Mehmood Yasir, Shahid Hira, Siddique Rida, Farooq Umar, Rizvi Syeda Momena, Uddin Mohammad N, Kazi Mohsin, Bourhia Mohammed, Dabiellil Fakhreldeen, Al Mughram Mohammed H
Riphah Institute of Pharmaceutical Sciences (RIPS), Riphah International University, PO. Box 38000, Faisalabad, Pakistan.
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, P.O. Box 38000, Faisalabad, Pakistan.
Sci Rep. 2025 Aug 12;15(1):29520. doi: 10.1038/s41598-025-12728-7.
The goal of this effort was to create mesoporous nanoparticles (MSNs) decorated with amine groups and loaded with liraglutide (LRT) for oral delivery. Amine-decorated MSNs were helpful for peptide entrapment and prolonged release of liraglutide, a GLP-1 analog. Liraglutide-loaded MSNs were made by using acetonitrile and water sol-gel techniques. Over the course of 24 h, the particles provided consistent drug release, with cumulative release reaching up to 90% in vitro. Differential dynamic light scattering, scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, Brunauer-Emmett-Teller (BET) analysis and differential scanning calorimetry (DSC) were used to characterize the synthesized formulation. The MTT assay was used to evaluate cell viability along with the hemolysis assay and was found to be safe. Particle size determination was performed by a zeta sizer; the size was 286 nm [Formula: see text], and the PDI and zeta potential were 0.29 and +8.89 mV, respectively. The drug entrapment efficiency was also very good at 56% ± 9%, and the drug release was more than 90.0% ± 9 within 24 h at all pH values tested. The efficacy of the particles was examined in a rat model of diabetes and contrasted with that of a group that received daily injections of liraglutide. Between 0 and 5 days after the start of treatment, lower blood sugar levels were observed in the particle treatment groups than in the injection groups. Overall, the liraglutide-loaded MSNs created in this work are effective in a rat model of diabetes, and as a result, we believe that they have great potential for clinical application.
这项工作的目标是制备表面修饰有胺基并负载利拉鲁肽(LRT)的介孔纳米颗粒(MSN),用于口服给药。胺修饰的MSN有助于肽的包封和利拉鲁肽(一种胰高血糖素样肽-1类似物)的缓释。负载利拉鲁肽的MSN通过乙腈和水溶胶-凝胶技术制备。在24小时内,这些颗粒呈现出持续的药物释放,体外累积释放率高达90%。采用差示动态光散射、扫描电子显微镜(SEM)、傅里叶变换红外(FTIR)光谱、布鲁诺尔-埃米特-泰勒(BET)分析和差示扫描量热法(DSC)对合成的制剂进行表征。MTT法用于评估细胞活力,并结合溶血试验,结果表明该制剂是安全的。通过zeta粒度分析仪测定粒径;粒径为286 nm [公式:见原文],多分散指数(PDI)和zeta电位分别为0.29和+8.89 mV。药物包封效率也非常好,为56%±9%,在所有测试的pH值下,24小时内药物释放率均超过90.0%±9%。在糖尿病大鼠模型中检测了这些颗粒的疗效,并与每日注射利拉鲁肽的组进行了对比。在治疗开始后的0至5天内,颗粒治疗组的血糖水平低于注射组。总体而言,本研究中制备的负载利拉鲁肽的MSN在糖尿病大鼠模型中有效,因此,我们认为它们具有巨大的临床应用潜力。