Inulin-Based Polymeric Micelles Functionalized with Ocular Permeation Enhancers: Improvement of Dexamethasone Permeation/Penetration through Bovine Corneas

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Ophthalmic drug delivery is still a challenge due to the protective barriers of the eye.A common strategy to promote drug absorption is the use of ocular permeation enhancers,while an innovative approach is the use of polymeric micelles. In the present work, the twomentioned approaches were coupled by conjugating ocular permeation enhancers (PEG2000,carnitine, creatine, taurine) to an inulin-based co-polymer (INU-EDA-RA) in order to obtainself-assembling biopolymers with permeation enhancer properties for the hydrophobic drugdexamethasone (DEX). Inulin derivatives were properly synthetized, were found to expose about2% mol/mol of enhancer molecules in the side chain, and resulted able to self-assemble at variousconcentrations by varying the pH and the ionic strength of the medium. Moreover, the ability ofpolymeric micelles to load dexamethasone was demonstrated, and size, mucoadhesiveness, andcytocompatibility against HCE cells were evaluated. Furthermore, the efficacy of the permeationenhancer was evaluated by ex vivo permeation studies to determine the performance of the usedenhancers, which resulted in PEG2000 > CAR > TAU > CRE, while entrapment ability studiesresulted in CAR > TAU > PEG2000 > CRE, both for fluorescent-labelled and DEX-loaded micelles.Finally, an increase in terms of calculated Kp and Ac parameters was demonstrated, comparedwith the values calculated for DEX suspension.
Lingua originaleEnglish
pagine (da-a)1-23
Numero di pagine23
Stato di pubblicazionePublished - 2021

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