Purchase this article with an account.
Lina Liu, Heather Sheardown; Development of Phenylboronic Acid Containing Mucoadhesive Hydrogel Materials for Ophthalmic Drug delivery applications. Invest. Ophthalmol. Vis. Sci. 2014;55(13):455.
Download citation file:
© ARVO (1962-2015); The Authors (2016-present)
Phenylboronic acid (PBA) is a synthetic ligand containing boron atoms interact with N-acetyl groups and diol groups of mucins or other biomolecules to form a complex at neutral and weakly basic environments (at pH 7-9) such as that of the ocular mucosa (pH7.8). It is hypothesized that polymers comprising of PBA may be useful in enhancing mucoadhesion, thus improving ophthalmic drug bioavailability and enhancing site specific targeting. In this study, PBA was employed to modify hydrogel ophthalmic materials to enhance mucoadhesion facilitating drug delivery to the eye or interacting with mucoadhesive wetting agents, creating a reloadable system to increase contact lens comfort.
Polymerizable N-acryloyl-m-aminophenylboronic acid (NAAPBA) was prepared and further copolymerized with other hydrogel monomers including HEMA, DMA and NVP using UV initiated free radical polymerization. The hydrogel materials without PBA were prepared as controls. H-NMR was used to confirm existence of acryl group in NAAPBA. Potential for mucoadhesion was examined using I125 labeled mucin. Wetting agent binding was investigated using florescently labelled hyaluronan (HA) and hydroxypropyl guar (HPG). Dexamethasone and atropine were selected as model drugs for releases studies.
Incorporation of 10% NAAPBA into these materials led to a significant increase in mucin adsorption. Atropine and dexamethasone can be released from these materials and the release profiles can be altered by manipulating PBA content. With an increase in PBA content, drug release was slowed and more sustained releases could be achieved. These PBA containing materials also demonstrated interaction with the wetting agents HA and HPG.
PBA was successfully incorporated into pHEMA, PVP and pDMA hydrogels respectively to form transparent modified materials. The materials demonstrated mucoadhesion and showed drug release and wetting agent binding potential.
This PDF is available to Subscribers Only