Hammad Reham Waheed, Sanad Rania Abdel-Basset, Abdelmalak Nevine Shawky, Torad Faisal A, Latif Randa
Department of Pharmaceutics, National Organization for Drug Control and Research, Giza, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
J Adv Res. 2020 Jan 28;23:83-94. doi: 10.1016/j.jare.2020.01.013. eCollection 2020 May.
Mosapride belongs to class IV in Biopharmaceutics Classification System and is used in the treatment of reflux esophagitis. It exhibits poor bioavailability due to limited permeability, solubility and extensive first-pass metabolism. In this study, intranasal mosapride-loaded cross-linked xyloglucan Pluronic micelles (MOS-XPMs) was formulated and optimized to improve the low solubility & bioavailability of MOS. The solid dispersion technique using 2 full factorial design was applied. (MOS-XPMs) (F4) had the highest desirability value (0.952) and, therefore, it was selected as an optimal system. Xyloglucan cross-linked in the shell of Pluronic micelles offered improved stability and mucoadhesiveness to MOS-XPMs. H NMR spectra ensured the cross-linking of xyloglucan with Pluronic micelle shell and micelle stabilization. A Pharmacodynamic study revealed that MOS-XPMs showed 1.5-fold increase in duodenal and cecal motility compared to MOS suspension and 1.7-fold increase compared to the oral marketed product. The new MOS-XPMs were shown to be successful at improving the therapeutic efficacy of mosapride.
莫沙必利属于生物药剂学分类系统中的IV类药物，用于治疗反流性食管炎。由于渗透性有限、溶解度低以及广泛的首过代谢，其生物利用度较差。在本研究中，制备并优化了鼻内给药的载莫沙必利交联木葡聚糖普朗尼克胶束（MOS-XPMs），以改善莫沙必利的低溶解度和生物利用度。采用二因素全因子设计的固体分散技术。（MOS-XPMs）（F4）具有最高的可取性值（0.952），因此被选为最佳体系。交联在普朗尼克胶束外壳中的木葡聚糖提高了MOS-XPMs的稳定性和粘膜粘附性。1H NMR光谱证实了木葡聚糖与普朗尼克胶束外壳的交联以及胶束的稳定性。药效学研究表明，与莫沙必利混悬液相比，MOS-XPMs使十二指肠和盲肠运动增加了1.5倍，与口服市售产品相比增加了1.7倍。新的MOS-XPMs在提高莫沙必利的治疗效果方面显示出成功。
