Pullulan Based Bioconjugates for Ocular Dexamethasone Delivery

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Kickova , E , Salmaso , S , Mastrotto , F , Caliceti , P & Urtti , A 2021 , ' Pullulan Based Bioconjugates for Ocular Dexamethasone Delivery ' , Pharmaceutics , vol. 13 , no. 6 , 791 . https://doi.org/10.3390/pharmaceutics13060791

Title: Pullulan Based Bioconjugates for Ocular Dexamethasone Delivery
Author: Kickova, Eva; Salmaso, Stefano; Mastrotto, Francesca; Caliceti, Paolo; Urtti, Arto
Other contributor: University of Helsinki, Division of Pharmaceutical Biosciences

Date: 2021-06
Language: eng
Number of pages: 19
Belongs to series: Pharmaceutics
ISSN: 1999-4923
DOI: https://doi.org/10.3390/pharmaceutics13060791
URI: http://hdl.handle.net/10138/332742
Abstract: Posterior segment eye diseases are mostly related to retinal pathologies that require pharmacological treatments by invasive intravitreal injections. Reduction of frequent intravitreal administrations may be accomplished with delivery systems that provide sustained drug release. Pullulan-dexamethasone conjugates were developed to achieve prolonged intravitreal drug release. Accordingly, dexamethasone was conjugated to similar to 67 kDa pullulan through hydrazone bond, which was previously found to be slowly cleavable in the vitreous. Dynamic light scattering and transmission electron microscopy showed that the pullulan-dexamethasone containing 1:20 drug/glucose unit molar ratio (10% w/w dexamethasone) self-assembled into nanoparticles of 461 +/- 30 nm and 402 +/- 66 nm, respectively. The particles were fairly stable over 6 weeks in physiological buffer at 4, 25 and 37 degrees C, while in homogenized vitreous at 37 degrees C, the colloidal assemblies underwent size increase over time. The drug was released slowly in the vitreous and rapidly at pH 5.0 mimicking lysosomal conditions: 50% of the drug was released in about 2 weeks in the vitreous, and in 2 days at pH 5.0. In vitro studies with retinal pigment epithelial cell line (ARPE-19) showed no toxicity of the conjugates in the cells. Flow cytometry and confocal microscopy showed cellular association of the nanoparticles and intracellular endosomal localization. Overall, pullulan conjugates showed interesting features that may enable their successful use in intravitreal drug delivery.
Subject: pullulan
ocular drug delivery
controlled release
317 Pharmacy

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