Formulasi dan Uji Efek Antidiabetes Nanoliposom Ekstrak Buah Terung Bulat Hijau (Solanum xanthocarpum Schrader & Wendland) pada Tikus Jantan

Abstract

Drug delivery systems can affect the effects of drugs in the body. One of the most rapidly used drug delivery systems is the nanoliposome form. This form can be applied in various drug dosage forms, both modern medicines and natural medicine in the form of extracts. Green round eggplant (GRE) (Solanum xanthocarpum Schrader & Wendland) is known to contain quercetin and flavonoids which act as antidiabetic, antioxidant and anti-inflammatory. This study aims to examine the nanoliposome formulation in green round eggplant extract which is the most active as an antidiabetic. The study was conducted experimentally on Wistar rats. Standardization and phytochemical screening were carried out on simplicia and extracts. The extract was obtained by multilevel maceration method using n-hexane (NHEGRE), ethyl acetate (EAEGRE), ethanol (EEGRE) and water (WEGRE) as solvents. The glucose tolerance test was carried out in normal experimental animals, while the antidiabetic, antioxidant and anti-inflammatory activity test was carried out in rats with type 2 diabetes mellitus induced by streptozotocin and nicotinamide in 3 stages. First, 6 groups (n=5): negative control (K(-)), positive control (Glibenclamide (K(+)), extract (NHEGRE; EAEGRE; EEGRE; WEGRE dose of 200 mg/kgbb), treated for 15 days with parameters of blood glucose levels. Second, optimization of nanoliposome formulations with organoleptic parameters of particle size, polydispersity index, zeta potential, particle size morphology, adsorption efficiency, stability and drug release test. Third, evaluation of the nanoliposome formulation was carried out on the most active extract treated for 21 days with the parameters of blood glucose levels, insulin levels, pancreatic histopathology, SOD, MDA and TnF-alpha. The characteristics of the simplicia and the extract meet the Indonesian Materia Medika standards. The results showed that in the glucose tolerance test, the highest percentage decrease of blood glucose levels at 120 minutes was observed in the group treated with EAEGRE 200 mg/kgbb, which was 60.91% and has not a significant difference with glibenclamide 0.45 mg/kgbb, which was 60.90%. In the antidiabetic activity test on the 15th day, the mean percentage decrease of KGD in each group of rats showed that the group treated with EAEGRE 200 mg/kgbw had the highest percentage decrease of blood glucose levels, which was 72.47% and has not a significant difference with glibenclamide 0.45 mg/kgbw, which was 72.38%. The results showed that the ethyl acetate extract had the most potential as an antidiabetic Based on the evaluation of the nanoliposome formulation, the chosen or optimum nanoliposome is the one made with 30 minutes of sonication time. The resulting nanoliposome is dark green in color, odorless, and has a thick consistency. The pH test results for F1, F2, and F3 are 5.97±0.06, 6.13±0.06, and 5.97±0.15, respectively. The particle size results for F1, F2, and F3 are 162.57±6.37 nm, 143.97±0.64 nm, and 154.17±0.51 nm, respectively. The polydispersity index (PI) results are F1 (0.239±0.02), F2 (0.263±0.07), and F3 (0.273±0.01). The zeta potential results are F1 (-42.133±0.586), F2 (-25.367±0.404), and F3 (- 53.367±0.115). All nanoliposome formulations are stable during storage at low temperature. The morphology of the nanoliposomes is spherical and multilamellar. Entrapment efficiency F1 (89.711 ± 0.873), F2 (92.981 ± 0.347), and F3 (90.670 ± 0.095), Formula I, II, and III meet the requirements for sustained release and belong to zeroorder with constant drug release. The results showed that in the test of decreasing blood glucose levels, the highest percentage was observed in the group treated with NEAEGRE (nanoliposome ethyl acetate extract of green round eggplant) at a dose of 100 mg/kgbw (body weight), which was 74.31%. The highest level of insulin was observed in the NEAEGRE 100 mg/kgbw group (615.223 pg/ml), Histopathology of the pancreas showed that the group treated with NEAEGRE at a dose of 100 mg/kgbw showed a histopathological picture that approached the normal group, The SOD level for NEAEGRE at a dose of 100 mg/kgbw was 11.73 ng/ml, The lowest MDA level was observed in the NEAEGRE 100 mg/kgbw group (4.619 ng/ml) and The lowest level of TNF-α was observed in the NEAEGRE 100 mg/kgbw group (1.213 pg/ml), Nanoliposomes of ethyl acetate extract of green round eggplant dose of 100 mg/kgbb showed the best antidiabetic, antioxidant and anti-inflammatory activities characterized by the lowest levels of blood glucose lev, MDA, and TNF-α and the highest levels of insulin and SOD with near-normal histopathological features.