Department of Pharmacy, Hangzhou Children's Hospital, No.195, Wenhui Road, Xiacheng District, Hangzhou City, Zhejiang Province, 310014, China.
AAPS PharmSciTech. 2018 Jan;19(1):470-480. doi: 10.1208/s12249-017-0853-7. Epub 2017 Aug 21.
Enterovirus 71 (EV71) is a pathogenic factor of severe hand, foot, and mouth disease (HFMD). No vaccine or specific treatment is currently available for EV71 infection. Hence, we developed a buccal mucoadhesive gel containing matrine to protect against HFMD. Mucoadhesive gels were prepared by Carbopol 974P and were combined with Carbopol 971P, sodium carboxymethyl cellulose (CMC-Na), or hydroxypropylmethy cellulose (HPMC K100M). The formulations were characterized in terms of tensile testing and continuous flow techniques for mucoadhesion. The rheological studies and in vitro drug release characteristics were also investigated. The results showed that combinations of two polymers significantly improved mucoadhesion, especially Carbopol 974P blended with HPMC. Carbopol 974P to HPMC blend ratios of 1:1 and 2:1 induced better mucoadhesion in the tensile test and continuous flow method, respectively. The most sustained release was obtained at a Carbopol 974P to HPMC ratio of 2.5:1. A predominantly non-Fickian diffusion release mechanism was obtained. The gel containing 2.5% Carbopol 974P combined with 1% HPMC showed good mucoadhesion properties and sustained drug release.
肠道病毒 71 型（EV71）是引起重症手足口病（HFMD）的致病因素。目前尚无针对 EV71 感染的疫苗或特效治疗药物。因此，我们开发了一种含有苦参碱的口腔黏膜黏附凝胶来预防 HFMD。黏膜黏附凝胶由 Carbopol 974P 制备，并与 Carbopol 971P、羧甲基纤维素钠（CMC-Na）或羟丙基甲基纤维素（HPMC K100M）结合。通过拉伸试验和连续流动技术对配方的黏附性能进行了表征。还研究了流变学特性和体外药物释放特性。结果表明，两种聚合物的组合显著改善了黏膜黏附性，尤其是 Carbopol 974P 与 HPMC 的组合。在拉伸试验和连续流动法中，Carbopol 974P 与 HPMC 的比例为 1:1 和 2:1 时分别诱导出更好的黏膜黏附性。Carbopol 974P 与 HPMC 的比例为 2.5:1 时，释放最持久。获得了主要为非菲克扩散释放机制。含有 2.5% Carbopol 974P 和 1% HPMC 的凝胶表现出良好的黏膜黏附性能和持续的药物释放。
