Echeverry Sandra M, Rey Diana P, Valderrama Ivonne H, Rodriguez Ingrid A, Sepúlveda Paula M, Araujo Bibiana Verlindo de, Silva Fátima Regina Mena Barreto, Aragón Diana Marcela
Departamento de Farmacia, Universidad Nacional de Colombia, Av. Carrera 30 # 45-03 Edif. 450, Bogotá 111321, Colombia.
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande Do Sul (UFRGS), Av. Ipiranga, 2752, Porto Alegre 90610-000, RS, Brazil.
Pharmaceutics. 2025 May 31;17(6):730. doi: 10.3390/pharmaceutics17060730.
Previous studies have shown that unformulated extracts of leaves exhibit promising antidiabetic activity. This research aimed to demonstrate that formulating the extract into a self-emulsifying drug delivery system (PLE-SEDDS) enhanced its antidiabetic activity in a high-fat-diet/streptozotocin-induced diabetic mouse model. : Blood glucose levels (BGLs) of diabetic mice were monitored during 21 days of oral administration of extract (PLE) and PLE-SEDDS. Control groups included metformin (positive control), vehicle, and SEDDS vehicle (negative controls). The animals underwent an oral glucose tolerance test (OGTT). The oxidative stress markers superoxide dismutase (SOD), catalase (CAT), and lipid peroxidation quantified by malondialdehyde (MDA) levels were measured in the kidney, liver, and pancreas, complemented with histopathological analysis. Additionally, plasma lipid profile parameters were evaluated. : The PLE-SEDDS formulation demonstrated superior efficacy compared to the PLE extract in improving antidiabetic outcomes. Animals treated with PLE-SEDDS exhibited a minimal increase in blood glucose levels (11.5%) during the OGTT, compared to 27.4% with PLE and over 77% in the vehicle groups. PLE-SEDDS also showed greater enhancement of SOD and CAT activity, along with a more pronounced reduction in MDA levels, indicating stronger protection against oxidative stress. Histological analysis revealed significant preservation of pancreatic islets, and lipid profile analysis showed greater reductions in triglycerides, cholesterol, and LDL-C, alongside increased HDL-C levels. : Altogether, these findings suggest that PLE-SEDDS exhibits superior antihyperglycemic, hypolipidemic, and antioxidant effects compared to the unformulated extract, making this novel formulation a promising option for treating type 2 diabetes mellitus.
先前的研究表明，树叶的未制剂化提取物具有良好的抗糖尿病活性。本研究旨在证明，将该提取物制成自乳化药物递送系统（PLE-SEDDS）可增强其在高脂饮食/链脲佐菌素诱导的糖尿病小鼠模型中的抗糖尿病活性。在口服提取物（PLE）和PLE-SEDDS的21天期间，监测糖尿病小鼠的血糖水平（BGLs）。对照组包括二甲双胍（阳性对照）、赋形剂和SEDDS赋形剂（阴性对照）。对动物进行口服葡萄糖耐量试验（OGTT）。在肾脏、肝脏和胰腺中测量氧化应激标志物超氧化物歧化酶（SOD）、过氧化氢酶（CAT）以及通过丙二醛（MDA）水平定量的脂质过氧化，并辅以组织病理学分析。此外，还评估了血浆脂质谱参数。与PLE提取物相比，PLE-SEDDS制剂在改善抗糖尿病结果方面表现出更高的疗效。接受PLE-SEDDS治疗的动物在OGTT期间血糖水平的升高最小（11.5%），而PLE组为27.4%，赋形剂组超过77%。PLE-SEDDS还显示出SOD和CAT活性的增强更大，同时MDA水平的降低更明显，表明对氧化应激的保护更强。组织学分析显示胰岛得到了显著保存，脂质谱分析显示甘油三酯、胆固醇和低密度脂蛋白胆固醇的降低更大，同时高密度脂蛋白胆固醇水平升高。总之，这些发现表明，与未制剂化的提取物相比，PLE-SEDDS具有更好的降血糖、降血脂和抗氧化作用，使这种新型制剂成为治疗2型糖尿病的一个有前景的选择。
