Perioli Luana, Ambrogi Valeria, Angelici Fausta, Ricci Maurizio, Giovagnoli Stefano, Capuccella Marinella, Rossi Carlo
Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Via del Liceo, 1, 06123 Perugia, Italy.
J Control Release. 2004 Sep 14;99(1):73-82. doi: 10.1016/j.jconrel.2004.06.005.
A new formulation for topical administration of drugs in the oral cavity has been developed using several film-forming and mucoadhesive polymers. The films have been evaluated in terms of swelling, mucoadhesion and organoleptic characteristics. The best film, containing polyvinylpyrrolidone (PVP) as film-forming polymer and carboxymethylcellulose sodium salt (NaCMC) as mucoadhesive polymer, was loaded with ibuprofen as a model compound and in vitro and in vivo release studies were performed. Statistical investigation of in vitro release revealed that the diffusion process was the main drug release mechanism and the Higuchi's model provided the best fit. In vivo studies showed the presence of ibuprofen in saliva (range 70-210 microg/ml) for 5 h and no irritation was observed. These mucoadhesive formulations offer many advantages in comparison to traditional treatments and can be proposed as a new therapeutic tool against dental and buccal diseases and disturbs.
利用几种成膜和粘膜粘附聚合物，已开发出一种用于口腔局部给药的新制剂。已对这些薄膜在溶胀、粘膜粘附和感官特性方面进行了评估。以聚乙烯吡咯烷酮（PVP）作为成膜聚合物和羧甲基纤维素钠盐（NaCMC）作为粘膜粘附聚合物的最佳薄膜，负载布洛芬作为模型化合物，并进行了体外和体内释放研究。体外释放的统计研究表明，扩散过程是主要的药物释放机制，Higuchi模型拟合效果最佳。体内研究显示，布洛芬在唾液中的存在时间为5小时（范围为70 - 210微克/毫升），且未观察到刺激现象。与传统治疗方法相比，这些粘膜粘附制剂具有许多优点，可作为治疗牙齿和口腔疾病及不适的新治疗工具。
