IMPROVEMENT OF EFFICACY AND SAFETY PROFILE OF SIMVASTATIN IN COMPARISON TO REFERENCE PRODUCT (ZOCOR TABLETS) USING NANOPARTICULATE FORMULATION APPROACH

Objective: Simvastatin, a HMG-CoA reductase inhibitor widely used in the treatment of Hyper (dys) lipidemia causes myotoxicity and hepatotoxicity. These safety issues limit dose of Simvastatin, lead to additional monitoring of the patients as well as discontinuation of therapy. To alleviate the adverse effects and to improve efficacy and safety profile, Simvastatin was encapsulated in the nanoparticulate formulation and compared with marketed reference formulation (Zocor tablets). Methods: The nano particles (NPs) were prepared using single emulsion diffusion method and optimized for particle size, PDI, zeta potential, encapsulation efficiency. Results: The efficacy and safety of final formulation were evaluated in HFD induced hyperlipidemic albino rats. The results suggested that the NPs have significant improvement of efficacy and reduction of the toxicity in comparison to marketed reference formulation. Conclusion: By encapsulating the Simvastatin in the NPs, the 50% dose reduction can be achieved without compromising efficacy

FORMULATION OF CURCUMINOID LOADED SOLID LIPID NANOPARTICLES IN ORDER TO IMPROVE ORAL BIOAVAILABILITY

Objective: Solid lipid nanoparticles (SLNs) of Curcuminoids were formulated and characterized in order to improve poor oral bioavailability of Curcumin. In vivo pharmacokinetics study in rats was conducted to demonstrate improved oral bioavailability.Methods: High pressure homogenization followed by ultrasonication method was adopted to formulate solid lipid nanoparticles of Curcumin. Compritol 888 ATO and Precirol ATO 5 were explored as solid lipids with LIPOID S 75 being used as surfactant. Freeze dried solid lipid nanoparticles were compared with marketed formulation of Curcumin (Adcumin®) in rat plasma using High Pressure Liquid Chromatography (HPLC) method using ultraviolet (UV) detector.Results: Particle size measurements performed on Solid lipid nanoparticles of Curcumin revealed the mean particle size of 200-300 nm for optimized formulations and entrapment efficiency of close to 80%. Sucrose and Dextrose were suitable cryoprotectants to prepare freeze dried solid lipid nanoparticles. Curcumin loaded solid lipid nanoparticles exhibited sustained release pattern during in vitro release kinetics.Conclusion: In vivo pharmacokinetics study in Swiss albino rats revealed that encapsulation of Curcumin into solid lipid nanoparticles increased oral bioavailability of Curcumin to 12 folds when compared with marketed formulation of Raw Curcumin (Adcumin®).Â

DEVELOPMENT AND VALIDATION OF NEW RP-HPLC METHOD FOR THE ESTIMATION OF LINEZOLID IN LINEZOLID GEL

Objective: Development and validation of new RP-HPLC method for the estimation of linezolid in linezolid gel.Methods: Linezolid was chromatographed on a reverse phase symmetry C18 column (150 x 4.6 mm x 3.5 µm) in a mobile phase consisting of potassium dihydrogen phosphate buffer (pH 4.6 adjusted with 10% orthophosphoric acid) and methanol in the ratio of 55:45. The mobile phase was pumped at a flow rate of 1.2 ml/min with detection at 250 nm.Results: The retention time for Linezolid was found about 2.94 min. The detector response was linear in the concentration of 20 µg/ml to 160µg/ml with correlation coefficient of 0.9997. The percentage recovery of Linezolid at target concentration was found to be 97.8%. The limit of detection and limit of quantification was found to be 10 μg/ml and 5 μg/ml respectively. All other validation parameter were within acceptance criteria.Conclusion: The proposed method was found to be simple, fast, accurate, precise and reproducible and could be used for routine quality control analysis of Linezolid in Linezolid gel.Â

Design and Characterization of Buccoadhesive Liquisolid System of an Antihypertensive Drug

Nifedipine is an antihypertensive BCS class II drug which has poor bioavailability when given orally. The objective of the present study was to increase the bioavailability of nifedipine, by formulation and evaluation of a buccoadhesive liquisolid system using magnesium aluminium silicate (Neusilin) as both carrier and coating material and dissolution media were selected based on the solubility studies. A mixture of carboxymethylcellulose sodium and carbomer was used as mucoadhesive polymers. Buccoadhesive tablets were prepared by direct compression. FTIR studies confirmed no interaction between drug and excipients. XRD studies indicated change/reduction in crystallinity of drug. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial specifications. The dissolution studies for liquisolid compacts and tablet formulations were carried out and it was found that nifedipine liquisolid tablets formulated from bioadhesive polymers containing 49% liquisolid system, 17.5% carbomer, and 7.5% carboxymethylcellulose sodium showed the best results in terms of dissolution properties. Prepared formulation batches were evaluated for swelling, bioadhesion strength, ex vivo residence time, and permeability studies. The optimized batch was showing promising features of the system. Formulating nifedipine as a buccoadhesive tablet allows reduction in dose and offers better control over the plasma levels

A Review on Liquisolid Systems

Solubility & dissolution rate enhancement from solid oral dosage form is a key issue for current formulation and development. This review discusses, out of several techniques available, liquisolid system to improve dissolution rate of water insoluble drugs and to enhance dissolution rate of water soluble drugs. Different carriers and coating materials like Fujicalin®, Neusilin®, Avicel®, and Aerosil® can be used as carrier materials to prepare liquisolid system. Various non-volatile solvents like propylene glycol, liquid polyethylene glycols, polysorbates, glycerine, N,N-dimethylacetamide and fixed oils can be used to dissolve water insoluble molecules. Liquid drugs can be mixed directly with carriers to produce liquisolid systems. Liquisolid systems can be used to either enhance or retard drug release

Formulation and characterization of dexmedetomidine HCL liposomes in gel for intraarticular administration

Rheumatoid arthritis (RA) is a musculoskeletal disorders that distresses joints and cartilage and may lead to bone degeneration. Intraarticular administration of the drug directly in joints causes relief but is limited by the half – life of the administered drug. The objective of the present investigation therefore was to prepare Dexmedetomidine HCl containing liposomes which were then loaded in xanthan gum gel for intraarticular administration to prolong the duration of drug release. Liposome formulations were prepared by using various ratio of 1,2-Dierucoyl-sn-glycero-3-phosphatidylcholine, 1,2-Dipalmitoyl-sn-glycero-3-phospho-rac-glycerol and cholesterol using thin film hydration method in a Rota evaporator. The liposomes were evaluated for size distribution, surface charge potential, entrapment efficiency for establishing the levels of formulation components and process parameters.  Scanning electron micrographs of the liposomes indicated the spherical topography of the prepared liposomes. The liposomes were then loaded in gel formulated using xanthan gum as the gelling agents. Viscosity and gel strength of the formulation was evaluated by rheometer. In Vitro Dissolution in simulated synovial fluid media indicated that the liposomes in gel could prolong the drug release for a period of 7 days