Thymoquinone is a bioactive constituent of Nigella sativa seeds. It has been reported to possess antihyperglycemic effect in rats. However, the effect of nanoformulation (NF) of thymoquinone has not been reported in literature. So, the present study was designed with the aim to investigate the effect of nanoformulation of thymoquinone in streptozotocin-nicotinamide induced type-2 diabetic rats and compare its effect with pure bioactive compound as well as metformin, a standard antidiabetic drug. It is the first study reporting the use of thymoquinone NF against diabetes.

Polymeric nanocapsules (NCs) of thymoquinone and metformin were prepared by nanoprecipitation method using gum rosin, a biocompatible polymer. Box-Behnken statistical analysis tool was used for the optimization of polymer and other excipients. The NCs were then characterized with respect to particle size, stability, morphology, and in vitro drug dissolution profiles. Furthermore, thymoquinone (20, 40 & 80 mg/kg), metformin (150 mg/kg) and their nanoformulations (20, 40 & 80 mg/kg for thymoquinone and 80 mg/kg for metformin) per se were administered for 21 successive days to type-2 diabetic rats. Body weight and blood glucose levels were measured every week for 3 weeks. Serum lipid profile and glycosylated hemoglobin were estimated on 22^nd day.

The nanocapsules were stable, spherical in shape and size was less than 100 nm. Thymoquinone-and metformin-loaded NCs showed sustained release profile as compared to their pure forms. Oral administration of thymoquinone, metformin and their nanoformulations significantly decreased blood glucose level and glycated haemoglobin; and improved the lipid profile of diabetic rats as compared to diabetic control rats. Thymoquinone-loaded NCs (containing 10, 20 and 40 mg of thymoquinone) produced dose-dependent antihyperglycemic effect and this effect was comparable to thymoquinone and metformin. In conclusion, thymoquinone nanocapsules (actually containing half of the doses of thymoquinone) produced better antihyperglycemic effect in type-2 diabetic rats as compared to thymoquinone alone.

胸腺醌是黑夜蛾种子的生物活性成分。据报道在大鼠中具有降血糖作用。然而，在文献中尚未报道胸腺嘧啶的纳米制剂（NF）的作用。因此，设计本研究的目的是为了研究胸腺嘧啶纳米制剂在链脲佐菌素-烟酰胺诱导的2型糖尿病大鼠中的作用，并将其与纯生物活性化合物以及标准降糖药二甲双胍的作用进行比较。这是第一项报道使用胸腺嘧啶核苷抗糖尿病的研究。

胸腺醌和二甲双胍的聚合物纳米胶囊（NCs）是使用生物相容性聚合物松香胶通过纳米沉淀法制备的。Box-Behnken统计分析工具用于优化聚合物和其他赋形剂。然后根据粒径，稳定性，形态和体外药物溶出曲线对NC进行表征。此外，连续连续21次给予胸腺嘧啶（20、40和80 mg / kg），二甲双胍（150 mg / kg）及其纳米制剂（胸腺醌分别为20、40和80 mg / kg和二甲双胍为80 mg / kg）。天到2型糖尿病大鼠。连续3周每周测量一次体重和血糖水平。血脂谱和糖化血红蛋白估计在22^次的一天。

纳米胶囊是稳定的，球形的并且尺寸小于100nm。与纯形式相比，胸腺醌和二甲双胍负载的NCs表现出持续释放特征。口服给予胸腺醌，二甲双胍及其纳米制剂可显着降低血糖水平和糖化血红蛋白。与糖尿病对照组相比，糖尿病大鼠的血脂水平得到改善。负载胸腺醌的NCs（包含10、20和40 mg胸腺醌）产生剂量依赖性的降血糖作用，并且这种作用与胸腺醌和二甲双胍相当。总之，与单独使用胸腺醌相比，胸腺醌纳米胶囊（实际上含有一半剂量的胸腺醌）在2型糖尿病大鼠中产生了更好的降血糖作用。