Szekalska Marta, Czajkowska-Kośnik Anna, Maciejewski Bartosz, Misztalewska-Turkowicz Iwona, Wilczewska Agnieszka Zofia, Bernatoniene Jurga, Winnicka Katarzyna
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2C, 15-222 Białystok, Poland.
Department of Pharmaceutical Technology, Medical University of Gdańsk, Hallera 107, 80-416 Gdańsk, Poland.
Pharmaceutics. 2023 Oct 3;15(10):2415. doi: 10.3390/pharmaceutics15102415.
The mucosal membrane of the oral cavity, due to its unique structure and availability, constitutes an appropriate site for the delivery of drugs, both with local and systemic effects. Mucoadhesive buccal films are drug dosage forms that due to their convenience of application, flexibility and size, are characterized by patients' compliance. Sodium alginate and pectin are natural polymers from the polysaccharides group, with mucoadhesive properties, that are widely applied to obtain buccal films. However, their hydrophilic nature and poor water resistance limit their application in sustained drug release formulations. Hence, the aim of this investigation was to design alginate/pectin buccal films by a one-step crosslinking technique-with the application of calcium carbonate. This technique was applied to prepare crosslinked alginate and alginate/pectin mucoadhesive films with a model antifungal drug-posaconazole. The obtained formulations were evaluated for the impact of crosslinking and pectin's presence on their pharmaceutical, mucoadhesive, mechanical and physicochemical properties. Additionally, the antifungal activity of the prepared films against spp. was evaluated. It was shown that pectin's presence in the formulations improved flexibility, mucoadhesion and antifungal activity. The crosslinking process reduced mucoadhesiveness and antifungal activity but significantly enhanced the mechanical properties and stability and enabled prolonged drug release.
口腔黏膜因其独特的结构和易获取性，成为局部和全身用药的合适给药部位。黏膜黏附性口腔膜剂是一种药物剂型，因其应用方便、柔韧性好且尺寸合适，具有患者依从性好的特点。海藻酸钠和果胶是多糖类天然聚合物，具有黏膜黏附特性，广泛用于制备口腔膜剂。然而，它们的亲水性和较差的耐水性限制了其在药物缓释制剂中的应用。因此，本研究的目的是通过一步交联技术——应用碳酸钙来设计海藻酸盐/果胶口腔膜剂。该技术用于制备含有模型抗真菌药物泊沙康唑的交联海藻酸盐和海藻酸盐/果胶黏膜黏附膜。评估所得制剂中交联和果胶的存在对其药学、黏膜黏附、机械和物理化学性质的影响。此外，还评估了所制备薄膜对 种的抗真菌活性。结果表明，制剂中果胶的存在改善了柔韧性、黏膜黏附性和抗真菌活性。交联过程降低了黏膜黏附性和抗真菌活性，但显著增强了机械性能和稳定性，并实现了药物的长效释放。
