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Mucoadhesive buccal films based on a graft co-polymer - A mucin-retentive hydrogel scaffold.
European Journal of Pharmaceutical Sciences ( IF 4.6 ) Pub Date : 2019-11-07 , DOI: 10.1016/j.ejps.2019.105142
Julia F Alopaeus 1 , Marie Hellfritzsch 2 , Tobias Gutowski 2 , Regina Scherließ 2 , Andreia Almeida 3 , Bruno Sarmento 4 , Nataša Škalko-Basnet 5 , Ingunn Tho 1
Affiliation  

From a patient-centric perspective, oromucosal drug delivery is highly attractive due to the ease of administration without the need of swallowing, and improved patient safety. The aim of the presented work was to prepare a buccal film using a self-forming micellar drug solubiliser as the film matrix, combining it with a mucoadhesive polymer for an enhanced retention on the buccal mucosa. Specifically, we propose the use of a graft co-polymer (Soluplus®), as a solubiliser and film former, supplemented with polymers with more hydrophilic properties and known mucoadhesive properties; hydroxypropyl methylcellulose (HPMC) or modified hydroxypropyl pea starch (Lycoat®). The film was manufactured by the solvent casting method. The resulting dual polymer film containing HPMC exhibited resistance to erosion and mucoadhesive properties superior to the control films of single polymers. In an in vitro oral cavity model, these properties were shown to correlate with increased residence time on simulated oral mucosa. Furthermore, all films containing the graft co-polymer showed similar permeability characteristics of furosemide towards buccal TR146 epithelial cells. This work illustrated that it is possible to manufacture dry, solid, dual polymer films containing an advanced drug delivery system with a cheap and simple method. The combination of a graft co-polymer with a mucoadhesive polymer transform into drug solubilising micelles in a mucin-retentive hydrogel scaffold with longer retention time on buccal mucosa for safe and enhanced advanced formulation.

中文翻译:

基于接枝共聚物的粘膜粘膜颊膜-一种粘蛋白固位水凝胶支架。

从以患者为中心的角度来看,口腔粘膜药物的递送非常引人注目,因为它易于给药而无需吞咽,并提高了患者的安全性。提出的工作的目的是使用自形成的胶束药物增溶剂作为膜基质制备颊膜,将其与粘膜粘附性聚合物结合以增强在颊粘膜上的保留。具体而言,我们建议使用接枝共聚物(Soluplus®)作为增溶剂和成膜剂,并补充具有更亲水性和已知粘膜黏着性的聚合物;羟丙基甲基纤维素(HPMC)或改性羟丙基豌豆淀粉(Lycoat®)。该膜通过溶剂流延法制造。所得的包含HPMC的双聚合物膜表现出优于单一聚合物的对照膜的耐侵蚀性和粘膜粘附性。在体外口腔模型中,这些特性显示与在模拟口腔粘膜上的停留时间增加相关。此外,所有包含接枝共聚物的薄膜均显示速尿对颊TR146上皮细胞的渗透性特征。这项工作表明,可以用便宜和简单的方法来制造包含先进药物输送系统的干燥,固态,双重聚合物薄膜。接枝共聚物与粘膜粘附性聚合物的结合在粘蛋白保持性水凝胶支架中转化为可溶解药物的胶束,并在颊粘膜上具有更长的保留时间,从而可以安全和增强先进的配方。
更新日期:2019-11-07
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