Bilayered buccal films as child-appropriate dosage form for systemic administration of propranolol
Bilayered buccal films as child-appropriate dosage form for systemic administration of propranolol
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DOI：
10.1016/j.ijpharm.2017.08.070
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发表时间：
2017-10-05
影响因子：
5.8
通讯作者：
Bigucci, Federica
中科院分区：
文献类型：
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作者：
Abruzzo, Angela;Nicoletta, Fiore Pasquale;Bigucci, Federica
口腔粘膜已成为儿科患者全身给药的一个有吸引力的部位。该途径简单且无创，即使唾液冲洗作用和粘膜的相对渗透性可降低药物吸收。粘膜粘附聚合物代表了增加制剂在应用部位的接触时间和改善药物吸收的常用策略。在不同的粘膜粘附剂型中，口腔膜特别适用于儿科人群，因为它们薄，适合粘膜表面，并且能够提供精确和灵活的剂量。本研究的目的是开发双层口腔膜释放盐酸普萘洛尔。通过浇铸和干燥添加有不同重量比的明胶（GEL）或壳聚糖（CH）的成膜聚合物（例如聚乙烯吡咯烷酮（PVP）或聚乙烯醇（PVA））的溶液来制备初级聚合物层。为了实现朝向颊粘膜的单向药物递送，将次级乙基纤维素层施加到初级层上。双层膜的特点是其物理化学（形态，厚度，药物含量和固态）和功能（吸水，粘膜粘附，药物释放和渗透）的性质。CH包含在PVP和PVA初级层中提供了最佳的粘膜粘附能力。含有CH的膜相对于含有GEL的膜提供了较低的药物释放，并且由于其干扰脂质组织的能力，增加了通过颊粘膜的渗透药物的量。第二层乙基纤维素层不影响药物的渗透，但可限制药物在口腔中的释放。(C)2017爱思唯尔B.V.保留所有权利。
Buccal mucosa has emerged as an attractive site for systemic administration of drug in paediatric patients. This route is simple and non-invasive, even if the saliva wash-out effect and the relative permeability of the mucosa can reduce drug absorption. Mucoadhesive polymers represent a common employed strategy to increase the contact time of the formulation at the application site and to improve drug absorption. Among the different mucoadhesive dosage forms, buccal films are particularly addressed for paediatric population since they are thin, adaptable to the mucosal surface and able to offer an exact and flexible dose. The objective of the present study was to develop bilayered buccal films for the release of propranolol hydrochloride. A primary polymeric layer was prepared by casting and drying of solutions of film-forming polymers, such as polyvinylpyrrolidone (PVP) or polyvinylalcohol (PVA), added with different weight ratios of gelatin (GEL) or chitosan (CH). In order to achieve unidirectional drug delivery towards buccal mucosa, a secondary ethylcellulose layer was applied onto the primary layer. Bilayered films were characterized for their physico-chemical (morphology, thickness, drug content and solid state) and functional (water uptake, mucoadhesion, drug release and permeation) properties. The inclusion of CH into PVP and PVA primary layer provided the best mucoadhesion ability. Films containing CH provided a lower drug release with respect to films containing GEL and increased the amount of permeated drug through buccal mucosa, thanks to its ability of interfering with the lipid organization. The secondary ethylcellulose layer did not interfere with drug permeation, but it could limit drug release in the buccal cavity. (C) 2017 Elsevier B.V. All rights reserved.