RESUMO
A promising controlled drug delivery system has been developed based on polymeric buccoadhesive bilayered formulation that uses a drug-free backing layer and a polymeric hydrophilic gel buccoadhesive core layer containing nifedipine. The DSC thermogravimetric analysis confirms the drug's entrapment in the gel layer and reveals no evidence of a potential interaction. Various ratios of bioadhesive polymers, including HPMC K100, PVP K30, SCMC, and CP 934, were combined with EC as an impermeable backing layer to ensure unidirectional drug release towards the buccal mucosa. The polymeric compositions of hydrophilic gel-natured HPMC, SCMC, and CP formed a matrix layer by surrounding the core nifedipine during compression. Preformulation studies were performed for all of the ingredients in order to evaluate their physical and flow characteristics. Ex vivo buccoadhesive strength, surface pH, swelling index, in vitro and in vivo drug release, and ex vivo permeation investigations were performed to evaluate the produced gel-based system. Rapid temperature variations had no appreciable impact on the substance's physical properties, pharmacological content, or buccoadhesive strength during stability testing using actual human saliva. It was clear from a histological examination of the ex vivo mucosa that the developed system did not cause any irritation or inflammation at the site of administration. The formulation NT5 was the best one, with a correlation coefficient of 0.9966. The in vitro and in vivo drug release profiles were well correlated, and they mimic the in vitro drug release pattern via the biological membrane. Thus, the developed gel-based formulation was found to be novel, stable, and useful for the targeted delivery of nifedipine.
RESUMO
The present study was made to investigate the protective effect of methanolic extract of Ficus benghalensis L., Moraceae, on isoniazid-rifampicin-induced hepatotoxicity in rats. Rats were divided into six different groups; group 1 served as a control, group 2 received isoniazid and rifampicin (100 mg/kg, i.p.), in sterile water, groups 3, 4 and 5 received 100, 200 & 300 mg/kg bw, p.o. methanolic extract of F. benghalensis and group 6 received Liv 52. All the treatment protocols followed 21 days and after rats were sacrificed blood and liver were used for biochemical and histological studies, respectively. Administration of isoniazid and rifampicin caused a significant elevation in the levels of liver marker enzymes (p<0.05 and p<0.01) and thiobarbituric acid reactive substances (p<0.001) in experimental rats. Administration of methanolic extracts of F. benghalensis significantly prevented isoniazid-rifampicin-induced elevation in the levels of serum diagnostic liver marker enzymes and TBARS level in experimental groups of rats. Morever, total protein and reduced glutathione levels were significantly (p<0.001) increased in treatment group. The effect of extract was compared with a standard drug, Liv 52. The changes in biochemical parameters were supported by histological profile. It is to be concluded that the methanolic extract of F. benghalensis protects against isoniazid and rifampicin-induced oxidative liver injury in rats.
RESUMO
The present study was made to investigate the protective effect of methanolic extract of Annona squamosa on isoniazid-rifampicin-induced hepatotoxicity in rats. Rats were divided into five different groups (n=6), group 1 served as a control, Group 2 received isoniazid (100 mg/kg, i.p.) and co-administered with rifampicin (100 mg/kg, i.p.), in sterile water, group 3 and 4 served as extract treatment groups and received 250 & 500 mg/kg bw, p.o methanolic extract of Annona squamosa and group 5 served as standard group and received silymarin 2.5 mg/kg bw, p.o. All the treatment protocols followed 21 days and after rats were sacrificed blood and liver were used for biochemical and histological studies, respectively. Administration of isoniazid and rifampicin caused a significant elevation in the levels of liver marker enzymes and thiobarbituric acid reactive substances (TBARS, oxidative stress markers) in experimental rats. Administration of methanolic extracts of Annona squamosa significantly prevented isoniazid-rifampicin-induced elevation in the levels of serum diagnostic liver marker enzymes (alanine amino transferase (ALT), aspartate amino transferase (AST), alkaline phosphatase (ALP) and gamma glutamate transpeptidase (γ-GT)), serum bilirubin, and TBARS level in experimental groups of rats. Moreover, total protein and reduced glutathione (GSH) levels were significantly increased in treatment group. The effect of extract was compared with a standard drug, silymarin. The changes in biochemical parameters were supported by histological profile. It is to be concluded that the methanolic extract of Annona squamosa protects against isoniazid and rifampicin-induced oxidative liver injury in rats.