Development, Characterization and Evaluation of Antidiabetic Effects of Resveratrol and Insulin Loaded Eudragit S100 Microparticles


Eren Böncü T., Yücel Ç.

III. International Science and Innovation Congress, Kayseri, Türkiye, 9 - 12 Haziran 2022, ss.17-18

  • Yayın Türü: Bildiri / Özet Bildiri
  • Basıldığı Şehir: Kayseri
  • Basıldığı Ülke: Türkiye
  • Sayfa Sayıları: ss.17-18
  • Erciyes Üniversitesi Adresli: Evet

Özet

Resveratrol (RSV), a strong antioxidant, is effective in diabetes by increasing the effectiveness of insulin, protecting beta cells that release insulin, and lowering blood glucose levels. In this study, in vitro characterization and antidiabetic effects of microparticles (MPs) containing RSV and insulin (Humulin® R), which is commercially available and accepted as a reference, were determined. MPs were prepared by emulsion solvent evaporation method using Eudragit S100 (ES100), FDA-approved and biocompatible polymer soluble at pH>7. Quantification of both drugs was performed in a validated UV spectrophotometer at wavelengths where they showed maximum absorbance (271 nm for insulin and 306 nm for RSV). Particle size (PS), zeta potential (ZP), encapsulation efficiency (EE%) and in vitro drug release of MPs were investigated. The PSs of insulin (F1) and RSV (F2) loaded MPs were 1035.7±13.5 nm and 1028.9±14.2 nm, and the ZPs were -36±3.1 mV and -35.6±2.9 mV, respectively. The EE% for insulin and RSV loaded MPs was 53.3% and 40.4%, respectively. As a result of in vitro release studies performed by static method by taking samples at 2nd, 6th and 24th hours in pH 7.4 phosphate buffer, drug releases from insulin and RSV loaded MPs were 44.7% and 49.7%, respectively. The toxicities of different concentrations of insulin (2-20 IU), resveratrol (2.5-100 µg/mL) and F1 and F2 containing in their non-toxic doses [79.3 µg/mL (2.3 IU/mL) and 66.5 µg/mL, respectively] were determined using the MTT (3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide) test on the beta TC cell line. Samples (1 mL) were administered to the control group and beta TC cells rendered diabetic by glucose stimulation to evaluate the antidiabetic effect of MPs. Glucose levels of the samples before and after 24 hours of incubation were determined using Glucose Liquicolor kit procedure. Stable RSV and insulin loaded ES100 MPs with acceptable EE%, favorable PS, ZP and in vitro release properties have been successfully produced. According to the MTT test results, while empty MPs showed over 80% viability, the MPs containing RSV and insulin at the determined doses showed over 70% viability. So, it was concluded that both insulin and RSV loaded MPs can be used safely. In order to evaluate the antidiabetic effect, it was accepted that diabetes occurred in the groups with glucose level ≥250 mg/dL. Glucose levels of both F1 and F2 formulations before and after incubation were significantly reduced in diabetic cells. It has been determined that RSV MPs have the same antidiabetic effect as the 2.19-fold dose of insulin, which plays a role in the basic treatment of diabetes. It has been proven by MTT studies that the RSV dose is also reliable. As a result, it was concluded that RSV can be used reliably as an alternative to insulin in the treatment of Diabetes Mellitus.