Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon.
Int J Nanomedicine. 2020 Dec 14;15:10099-10112. doi: 10.2147/IJN.S288552. eCollection 2020.
Gastric ulcer is a prevalent disease with various etiologies, including non-steroidal anti-inflammatory drugs and alcohol consumption. This study aimed to explore the dual gastric protection effect of tadalafil and limonene as a self-nanoemulsifying system (SNES)-based orodispersible tablets.
Tadalafil-loaded limonene-based SNES was prepared, and the optimum formula was characterized in terms of particle size (PS), polydispersity index (PDI), and zeta potential (ZP) then loaded on various porous carriers to formulate lyophilized orodispersible tablets (ODTs). The ODTs were evaluated via determining hardness, friability, content uniformity, wetting, and disintegration time. The selected ODT was examined for its gastric ulcer protective effect against alcohol-induced ulcers in rat model. Ulcer score and ulcer index were computed for rats stomachs that were inspected macroscopically and histopathologically.
The prepared SNES had droplet size of 104 nm, polydispersity index of 0.2, and zeta potential of -15.4 mV. From the different ODTs formulated, the formula with superior wetting time: 23.67 s, outstanding disintegration time: 28 s, accepted hardness value: 3.11 kg/cm and friability: 0.6% was designated. A significant gastroprotective effect of the unloaded and tadalafil-loaded ODTs was recognized compared to the omeprazole pre-treated group. Moreover, the histopathological analysis displayed very mild inflammation in the limonene-based ODTs group and intact structure in the tadalafil-loaded pre-treated animals.
Limonene gastroprotective effect functioned along with tadalafil in the form of SNES-incorporated ODTs could serve as a promising revenue for better efficacy in gastric ulcer prevention.
胃溃疡是一种常见疾病，其病因多种多样，包括非甾体抗炎药和酒精摄入。本研究旨在探讨他达拉非和柠檬烯作为自微乳释系统（SNES）为基础的口腔分散片的双重胃保护作用。
制备他达拉非负载柠檬烯的 SNES，对最佳配方的粒径（PS）、多分散指数（PDI）和zeta 电位（ZP）进行表征，然后将其负载到各种多孔载体上，制成冻干口腔分散片（ODT）。通过测定硬度、脆碎度、含量均匀性、润湿性和崩解时间来评价 ODT。对所选 ODT 进行了酒精诱导大鼠胃溃疡的胃保护作用的研究。对大鼠胃进行宏观和组织病理学检查，计算溃疡评分和溃疡指数。
所制备的 SNES 的粒径为 104nm，多分散指数为 0.2，zeta 电位为-15.4mV。从不同的 ODT 配方中，选择具有优异润湿性时间（23.67s）、卓越崩解时间（28s）、可接受硬度值（3.11kg/cm）和脆碎度（0.6%）的配方。与奥美拉唑预处理组相比，未负载和负载他达拉非的 ODT 的胃保护作用显著。此外，组织病理学分析显示，柠檬烯 ODT 组的炎症非常轻微，而负载他达拉非的预处理动物的结构完整。
以 SNES 为载体的柠檬烯和他达拉非联合应用可能成为预防胃溃疡的一种有前途的方法。
