A NANOSCALE DENDRITIC MACROMOLECULES BASED ON ETHANE 1,2-DIAMINE AS POTENTIAL DRUG CARRIERS FOR NSAIDS: SYNTHESIS, CHARACTERIZATION AND APPLICATIONS

Objective: The present work deals with the objective of development and characterization of novel dendritic macromolecules as solubility enhancer and carrier for sustained release of Ketoprofen. Cytotoxicity and hemolytic assay of dendritic macromolecules were also estimated as an objective to evaluate its toxicity and biocompatibility. Methods: Dendritic macromolecules were synthesized using divergent method. Synthesized macromolecules were characterized by spectral techniques such as FTIR, 1H-NMR, 13C-NMR electro-spray ionization mass spectrometry and elemental analysis. Enhanced aqueous solubility of ketoprofen was evaluated with respect to pH, generation number and concentration of dendrimer using Higuchi and Connors method. Sustained release of ketoprofen from ketoprofen loaded dendrimers was measured and compared with that of free ketoprofen. Hemolytic assay and cytotoxicity of G3 dendrimer on A-549 cell lines were studied to evaluate toxicity and biocompatibility of dendrimer. All dendritic macromolecules were fully characterized by spectral techniques. Results: Solubility study revealed that aqueous solubility of ketoprofen by dendrimer increased with increase in pH, concentration and generation of dendrimer. Ketoprofen was released slowly from ketoprofen loaded dendrimer compared to that of free ketoprofen. Dendritic macromolecules were less cytotoxic and showed less hemolytic potential. Conclusion: It can be concluded that dendrimer have high potential as carriers and solubility enhancers of hydrophobic drug. Keywords: Triazine based dendrimer, Ketoprofen, Drug Carrier, Cytotoxicity, Hemolysis

NOVEL HYDROXYL TERMINATED DENDRIMERS AS POTENTIAL DRUG CARRIERS: SUSTAINED RELEASE, HEMOLYSIS AND CYTOTOXICITY STUDY

Objective: Potential of novel hydroxyl terminated dendrimer generations G1(OH)8, G2(OH)32 and G3(OH)128 as solubility enhancers of model drug ketoprofen was evaluated. G3(OH)128 dendrimer was further explored as the novel carrier for sustained release of ketoprofen. Cytotoxicity and hemolytic potential of G3(OH)128 dendrimer were studied to evaluate toxicity of dendrimer. Methods: Higuchi and Connors method was employed to evaluate improved solubility of ketoprofen at different pH and dendrimer generation. Ketoprofen was loaded into G3(OH)128 dendrimer by inclusion complex method. Ketoprofen loaded dendrimer was characterized by Flourier Transform infrared spectroscopy. Sustained release of ketoprofen from ketoprofen loaded dendrimers was studied and compared to that of free ketoprofen. Cytotoxicity of dendrimers on A-549 cell lines were studied by MTT assay technique. Hemolytic potential of G3 dendrimer was also studied. Results: Solubility of practically insoluble ketoprofen was improved up to 0.77-4.89 mg/ml by dendrimer generations. Solubility of ketoprofen was increased with increase in pH, concentrationand generation number of dendrimer. Ketoprofen was released relatively slowly from ketoprofen loaded dendrimer compared to free ketoprofen. Cytotoxicity and hemolytic assay revealed that dendrimers were less toxic compared to PAMAM dendrimers. Conclusion: Improved solubility of ketoprofen by dendrimer generations, its slow release from G3(OH)128 dendrimer and cytotoxicity and hemolytic assay showed dendrimers have potential as drug carriers. Keywords: Triazine Based Dendrimer, Sustained Release, Cytotoxicity, Hemolysis, Ketoprofen, Encapsulation

Method Development and Validation for Simultaneous Estimation of Benidipine Hydrochloride and Metoprolol Succinate in Tablet

Present work focusing in developing and validating a new high performance liquid chromatography method for estimation of Metoprolol Succinate and Benidipine Hydrochloride in their combine tablet dosage form. The method was performed on Shimadzu LC-20AT instrument using C18 (250 mm x 4.6 mm, 5 µm) Hypersil BDS Column and Potassium Dihydrogen Phosphate Buffer (pH 4.0): Methanol (65: 35% v/v) as mobile phase at ambient temperature. Detection was carried out at 269 nm. Concentration range 4-12 µg/ml for Benidipine Hydrochloride and 25-75 µg/ml for Metoprolol Succinate . The Percentage recovery of Benidipine Hydrochloride and Metoprrolol succinate was found to be 99.59% and 99.39 respectively. Correlation coefficient for Metoprolol succinate and Benidipine Hydrochloride was found 0.9995 and 0.9997 respectively. The Rt values for Metoprolol succinate and Benidipine Hydrochloride were found to be 3.4 and 5.9 min respectively. The method was validated according to the guidelines of International Conference on Harmonisation (ICH) and was successfully employed in the estimation of commercial formulations. Keywords:  Metoprolol Succinate, Benidipine Hydrochoride, HPLC, Mobile Phase

Sonochemistry: Non-Classical Way of Synthesis

This review presents the detailed picture of current knowledge on ultrasound assisted chemical reactions and its green approach in chemical synthesis. This article illustrates the theoretical background and details about ultrasound, its mechanism (cavitation, the driving force) in chemical synthesis, types of reactions with different systems and its utility. All the reported applications have shown that Sonochemistry, ultrasound assisted chemical reaction is a green and economical viable approach for drug, impurity or chemical intermediate synthesis. Keywords: Cavitation, Sonocatalysis, Sonochemistry Ultrasoun

Anterior tibial spine (ACL avulsion) fracture treated with open reduction and fixation with screw: surgical technique, functional and clinico-radiological outcomes

Background: The anterior tibial spine fracture occurs almost at a same frequency both in adolescents and in adults. These injuries are often overlooked at emergency room. Stable internal fixation requires to gain optimum function of ACL by securing its length and nascent tension. We treated anterior tibial spine (ACL avulsion) fracture patient with open reduction and screw fixation.Methods: Study of Ten patients of anterior tibial spine (ACL avulsion) fracture, with minimum of 06 months and maximum of 18 months follow up. Classification of anterior tibial spine (ACL avulsion) a fracture done by Meyer and Mckeever. All patients operated with open reduction and internal fixation with screw via medial parapatellar approach. Functional and clinical outcome measured with Lysholm knee score at final follow up.Results: We studied 10 patients with anterior tibial spine (ACL avulsion) fractrure where mean age of patient was 36.4 years. Mean radiological healing was 10.6 weeks in anterior tibial spine (ACL avulsion) fracture. We observed mean motion of knee 133 degree in anterior tibial spine (ACL avulsion) fracture. Mean Lysholm score at final follow up was 86.8.Conclusions: Open reduction for anterior tibial spine (ACL) fracture provides direct visualization with easy application of screws ultimately confers stable osteosynthesis enables to start early range of motion and further rehabilitation protocol. Open reduction internal fixation is comparative less technically demanding, less expansive and gives excellent to good results as compared to other techniques.

Successful Ayurvedic management of Hepatic Cirrhosis Complex with Ascites - A Case Study

Hepatic cirrhosis of liver is an inflammatory condition of the liver caused by various factors specially excessive alcohol consumption over an extended period of time. When alcohol gets processed in the liver, it produces highly toxic chemicals. These chemicals can fatally injure the liver cells. Normally the treatment is too much time consuming, difficult and inadequate Ayurvedic treatment serves as a promising different modality. In present study the case of alcoholic cirrhosis complicated with Ascites is presented. The patient was given Ayurvedic treatment with Vardhamana Pippali, Katuki Churna, Punarnavadi Kvatha, Bhrungaraja Panchanga Churna, Arogyavardhini Rasa, Mixture of Bhumyamalaki Panchanga Churna, Sharpunkha Mula Churna and Sveta Parpati. This treatment approach has improved condition of patient greatly by bringing hepatitis from Child-Pugh stage C to stage B with improvement in sign and symptoms as well as in ascetic condition

Evaluation of the Effect of Hydroalcoholic Extracts of Cassia Occidentalis Leaves in Neutrophil Adhesion Test in Rats

Evaluation of the effect of hydroalcoholic extracts of Cassia occidentalis leaves in neutrophil adhesion test in Rats. The effect of oral administration of hydroalcoholic extract of Cassia occidentalis leaves on neutrophil has been studied and is compared with control group on rats. The differential leukocyte count (DLC) was performed by fixing the blood smears and staining with leucofine and percent neutrophils in each sample was determined. After the initial counts, blood samples were incubated with 80 mg/ml of nylon fibers for 10 min at 37ºC. Supplementation with hydroalcoholic extract of Cassia occidentalis leaves significantly decreased neutrophil adhesion. The results indicate that the leaf of Cassia occidentalis is endowed with protected neutrophil adhesion. These effects could conclude that Cassia occidentalis has an antiasthmatic property. Keywords: Cassia occidentalis, Neutrophil adhesion, analysis of varianc

Thyroid cancer and nonsteroidal anti-inflammatory drug use: a pooled analysis of patients older than 40 years of age

Background: Cyclooxygenase (COX-2) has been associated with tumor growth and metastasis in several cancers, including thyroid cancer. For this reason, several investigators have studied COX-2 inhibitors in preclinical models of thyroid cancer and found antineoplastic effects. Thus, the primary aim of this study was to assess if the use of nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with a reduced incidence of thyroid cancer. A second aim of the study was to determine additional risk or protective factors for thyroid cancer. Methods: Three large prospective population-based studies (the NIH-AARP Diet and Health Study; the Prostate, Lung, Colorectal and Ovarian Cancer Screening Trial; and the U.S. Radiologic Technologists Study) were pooled to investigate the association between self-reported frequency of aspirin and nonaspirin NSAID use one year prior to baseline (no use, ≤2/week, >2–6/week, and ≥7/week) and subsequent risk of thyroid cancer. A Cox regression proportional hazard model was used to estimate aggregated hazard ratios (HR) adjusted for cohort, sex, race/ethnicity, weight, smoking status, and alcohol intake. Results: There were 388,577 participants in the pooled cohort, with 481 cases of thyroid cancer. No significant risk reduction was observed with regular use of nonaspirin NSAIDs (HR = 1.14 [confidence interval (CI) 0.84–1.55]), and/or regular use of aspirin (HR = 1.06 [CI 0.82–1.39]). The multivariate regression analysis confirmed as previously reported in the literature that female sex, obesity class I (body mass index [BMI] = 30–34.99 kg/m(2)), and obesity class II (BMI = 35–35.99 kg/m(2)) were independently associated with an increased thyroid cancer risk. Current smoking status and moderate and excessive alcohol use were also confirmed as independent risk factors associated with a reduced thyroid cancer risk. Conclusions: Neither nonaspirin NSAIDs nor aspirin use is associated with a reduced risk of thyroid cancer. Women and obesity are associated with an increased risk of thyroid cancer, whereas smoking and alcohol use are associated with decreased risk of thyroid cancer