Acrylated Eudragit® E PO as a novel polymeric excipient with enhanced mucoadhesive properties for application in nasal drug delivery

Abstract

Eudragit ® E PO (EPO) is a terpolymer based on N,N-dimethylaminoethyl methacrylate with methylmethacrylate and butylmethacrylate, produced by Evonik Industries AG as a pharmaceutical excipient. In this work, EPO was chemically modified through reaction with acryloyl chloride. The successful modification of EPO was confirmed by FTIR, NMRspectroscopy, elemental and thermal analysis. The degree of acrylation was determined by permanganatometric titration. The slug mucosal irritation test was used to demonstrate nonirritant nature of EPO and its acrylated derivatives (AEPO). The mucoadhesive properties of EPO and AEPO were evaluated using freshly excised sheep nasal mucosa and it was demonstrated that acrylated polymers facilitated greater retention of sodium fluorescein on mucosal surfaces compared to solution mixture of this dye solution with EPO as well as free dye.

Recent Advancements in Using Polymers for Intestinal Mucoadhesion and Mucopenetration

“…These materials attract a lot of interest not only due to their mucoadhesive properties, but also because they are able to form hydrogels. Here, we will only highlight a few very recent examples in the context of adhesion to intestinal mucosa, although many interesting reports are focusing on applications such as wound dressing,43 ocular drug delivery,44 cargo delivery to different types of cancer,45 or adhesion to the tongue,46 the bladder mucosa,47 the nasal mucosa,48 or the buccal mucosa 49. For instance, the encapsulation of probiotic Lactobacillus acidophilus into alginate and chitosan‐alginate microspheres resulted in not only a slightly better mucoadhesion rate, but also in a 1.7× improved survival rate of the encapsulated probiotic compared to the free Lactobacillus acidophilus after 2 h exposure to simulated gastric fluid 50.…”

Progress and Current Trends in the Synthesis of Novel Polymers with Enhanced Mucoadhesive Properties

“…In order to enhance the mucoadhesive capabilities of cationic PDMAEMA nanogels, Brannigan et al quaternized the tertiary amine of the DMAEMA repeat units with acryloyl chloride, yielding highly mucoadhesive nanogels which were capable of encapsulating and releasing therapeutic compounds for the ocular drug delivery . Most recently, Porfiryeva et al used similar reaction for acrylation of Eudragit EPO, a terpolymer based on N,N‐dimethylaminoethyl methacrylate with methylmethacrylate and butylmethacrylate. This material is manufactured by Evonik Industries AG and is approved as a pharmaceutical excipient.…”

А Study of Haloperidol Release from Polycomplex Nanoparticles Based on Eudragit^® Copolymers

“…Эксперименты в независимых вертикальных ячейках Франца (PermeGear, США) проводились вручную в течение 3 часов с номинальным объемом акцепторного отсека 19 мл. В качестве буфера использовали искусственную назальную жидкость со значением pH = 5,8 [30] Исследование высвобождения также проводили модифицированным методом USP IV на тестере растворения DFZ II «Проточная ячейка» (ERWEKA GmbH, Германия) в конфигурации «закрытая петля». Обработка результатов проводилась с помощью программного обеспечения Disso.NET USP IV (ERWEKA GmbH, Германия).…”