Abstract: In the present study, the reactions involving 4-bromo-2,6-bis-hydroxymethyl-phenol (BBHMP) and nicotinamide (NA) in the presence of Pd(II) ions were investigated. Optimum conditions for the reactions were established as pH = 7 and λ = 450 nm. According to absorbance measurements, the molar ratio of BBHMP: NA: Pd2+ was found to be 1: 2: 2. As a result of physicochemical, spectrophotometric and thermal analyses, the reactions of BBHMP and NA with Pd(II) are complexation reactions and one molecule of BBHMP and two molecules of NA react with two molecules of the Pd(II) ion.
Abstract: The aim of the present study was to evaluate the
mucoadhesion and the release of nicotinamide gel formulations using
in vitro methods. An agar plate technique was used to investigate the
adhesiveness of the gels whereas a diffusion apparatus was employed
to determine the release of nicotinamide from the gels. In this
respect, 10% w/w nicotinamide gels containing bioadhesive
polymers: Carbopol 934P (0.5-2% w/w), hydroxypropylmethyl
cellulose (HPMC) (4-10% w/w), sodium carboxymethyl cellulose
(SCMC) (4-6% w/w) and methylcellulose 4000 (MC) (3-5% w/w)
were prepared. The gel formulations had pH values in the range of
7.14 - 8.17, which were considered appropriate to oral mucosa
application. In general, the rank order of pH values appeared to be
SCMC > MC4000 > HPMC > Carbopol 934P. Types and
concentrations of polymers used somewhat affected the
adhesiveness. It was found that anionic polymers (Carbopol 934 and
SCMC) adhered more firmly to the agar plate than the neutral
polymers (HPMC and MC 4000). The formulation containing 0.5%
Carbopol 934P (F1) showed the highest release rate. With the
exception of the formulation F1, the neutral polymers tended to give
higher relate rates than the anionic polymers. For oral tissue
treatment, the optimum has to be balanced between the residence
time (adhesiveness) of the formulations and the release rate of the
drug. The formulations containing the anionic polymers: Carbopol
934P or SCMC possessed suitable physical properties (appearance,
pH and viscosity). In addition, for anionic polymer formulations,
justifiable mucoadhesive properties and reasonable release rates of
nicotinamide were achieved. Accordingly, these gel formulations
may be applied for the treatment of oral mucosal lesions.
Abstract: This study has investigated the antidiabetic and
antioxidant potential of Pseudovaria macrophylla bark extract on
streptozotocin–nicotinamide induced type 2 diabetic rats. LCMSQTOF
and NMR experiments were done to determine the chemical
composition in the methanolic bark extract. For in vivo experiments,
the STZ (60 mg/kg/b.w, 15 min after 120 mg/kg/1 nicotinamide, i.p.)
induced diabetic rats were treated with methanolic extract of
Pseuduvaria macrophylla (200 and 400 mg/kg·bw) and
glibenclamide (2.5 mg/kg) as positive control respectively.
Biochemical parameters were assayed in the blood samples of all
groups of rats. The pro-inflammatory cytokines, antioxidant status
and plasma transforming growth factor βeta-1 (TGF-β1) were
evaluated. The histological study of the pancreas was examined and
its expression level of insulin was observed by
immunohistochemistry. In addition, the expression of glucose
transporters (GLUT 1, 2 and 4) were assessed in pancreas tissue by
western blot analysis. The outcomes of the study displayed that the
bark methanol extract of Pseuduvaria macrophylla has potentially
normalized the elevated blood glucose levels and improved serum
insulin and C-peptide levels with significant increase in the
antioxidant enzyme, reduced glutathione (GSH) and decrease in the
level of lipid peroxidation (LPO). Additionally, the extract has
markedly decreased the levels of serum pro-inflammatory cytokines
and transforming growth factor beta-1 (TGF-β1). Histopathology
analysis demonstrated that Pseuduvaria macrophylla has the
potential to protect the pancreas of diabetic rats against peroxidation
damage by downregulating oxidative stress and elevated
hyperglycaemia. Furthermore, the expression of insulin protein,
GLUT-1, GLUT-2 and GLUT-4 in pancreatic cells was enhanced.
The findings of this study support the anti-diabetic claims of
Pseudovaria macrophylla bark.