Wu Yanping, Geng Jiayue, Cheng Xiaohong, Yang Ying, Yu Yu, Wang Lili, Dong Quanjiang, Chi Zhe, Liu Chenguang
College of Marine Life Sciences, Ocean University of China, No.5 Yushan Road, Qingdao 266003, China.
Qingdao Youdo Bioengineering Co. Ltd., No. 175 Zhuzhou Road, Qingdao 266101, China.
ACS Omega. 2022 Aug 15;7(33):29086-29099. doi: 10.1021/acsomega.2c02953. eCollection 2022 Aug 23.
infection is a leading cause of gastritis and peptic ulcer. Current treatments for are limited by the increase in antibiotic-resistant strains and low drug delivery to the infection site, indicating the need for effective delivery systems of antibiotics. Although liposomes are the most successful drug delivery carriers that have already been applied commercially, their acidic stability still stands as a problem. Herein, we developed a novel nanoliposome using cosmetic raw materials of mannosylerythritol lipid-B (MEL-B), soy bean lecithin, and cholesterol, namely, LipoSC-MELB. LipoSC-MELB exhibited enhanced stability under the simulated gastric-acid condition, owing to its strong intermolecular hydrogen-bond interactions caused by the incorporation of MEL-B. Moreover, amoxicillin-loaded LipoSC-MELB (LipoSC-MELB/AMX) had a particle size of approximately 100 nm and exhibited sustained drug release under varying pH conditions (pH 3-7). Besides, LipoSC-MELB/AMX exhibited significantly higher anti- and anti- biofilm activity as compared with free AMX. Furthermore, LipoSC-MELB was able to carry AMX across the barriers of gastric mucus and biofilms. Remarkably, in vivo assays indicated that LipoSC-MELB/AMX was effective in treating infection and its associated gastritis and gastric ulcers. Overall, the findings of this study showed that LipoSC-MELB was effective for gastromucosal delivery of amoxicillin to improve its bioavailability for the treatment of infection.
感染是胃炎和消化性溃疡的主要病因。目前针对这些疾病的治疗方法受到抗生素耐药菌株增加以及药物向感染部位递送效率低的限制,这表明需要有效的抗生素递送系统。尽管脂质体是已经在商业上应用的最成功的药物递送载体,但其酸性稳定性仍然是一个问题。在此,我们使用甘露糖赤藓糖醇脂质 -B(MEL -B)、大豆卵磷脂和胆固醇等化妆品原料开发了一种新型纳米脂质体,即LipoSC -MELB。由于MEL -B的掺入导致其分子间存在强烈的氢键相互作用,LipoSC -MELB在模拟胃酸条件下表现出增强的稳定性。此外,载有阿莫西林的LipoSC -MELB(LipoSC -MELB/AMX)粒径约为100 nm,并且在不同pH条件(pH 3 - 7)下表现出药物的持续释放。此外,与游离阿莫西林相比,LipoSC -MELB/AMX表现出显著更高的抗菌和抗生物膜活性。此外,LipoSC -MELB能够携带阿莫西林穿过胃黏液和生物膜屏障。值得注意的是,体内试验表明LipoSC -MELB/AMX在治疗幽门螺杆菌感染及其相关的胃炎和胃溃疡方面是有效的。总体而言,本研究结果表明LipoSC -MELB对于阿莫西林的胃黏膜递送是有效的,可提高其治疗幽门螺杆菌感染的生物利用度。