Future medicinal chemistry · 2015
A potential tailor-made hyaluronic acid buccal delivery system comprising rotigotine for Parkinson's disease?
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Laffleur Flavia, Wagner Julian, Barthelmes Jan
Аннотация
AIMS: Parkinson's disease (PD) affects over 10 million people around the world. Dysphagia is one of its main problems. Therefore, mucosal delivery is beneficial for patient compliance. This study aimed to synthesize mucoadhesive hyaluronic acid (HA) comprising rotigotine for the treatment of PD.
MATERIALS & METHODS: HA - a biocompatible, naturally occurring polysaccharide - was chemically modified with the thiol-bearing ligand cysteine ethyl ester via amide bond formation (HAC). HAC was evaluated in terms of stability, cytotoxicity, permeation enhancement, controlled drug release and mucoadhesiveness.
RESULTS: HAC showed 1.49-fold higher stability, 3.47-fold improved swelling capacity and 12.16-fold augmentation in mucoadhesion. Additionally, HAC exhibited 1.18-fold permeation enhancement over HA.
DISCUSSION: Taking the findings into consideration, HAC represents a pillar of mucosal buccal delivery in the treatment of PD.
MATERIALS & METHODS: HA - a biocompatible, naturally occurring polysaccharide - was chemically modified with the thiol-bearing ligand cysteine ethyl ester via amide bond formation (HAC). HAC was evaluated in terms of stability, cytotoxicity, permeation enhancement, controlled drug release and mucoadhesiveness.
RESULTS: HAC showed 1.49-fold higher stability, 3.47-fold improved swelling capacity and 12.16-fold augmentation in mucoadhesion. Additionally, HAC exhibited 1.18-fold permeation enhancement over HA.
DISCUSSION: Taking the findings into consideration, HAC represents a pillar of mucosal buccal delivery in the treatment of PD.