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Purpose: This study aimed to prepare, characterize, examine the stability and evaluation of the antibacterial activity of Indonesian propolis extract-loaded self-emulsifying (PESE). Methods: Oil, emulsifier, and co-emulsifier were selected as the carrier for the PESE formulation through a propolis-extract solubility test on each carrier, followed by evaluation of the nanoemulsion region in a pseudo ternary phase diagram. Pre-concentrate of PESE was prepared with the addition of 150 mg/mL propolis extract followed by characterization for the transmittance, globule size, zeta potential, thermodynamic stability, robustness to dilution, and accelerated stability. The selected formulation was tested for antibacterial activity using a microdilution method. Results: The PESE characterization produced a clear nanoemulsion with a globule size ranging from 13 to 45 nm and zeta potential of less than −38 mV. The PESE formulation with a composition of 150 mg/mL propolis extract, 20% castor oil, 40%–70% Kolliphor EL, and 10%–40% polyethylene glycol (PEG) 400 were thermodynamically stable. The PESE formulation with the composition of 20% castor oil, 40% Kolliphor EL, and 40% PEG 400 was the optimum formulation that passed the robustness to dilution evaluation and an accelerated stability test for 3 months. The antibacterial activity test on this formulation indicated improved activity against Escherichia coli and Staphylococcus aureus compared with that of propolis extract. Conclusion: These studies demonstrated that PESE in optimum formulation could be used as an antibacterial, particularly in E. coli and S. aureus. [ABSTRACT FROM AUTHOR]

Purpose: Insulin resistance is a characteristic of non-insulin-dependent diabetes mellitus associated with obesity and caused by the failure of pancreatic beta cells to secrete sufficient amount of insulin. Andrographolide (AND) improves beta-cell reconstruction and inhibits fat-cell formation. This research aimed to improve the delivery of water-insoluble AND in self-nanoemulsifying (ASNE) formulation, tested in streptozotocin (STZ)-induced diabetic rats and 3T3-L1 preadipocyte cells. Methods: A conventional formulation of AND in suspension was used as a control. The experimental rats were orally administered with self-nanoemulsifying (SNE) and suspension of AND for 8 days. Measurements were performed to evaluate blood glucose levels in preprandial and postprandial conditions. Immunohistochemistry was used to assess the process of islet beta cell reconstruction. In vitro study was performed using cell viability and adipocyte differentiation assay to determine the delivery of AND in the formulation. Results: ASNE lowered blood glucose levels (day 4) faster than AND suspension (day 6). The histological testing showed that ASNE could regenerate pancreatic beta cells. Therefore, ASNE ameliorated pancreatic beta cells. The in vitro evaluation indicated the inhibition of adipocyte differentiation by both AND and ASNE, which occurred in a time-dependent manner. ASNE formulation had better delivery than AND. Conclusion: ASNE could improve the antidiabetic activity by lowering blood glucose levels, enhancing pancreatic beta cells, and inhibiting lipid formation in adipocyte cells. [ABSTRACT FROM AUTHOR]

Purpose: This study aimed to prepare, characterize, examine the stability and evaluation of the antibacterial activity of Indonesian propolis extract-loaded self-emulsifying (PESE). Methods: Oil, emulsifier, and co-emulsifier were selected as the carrier for the PESE formulation through a propolis-extract solubility test on each carrier, followed by evaluation of the nanoemulsion region in a pseudo ternary phase diagram. Pre-concentrate of PESE was prepared with the addition of 150 mg/mL propolis extract followed by characterization for the transmittance, globule size, zeta potential, thermodynamic stability, robustness to dilution, and accelerated stability. The selected formulation was tested for antibacterial activity using a microdilution method. Results: The PESE characterization produced a clear nanoemulsion with a globule size ranging from 13 to 45 nm and zeta potential of less than -38 mV. The PESE formulation with a composition of 150 mg/mL propolis extract, 20% castor oil, 40%-70% Kolliphor EL, and 10%-40% polyethylene glycol (PEG) 400 were thermodynamically stable. The PESE formulation with the composition of 20% castor oil, 40% Kolliphor EL, and 40% PEG 400 was the optimum formulation that passed the robustness to dilution evaluation and an accelerated stability test for 3 months. The antibacterial activity test on this formulation indicated improved activity against Escherichia coli and Staphylococcus aureus compared with that of propolis extract. Conclusion: These studies demonstrated that PESE in optimum formulation could be used as an antibacterial, particularly in E. coli and S. aureus ., (© 2021 The Authors.)