Daidzein (DZ), a water-insoluble isoflavone, has many beneficial effects (anti-inflammatory, antioxidant, and anticancer effects, etc.) on human health. DZ has a very low oral bioavailability related to its physicochemical properties (low solubility, intense metabolism of DZ in the intestine and liver). This study aimed to prepare and in vitro characterize the nanosuspension formulations of DZ to improve the poor solubility and efficacy of DZ. DZ nanosuspension formulations were prepared with media milling technique using zirconium oxide beads as milling media. Pluronic F127 and polyvinylpyrrolidone (PVP) K30 (formulation A; F-A) and sodium dodecyl sulfate (SDS) (SDS + pluronic F127 + PVP K30; formulation B; F-B) were used as stabilizers. The nanosuspension formulations were evaluated for morphological properties, particle sizes, zeta potential, DZ content, saturation solubility, dissolution, and their cytotoxic effects on RG2 glioblastoma tumor cells. F-A and F-B formulations were nanosized (in the range of about 181-235 nm) and had negative zeta potential values before and after lyophilization. The DZ content of F-A and F-B formulations were found to be 93.68±0.78% and 89.75±0.49%, respectively. Fourier transform infrared spectroscopy analysis showed that there was no significant interaction between DZ and the excipients. Differential scanning calorimetry and X-ray diffraction analyses confirmed no change in the crystal structure of DZ in F-A and F-B formulations. In this study, the nanosuspension formulations were successfully prepared and characterized in vitro. Nanosuspension formulations increased the saturation solubility, dissolution rate, and cytotoxic effect of DZ.
12 October 2020 in The International Journal of Lower Extremity Wounds
Wound healing remains a challenging clinical problem, especially in the presence of diabetes. Diabetic patients have the impaired ability to fight infection and insufficient inflammatory response. The aim of this study was to evaluate the effects of boronophenylalanine (BFA) and/or Zn-containing nanoemulsion (NE) formulations on wound healing in diabetic rats. MTT and scratch assays were performed to evaluate the proliferative effects of BFA and/or Zn on human dermal fibroblast (HDF) cells and the migration of these cells, respectively. The BFA and/or Zn-NE were prepared, and the effects of NEs on wound healing in diabetic rats were evaluated by applying once a day for 14 days. MTT assay showed that 10 to 25 µM BFA and/or 50 µM Zn had very significant positive effects on cell proliferation. In the scratch assay, 10 µM BFA significantly increased the migration of HDF cell compared with control. The droplet sizes of all the NEs were <115 nm and their zeta potential values were in range of (−) 23.9 ± 2.356 to (−) 33.1 ± 1.438 mV. There was a significant reduction in the wound contraction values (%) of the groups treated with the BFA and/or Zn-NE on the 14th day compared with the untreated diabetic rats group. According to histopathological findings, wound healing was nearly complete in BFA and/or Zn-NE compared with untreated diabetic rats. Especially, the group treated with the NE containing the low concentration of BFA showed highly promising results in wound healing of diabetic rats within 14 days with complete epithelialization and the completely closed wound area.
12 January 2022 in European Journal of Drug Metabolism and Pharmacokinetics
Çimento, beton üretimi içine kullanılan kalsiyum esaslı bağlayıcıların başında gelmektedir. Ayrıca uçucu kül, yüksek fırın cürufu, silis dumanı gibi endüstriyel atıkların çimento yerine kullanımı da her geçen gün artmaktadır. Günümüzde uçucu kül gibi endüstriyel atıkların beton ve çimento sektöründe kullanılması ile çevresel problemler azaltılmaktadır. Ancak çimento ve uçucu kül bünyesinde Pb, Cu, Sn, Cr, As, Mo, V, Co ve Cd gibi insan sağlığı açısından zararlı olan ağır metaller bulunmaktadır. Ağır metaller, DNA parçalanması, kromozom bozuklukları, cilt lezyonları, solunum ve sinir siteminde kalıcı hasarlara yol açmaktadır. Fakat belirtilen ağır metaller C-S-H, CH, etrenjit, monosülfat gibi hidratasyon ürünleri tarafından bağlanmaktadır. Bu sayede insan ve ekosistem için zararlı olan uçucu kül gibi endüstriyel atıklar bertaraf edilmektedir.