Nagesh H. Aloorkar

Microsponges based novel drug delivery system for augmented arthritis therapy

The motive behind present work was to formulate and evaluate gel containing microsponges of diclofenac diethylamine to provide prolonged release for proficient arthritis therapy. Quasi-emulsion solvent diffusion method was implied using Eudragit RS-100 and microsponges with varied drug–polymer ratios were prepared. For the sake of optimization, diverse factors affecting microparticles physical properties were too investigated. Microsponges were characterized by SEM, DSC, FT-IR, XRPD and particle size analysis, and evaluated for morphology, drug loading, in vitro drug release and ex vivo diffusion as well. There were no chemical interactions between drug and polymers used as revealed by compatibility studies outcomes. The drug polymer ratio reflected notable effect on drug content, encapsulation efficiency and particle size. SEM results revealed spherical microsponges with porous surface, and had 7.21 μm mean particle size. The microsponges were then incorporated in gel; which exhibited viscous modulus along with pseudoplastic behavior. In vitro drug release results depicted that microsponges with 1:2 drug–polymer ratio were more efficient to give extended drug release of 75.88% at the end of 8 h; while conventional formulation get exhausted incredibly earlier by releasing 81.11% drug at the end of 4 h only. Thus the formulated microsponge-based gel of diclofenac diethylamine would be a promising alternative to conventional therapy for safer and efficient treatment of arthritis and musculoskeletal disorders.

Protective effect of Tritone (Livosone) on oxidative DNA damage and its hepatoprotective potential against various hepatotoxic agent in wistar rats

AIM To evaluate antioxidant activity, DNA damage inhibition and hepatoprotecitve potential of polyherbal formulation Tritone (Livosone). METHODS In vitro antioxidant activity of Tritone formulation was performed by using DPPH assay. Hepatoprotecitve potential of Tritone was evaluated against various hepatotoxic agents including Paracetamol (2g/kg b. wt p.o. single dose on 15th day), Galactosamine (400mg/kg b. wt. i.p. single dose on 8th day) and Alcohol (30% p.o.1ml/100g of rat for 15days). Tritone formulation at the doses of (40.5, 81 and 162mg/kg) and standard silymarin (100mg/kg) and Liv52 (270mg/kg) were administered p.o. The hepatoprotective assessment was done by estimating biochemical parameters: SGOT, SGPT, ALP and Total Bilirubin total protein and ChE levels. Additionally histopathological and DNA fragmentation study of Tritone was also performed. RESULT Administration of hepatotoxins (paracetamol, D-GaiN and alcohol) in experimental animals showed significant biochemical, histological deterioration and DNA fragmentation. Pretreatment with Tritone (Livosone) shows significant reduction in serum SGOT, SGPT, ALP and total bilirubin levels and shows significant elevation in total protein and cholinesterase (ChE) levels compared to groups treated with hepatotoxic agents. Histopathological observations of rat liver pretreated with Tritone (Livosone) shows significant protection against hepatic damage. Inhibition of DNA fragmentation by Tritone indicates protective effect of formulation on liver at molecular level. Finally all the results were compared with standard drugs Silymarin and Liv52. CONCLUSION Correlation of antioxidant activity, biochemical results, histopathological changes and inhibition of DNA damage after treatment with Tritone shows maximum hepatoprotective potential at dose 81mg/kg and 162mg/kg.