10.1021/acsbiomaterials.7b00706.s001
Christina Karavasili
Christina
Karavasili
Anastasia Komnenou
Anastasia
Komnenou
Orestis L. Katsamenis
Orestis
L. Katsamenis
Glykeria Charalampidou
Glykeria
Charalampidou
Evangelia Kofidou
Evangelia
Kofidou
Dimitrios Andreadis
Dimitrios
Andreadis
Sotirios Koutsopoulos
Sotirios
Koutsopoulos
Dimitrios G. Fatouros
Dimitrios G.
Fatouros
Self-Assembling Peptide Nanofiber Hydrogels for Controlled
Ocular Delivery of Timolol Maleate
American Chemical Society
2017
vivo permeation studies
AUC
I-CONH
drug solution
vivo studies
self-assembling peptide sequence
CONH 2 hydrogel
electron microscopy studies
Timolol Maleate
Controlled Ocular Delivery
24 h
self-assembling peptide hydrogels
CONH 2 peptide
Self-Assembling Peptide Nanofiber Hydrogels
β- blocker timolol maleate
form hydrogels
Ac
rheological studies
CONH 2
drug delivery
drug-loaded hydrogels
Histological studies
2017-11-04 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Self-Assembling_Peptide_Nanofiber_Hydrogels_for_Controlled_Ocular_Delivery_of_Timolol_Maleate/5605735
The
self-assembling peptides Ac-(RADA)<sub>4</sub>-CONH<sub>2</sub> and
Ac-(IEIK)<sub>3</sub>I-CONH<sub>2</sub>, which form hydrogels
in physiological conditions, were evaluated as carriers for ocular
delivery of the β-blocker timolol maleate. Electron microscopy
studies revealed that hydrogels contain nanofibers, whereas rheological
studies showed that the Ac-(IEIK)<sub>3</sub>I-CONH<sub>2</sub> self-assembles
in a stiffer hydrogel compared with the Ac-(RADA)<sub>4</sub>-CONH<sub>2</sub> peptide. The in vitro release and ex vivo permeation studies
demonstrated controlled release and transport of the drug through
the cornea, which depended on the self-assembling peptide sequence.
In vivo studies in rabbits showed significant increase in the area
under the concentration–time curve (AUC) after administration
of the drug through the Ac-(RADA)<sub>4</sub>-CONH<sub>2</sub> hydrogel
compared to drug solution, whereas a sustained reduction of intraocular
pressure for up to 24 h after instillation was achieved for both drug-loaded
hydrogels. Histological studies revealed good ocular tolerability
upon application of the formulations, suggesting that self-assembling
peptide hydrogels are promising systems for sustained ocular drug
delivery.