International Journal of Pharmaceutical Sciences and Drug Research

308-314

Authors: D. Nagasamy Venkatesh*, H. C Kiran, S. Shashikumar, V. Indurekha, K. J Thirumalai Subramaniam, A. Uma Rani

Dendrimers are synthetic, highly branched, monodisperse macromolecules of nanometer dimensions with exact and large number of functional groups, distributed with unprecedented control, makes them a promising scaffolds, for drug delivery. Dendrimers serves as an ideal vehicle for cancer therapy, immunology, vaccines, antivirals, biosensors for diagnostics, neuron capture therapy, photodynamic therapy and photo thermal therapy. Dendrimers chemistry is one of the most fascinating and rapidly expanding areas in the field of chemistry. Prior to the dendrimer technology, nanoparticle drug delivery systems were one of the choicest systems owing to their selectivity and stability of therapeutic agents incorporated into the system. However, few drawbacks such as reticuloendothelial system (RES) uptake, drug leakage, immunogenicity, hemolytic toxicity, cytotoxicity, hydrophobicity etc., impede the usage of these nanostructures. Further, these shortcomings shall be circumvented by modifying the surface engineering, such as poly ester dendrimer, arginine dendrimer, glycol dendrimer, PEGylated dendrimers etc., Unique properties of uniform size, water solubility, modifiable surface functionality and availability of internal cavities makes them intriguing carrier for biological and drug delivery system. In the present review, we focused on the bioactive agents that can be easily encapsulated into the interior cavity (or) chemical attachment, conjugation (or) physically adsorbed on to the dendrimer surface to serve the desired properties of the carrier to cater specific needs of the active components, its characterization and application.

321-328

Authors: Karva G. S.1*, Katariya V. R.2, Shahi S. R.1

The aim of present work was to improve the dissolution rate of Ritonavir by preparing micro-particles with certain hydrophilic polymers via spray drying technique. Role of spray drying method was studied for solubility enhancement of poorly aqueous soluble model Ritonavir using solid dispersion approach. All the carriers showed dissolution improvement vis-à-vis pure drug in varying degrees. The solid dispersions were characterized in comparison with pure drug and corresponding Physical mixture (PM). The prepared solid dispersion were evaluated by drug content analysis, saturation solubility, DSC (Differential scanning calorimeter), SEM (Scanning electron microscopy), PXRD (Powder X-ray diffraction), FTIR (Fourier transform infrared spectroscopy).and in vitro drug release. Absence of pure drug peaks in PXRD suggests transformation of crystalline drug into an amorphous form. The transformation of Ritonavir from crystalline to amorphous state by spray drying and the hydrophilic coating of drug particles by the polymers are considered for improvement of Solubility and dissolution of Ritonavir.

334-339

Authors: Dharmik D Patel1*, Ketan P Modi2, Anil K Patel3

The present study was conducted to find out the changes in immunosuppressant drug prescription pattern and trends in kidney transplant patients. In this study 613 Indian transplant patients who underwent kidney transplantation between July 2004 and June 2011 were enrolled. Various data of all transplant patients including immunosuppressant drug medication, changes in the prescription, use of antibody for induction and antirejection treatment were collected during their hospital stay and ambulatory visit. Antibody use as an induction agent has increased from during the study period. Induction was used in 23.1% during the year 2005 and increased to 44.4% during the year 2009. Among induction agent ATG was most commonly preferred agent, followed by daclizumab and basiliximab (24% ATG Vs 6.9% daclizumab Vs 6.9% basiliximab). Use of tacrolimus has increased (94% on tacrolimus vs 6% on cyclosporine in 2010). Mycophenolate mofetil is most commonly used antiproliferative agent (80% on MMF vs 20% on azathioprine in 2010). Trend is towards more use of MMF though azathioprine is being used in significant number of patients. Analysis of maintenance immunosuppression after renal transplant showed 60% patient maintained their original regimen over 7 years of follow up. Sirolimus was introduced in 1.5 to 7% patients during follow up period. Anti rejection treatment was required in 22-47% renal transplant recipients and trend towards decreasing rejection episode was seen. Steroids were used in the treatment of rejection in 90-100% patients. Use of ATG for treatment of rejection has increased from 11.5% in 2005 to 40% in 2010-11. By this study we conclude that immunosuppressant drugs have passed through significant changes during the year 2005 to 2011. Use of ATG as an induction agent and for treatment of rejection has increased. Similarly MMF and tacrolimus are most commonly used in maintenance regimen for renal transplant patients.

345-348

Authors: Praveen R.P.*, Ashalatha S Nair

Myxopyrum smilacifolium is a large woody climbing shrub belonging to the family Oleaceae which is known for many medicinal properties. In the present study, initially a short term cytotoxic study (3 hours) with hepatocarcinoma cell line HepG2 using Trypan Blue Assay was carried out against methanolic extracts of root and callus and found an appreciable result for both extracts. Then the study was extended to the same cell line employing MTT assay. In this procedure extracts were subjected to 24 hours treatment and cytotoxicity was measured using a colorimetric method based on the ability of metabolic active cells to cleave the yellow tetrazolium salt MTT to an insoluble purple formazan crystal. A concentration dependent activity was observed in both Trypan Blue as well as MTT assay. The results showed that both the extracts possess potent cytotoxic activity. IC50 value from MTT assay was found to be 63.75µg/l and 98.75µg/l for root and callus extracts respectively. To the best of our knowledge, this is the first study to demonstrate the cytotoxic potential of callus extracts of Myxopyrum smilacifolium Blume.

354-360

Authors: Samir Baniya1*, Dhananjaya D.R.1, Ankit Acharya2, Bishal Dangi1, Arjun Sapkota1

The present study was designed to evaluate the cardioprotective potential of Citrus grandis (L.) Osbeck (CGO) peel extract in rats. Citrus grandis (L.) Osbeck peel extract was evaluated for protection against cyclophosphamide (200 mg/kg body wt., i.p.) and doxorubicin (15 mg/kg body wt., i.p.) induced cardiotoxicity in male albino rats. Biomarkers like lactate dehydrogenase (LDH), alanine aminotransaminase (ALT), aspartate aminotransaminase (AST), alkaline phosphatase (ALP), total cholesterol (TC), triglyceride (TG) and creatinine kinase (CK-MB) along with heart weight index and antioxidant enzymes was considered to determine the cardioprotective property. Histopathological study was also carried out on heart of experimental animals. The CGO peel extract was found to contain alkaloids, flavonoids, steroids and triterpenoids, saponins, phenolic compounds and tannin as chemical constituents. Cyclophosphamide (CYP) and doxorubicin (DOX) treated groups exhibited significant increase in LDH, ALT, AST, ALP, TC, TG and CK-MB level and decrease in catalase (CAT), superoxide dimutase (SOD) when compared to control group. Pretreatment with different doses of CGO significantly reduced the serum biomarkers and increased the tissue antioxidant level when compared to DOX and CYP alone treated groups. Moreover, treatment with CGO also improved CYP induced changes in histopathology of heart which may be due to its antioxidant property. The Citrus grandis (L.) Osbeck exerted protective effect against CYP and DOX induced cardiotoxicity in rats, which may be due its lipid lowering and antioxidant properties. These findings might be helpful to understand the beneficial effects of CGO extract against myocardial injury although further study is needed to confirm its mechanism.

365-369

Authors: Parth U. Patel*, T. Y. Pasa, Khushbu A. Thakor, Ruchita J. Chauhan

A stability indicating RP-UPLC method was developed and validated for simultaneous estimation Ofloxacin and Ornidazole in tablet dosage form. The separation was achieved under optimized chromatographic condition on a Waters® C18 Acquity UPLC BEH (100 mm × 2.1 mm, 1.7μm) column with mobile phase consist of Water: Acetonitrile: Triethylamine in the ratio of 85: 15: 0.1 v/v. An isocratic elution at a flow rate of 0.2 ml/min at ambient oven temperature was carried out with PDA detection at 300 nm. The retention time for Ofloxacin and Ornidazole was 3.9 min and 6.4 min respectively. The degradation was observed under acidic, alkali, oxidative, photolytic and thermal conditions. The linearity was found to be in the concentration range of 50-150μg/ml for Ofloxacin and 125-375μg/ml for Ornidazole. The % recoveries at 50% were found to be 100.46% & 100.22% for Ofloxacin & Ornidazole respectively. The % recoveries at 100% were found to be 99.70% & 99.83% for Ofloxacin & Ornidazole respectively. The % recoveries at 150% were found to be 99.67% & 100.30% for Ofloxacin & Ornidazole respectively. The method was validated as per ICH guideline and the values were found to be within the limits. So, the proposed method was found to be simple, linear, accurate, precise, stability indicating, robust and specific.