基于接枝共聚物的粘膜粘附口腔膜 - 一种粘蛋白保留水凝胶支架。

Mucoadhesive buccal films based on a graft co-polymer - A mucin-retentive hydrogel scaffold.

机构信息

Department of Pharmacy, University of Oslo, Norway.

Department of Pharmaceutics and Biopharmaceutics, Kiel University, Germany.

出版信息

Eur J Pharm Sci. 2020 Jan 15;142:105142. doi: 10.1016/j.ejps.2019.105142. Epub 2019 Nov 7.

Abstract

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.

摘要

从以患者为中心的角度来看,口腔黏膜给药具有很大的吸引力,因为它无需吞咽即可轻松给药,并且提高了患者的安全性。本工作的目的是制备一种口腔膜,使用自形成胶束药物增溶剂作为膜基质,并结合一种具有更好的黏附性聚合物,以增强在口腔黏膜上的保留时间。具体来说,我们建议使用接枝共聚物(Soluplus®)作为增溶剂和成膜剂,并添加具有更亲水性质和已知黏附性质的聚合物;羟丙基甲基纤维素(HPMC)或改性羟丙基豌豆淀粉(Lycoat®)。该膜是通过溶剂浇铸法制造的。由 HPMC 组成的双聚合物膜表现出抗侵蚀性和优于单一聚合物对照膜的黏附性。在体外口腔模型中,这些性质与模拟口腔黏膜上的停留时间增加相关。此外,所有包含接枝共聚物的膜均显示出与类似的渗透特性,即向口腔 TR146 上皮细胞中传递呋塞米。这项工作表明,使用廉价且简单的方法制造含有先进药物递送系统的干、固、双聚合物膜是可能的。接枝共聚物与黏附性聚合物的结合可在黏蛋白保留的水凝胶支架中转化为药物增溶胶束,从而在口腔黏膜上具有更长的保留时间,实现安全且增强的先进制剂。

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