylamide hydrochloride) functionalities of the active site of HMG-CoA. Best performing CLs loaded >6 mg/g, in vitro fulfilled the release demands for daily wearing, and showed anti-inflammatory activity (lowering TNF-α). High hydrostatic pressure sterilization preserved the stability of both the drug and the hydrogel network. Ex vivo tests revealed the ability of pravastatin to accumulate in cornea and sclera and to penetrate through transscleral route. In vivo tests (rabbits) confirmed that, compared to eye drops and for the same dose, CLs provided significantly higher pravastatin levels in tear fluid within 1 to 7 h of wearing. Moreover, after 8 h wearing pravastatin was present in cornea, sclera, aqueous humour and vitreous humour. Strong correlations between percentages of drug released in vitro and in vivo were found. Effects of volume and proteins on release rate and Levy plots were identified
PB Elsevier
YR 2022
FD 2022
LK http://hdl.handle.net/10347/29113
UL http://hdl.handle.net/10347/29113
LA eng
NO Journal of Controlled Release 348 (2022) 431-443
NO This project was 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). The work was also partially supported by MCIN [PID 2020-113881RB-I00/AEI/10.13039/501100011033], Spain, Xunta de Galicia [ED431C 2020/17], FEDER and by Fundação para a Ciência e a Tecnologia (FCT, Portugal) [UIDB/00100/2020 and PTDC/CTM-CTM/2353/2021]. M. Vivero-Lopez acknowledges Xunta de Galicia (Consellería de Cultura, Educación e Ordenación Universitaria) for a predoctoral research fellowship [ED481A-2019/120]
DS Minerva
RD 28 abr 2026