Development of Anti-diabetic Niosomes Formulation Containing Metformin and Gliclazide

Metformin/Gliclazide niosomes were formulated with span 60 by ether injection method. Three batches MG1-MG3 were prepared in order to study influence of drug polymer ratio on the niosomes formation and in vitro drug release. The formulated niosomes were characterized by drug entrapment, vesicle size determination, and in vitro drug release. Optimized concentration of span 60 and cholesterol was found to be 1:1. In the in-vitro study, niosomes formulation of MG1 showed high percentage of drug release, 40.18 to 45.75% for about 8 hrs. This indicated that this batch of niosomes formulation exhibit sustained drug release pattern as the niosomes act as reservoir system for continuous delivery of drug. The quantity of Metformin/Gliclazide present in the niosomes and the release medium were estimated by a validated HPLC method. The formulated niosomes had acceptable physicochemical characters and released the drug over 6-8 h. The data obtained from in vitro release studies were fitted with various kinetic models and was found to follow Higuchi kinetics

Synthesis and antimicrobial activity of some newer semicarbazone analogues

On the basis of literature review Semicarbazones have been potent in activities such as antifungal, antibacterial, antituberculosis, anticancerous etc. Till date various works has been done however still there is tremendous opportunities which can be explored. So, we planned for the synthesis of Semicarbazone derivaties and checking their antimicrobial activities. Biological activity was determined for all 19 synthesized compounds against bacteria (gram positive and gram negative) by MIC(Minimum Inhibitory Concentration) method

Synthesis, Characterization and Pharmacological evaluation of some newer Benzothiazole derivatives

The objective of the present work is to develop safer new chemical entities that show good anticonvulsant effects and antimicrobial actions. The current work describes the synthesis of Benzothiazole derivatives with encouraging anticonvulsant activity against MES and scPTZ tests with interesting pattern of antimicrobial effects. The synthesized Benzothiazole derivatives could be considered as lead molecule for the development of therapeutic agents. Many polycyclic and fused ring systems containing the thiazolenucleus(I) are well known. The most important is bicyclic system wherein the second ring benzene is fused to the 4,5 position of thiazole ring i.e. Benzothiazole.(II

Formulation and Evaluation of Mesalamine Nanosphere Tablet

Nanospheres are the particles having the size range between 10-200 nm in diameter. Nanospheres can be amorphous or crystalline in nature and also they have the ability to protect the drug from enzymatic and chemical degradation. For the preparation of standard calibration curve of Mesalamine with Phosphate buffer pH 6.8 and Absorbance of µg/ml solution was measured between 200-400nm by using Shimadzu 1601 UV/Vis double beam spectrophotometer. Nanosphare containing Mesalamine were prepared using nanoprecipitation method. 200 mg of polymer (Eudragit RS and L) was dissolve in 50 ml water. Drug was dissolve in 20 ml of methanol. Both solution were mixed and add 50 ml of water and stirred for half an hour. Methanol and water was evaporated under reduced pressure using rotary flash evaporator until 10 ml of solution was remaining. Than this suspension was centrifuge at 15000 rpm at 40C for half an hour. The supernatant was discarded and remaining portion was washed with distilled water. The nano-sphares was dried over night at 600C and stored in desiccators. The surface morphology (roundness, smoothness, and formation of aggregates) and particle size was studied by scanning electron microscopy (SEM). Zeta potential of the best formulation (F4) was determined by zeta potential probe model DT- 300. Mesalamimne, Dextrose and Lactose were taken in required quantities mixed and granulating agent (Starch past) was added and passed through #40 sieves, then lubricant magnesium stearate and talc was added then compressed into tablets by rotary tablet punching machine. Then film coating is done by 6% w/v solution of Cellulose acetate Phthalate in isopropyl alcohol using 2% tween-80 as plasticizer in coating pan. The weight of tablet was kept constant for all formulations. Nanosphare tablet formulation F-2 Showed maximum drug (97.75%) released and formulation F-4 showed 92.58% drug release. The In-vitro drug released study result showed that formulation F-2 96.58% drug was released after 17 hours which is highest drug release amongst all other tablet formulation. &nbsp

Formulation and In-Vitro Evaluation of Niosomal drug Delivery in Cancer Chemotherapy

Drug delivery systems are defined as formulations aim for transportation of a drug to the desired area of action within the body. The aim of the study was to investigate the feasibility of using Niosomes as a drug delivery system for Cisplatin By entrapment of drug in Niosomes, dose also could be reduced. Niosomes were prepared by Ethanol injection method using cholesterol and Surfactant. Particle size, zeta potential, entrapment efficiency and in vitro drug release studies were performed. The targeted niosome delivery system is composed of drug, surfactant and cholesterol. With regard to the influence of formulation variables on the percent drug loading (PDL), different compositions with varying ratios of surfactant and cholesterol were studied. In –Vitro drug release mechanism was studied for 24 hours

Formulation and Evaluation of Floating Tablets of Sitagliptin with Extract of Triphala

The aim of the present work is to formulate, optimize and evaluate hydrodynamically balanced antidiabetic system incorporated with sitagliptin and phytochemical constituents of Triphala extract for the treatment of constipation associated with diabetes.  The Triphala churna of two different ratios, 1:1:1 (TC1) and 1:2:4 (TC2) were subjected to hot percolation using Soxhlet apparatus using methanol as solvent. The floating matrix tablets of Sitagliptin with methanolic Triphala extract was prepared by wet granulation technique using HPMC K4M as polymer, starch/honey as binder and sodium bicarbonate & citric acid as effervescent agents by 24 factorial design.  The compatibility studies showed that there is no chemical interaction between the drug, polymer and the excipients used in the tablets.  The independent variables are drug & Triphala extract ratio (X1), Triphala proportion (X2), binder used for granulation (X3), and amount of effervescent excipients used (X4).  The dependent variables are hardness (Y1), buoyancy lag time (Y2), total floating time (Y3), in-vitro drug release (Y4), and T50% (Y5).  The prepared floating tablets were subjected to all post compression parameters such as hardness, friability, swelling capacity, buoyancy, total floating time, drug content & in-vitro drug release and were found to be within normal limits.  Based on drug content, buoyancy lag time and in-vitro drug release the formulations F14 and F16 were selected for in-vivo study of the formulation.  Keywords:  Triphala, Sitagliptin, honey, floating tablet.&nbsp

ACUTE TOXICITY AND IN-VIVO LAXATIVE STUDIES OF THE TRIPHALA EXTRACT IN EXPERIMENTAL ANIMALS

Triphala has been extensively used in traditional medicine for laxative, antidiabetic, expectorant, astringent, anti-aging etc.  The acute toxicity of methanolic extracts of Triphala in 300 mg, 600 mg, and 1000 mg/kg has not yet been studied.  The current studies were done by employing Swiss Albino mice as experimental animal. The methanolic extracts of Triphala were considered safe up to a dose of 1000 mg/kg when evaluated for acute oral toxicity in accordance with the OECD (Organization for Economic Cooperation and Development) guidelines. The results of acute toxicity showed no signs of toxicity such as general behaviour changes, mortality, changes on gross appearance or histopathological changes of the internal organs of rats. The examinations of signs of acute toxicity showed no abnormalities in the test groups as compared to the controls. Haematological and blood chemical values in treated groups were normal in comparison with the control group.  Therefore, the extract of Triphala given orally to mice did not produce acute toxicities.  The laxative activity on Albino Wistar rats shows that the Triphala extract has significant positive effect on constipated animals. &nbsp

Relaxin, a pleiotropic vasodilator for the treatment of heart failure

Relaxin is a naturally occurring peptide hormone that plays a central role in the hemodynamic and renovascular adaptive changes that occur during pregnancy. Triggering similar changes could potentially be beneficial in the treatment of patients with heart failure. The effects of relaxin include the production of nitric oxide, inhibition of endothelin, inhibition of angiotensin II, production of VEGF, and production of matrix metalloproteinases. These effects lead to systemic and renal vasodilation, increased arterial compliance, and other vascular changes. The recognition of this has led to the study of relaxin for the treatment of heart failure. An initial pilot study has shown favorable hemodynamic effects in patients with heart failure, including reduction in ventricular filling pressures and increased cardiac output. The ongoing RELAX-AHF clinical program is designed to evaluate the effects of relaxin on the symptoms and outcomes in a large group of patients admitted to hospital for acute heart failure. This review will summarize both the biology of relaxin and the data supporting its potential efficacy in human heart failure

Effect of Smoking on Circulating Angiogenic Factors in High Risk Pregnancies

Objective: Changes in maternal concentrations of the anti-angiogenic factors, soluble fms-like tyrosine kinase 1 (sFlt1) and soluble endoglin (sEng), and the pro-angiogenic placental growth factor (PlGF) precede the development of preeclampsia in healthy women. The risk of preeclampsia is reduced in women who smoke during pregnancy. The objective of this study was to investigate whether smoking affects concentrations of angiogenic factors (sFlt1, PlGF, and sEng) in women at high risk for developing preeclampsia. Study Design: We performed a secondary analysis of serum samples from 993 high-risk women (chronic hypertension, diabetes, multifetal gestation, and previous preeclampsia) in a preeclampsia prevention trial. sFlt1, sEng and PlGF were measured in serum samples obtained at study entry, which was prior to initiation of aspirin (median 19.0 weeks' [interquartile range of 16.0-22.6 weeks']). Smoking status was determined by self-report. Results: sFlt1 was not significantly different in smokers from any high-risk groups compared to their nonsmoking counterparts. PlGF was higher among smokers compared to nonsmokers among diabetic women (142.7 [77.4-337.3] vs 95.9 [48.5-180.7] pg/ml, p = 0.005) and women with a history of preeclampsia (252.2 [137.1-486.0] vs 152.2 [73.6-253.7] pg/ml, p = 0.001). sEng was lower in smokers with multifetal gestations (5.8 [4.6-6.5] vs 6.8 [5.5-8.7] ng/ml, p = 0.002) and trended lower among smokers with diabetes (4.9 [3.8-5.6] vs 5.3 [4.3-6.3] ng/ml, p = 0.05). Smoking was not associated with a lower incidence of preeclampsia in any of these groups. Conclusions: In certain high-risk groups, smoking is associated with changes in the concentrations of these factors towards a pro-angiogenic direction during early pregnancy; however, there was no apparent association between smoking and the development of preeclampsia in our cohort

Soluble fms-Like Tyrosine Kinase 1 (sFlt1), Endoglin and Placental Growth Factor (PlGF) in Preeclampsia among High Risk Pregnancies

Background: Differences in circulating concentrations of antiangiogenic factors sFlt1 and soluble endoglin (sEng) and the pro-angiogenic growth factor PlGF are reported to precede the onset of preeclampsia weeks to months in low-risk pregnant women. The objective of this study was to investigate whether similar changes can be detected in pregnant women at high-risk to develop the syndrome. Methods: This study is a secondary analysis of the NICHD MFMU trial of aspirin to prevent preeclampsia in high-risk pregnancies. Serum samples were available from 194 women with pre-existing diabetes, 313 with chronic hypertension, 234 with multifetal gestation, and 252 with a history of preeclampsia in a previous pregnancy. Samples collected across pregnancy were analyzed in a blinded fashion for sFlt1, sEng and PlGF. Results: The odds of developing preeclampsia were significantly increased among women with multiple fetuses for each 2- fold elevation in sFlt1, sEng and the ratio of angiogenic factors (e.g. OR 2.18, 95% CI 1.46-3.32), and significantly decreased for each 2-fold elevation in circulating PlGF (OR 0.50, 95% CI 0.30-0.82) between 7 and 26 weeks' gestation. Cross-sectional analysis of the angiogenic factors across gestation showed significant differences during the third trimester in women who develop preeclampsia compared with appropriate controls in all high-risk groups. However, when data were examined in relation to the gestational week when preeclampsia was diagnosed only sFlt1 was significantly higher 2 to 5 weeks before the clinical onset of preeclampsia and only in women with previous preeclampsia. Conclusions: The pattern of elevated concentrations of sFlt1 and sEng, and low PlGF in high-risk pregnant subjects who develop preeclampsia is similar to that reported in low-risk pregnant women. However, differences in these factors among high-risk women who do and do not develop preeclampsia are modest, and do not appear to be clinically useful predictors in these high-risk pregnant women