Mitigation of acrylamide by l-asparaginase from Bacillus subtilis KDPS1 and analysis of degradation products by HPLC and HPTLC

The use of bacterial l-asparaginase (LA) is one of the alternative approaches for acrylamide reduction in food stuffs as it catalyzes the conversion of l-asparagine to l-aspartic acid and ammonia. In present investigation, purification of extracellular LA from isolate of Bacillus subtilis sp. strain KDPS-1 was carried out by solid state fermentation process. The effects of solid substrates, initial moisture content, moistening agents, temperature, and incubation time on LA production was studied, and the highest asparaginase activity (47 IU/ml) was achieved in the medium having orange peel as substrate. The enzyme was purified to homogeneity by diethylaminoethyl (DEAE) cellulose ion exchange chromatography; with 84.89 % yield and 12.11 fold purity. LA showed stimulant activity against β-mercaptoethanol and was greatly inhibited by Zn(2+) and Hg(2+) metal ions. Reduction of acrylamide in fried potatoes was detected by high performance liquid chromatography, which showed clear degradation of acrylamide by height and area (%) in the chromatograms of standard sample to that of the test sample. Hydrolysates analysis by high performance thin layer chromatography confirmed the test sample to be LA

Toxicological Evaluation of Crude Alkaloid Fraction Isolated From Indian Folklore Plant Telosma Pallida (Roxb) wg Craib Root Using Probit Value Analysis

Present study first time reported the toxicological profile of Telosma pallida (TP) crude alkaloid fraction (CAF) isolated from the root of the climber plant by brine shrimp lethality test (BLT). Telosma pallida is a perennial herb found throughout the Junagadh district and surrounding. Previous studies showed the use of these alkaloids in the inhibition of thymidylate synthetase enzymes and cell growth. Brine shrimp toxicity study was carried out with Artemia salina Leach. In this assay, brine shrimp was hatched in sea salt water and allowed to contact with various concentrations of the crude alkaloid fractions. At 500μg/ml, highest mortality was found 74.44±0.35%whereas in the case of positive control, at the dose of 50μg/ml, 80.00±0.609% mortality was found. LD50 values for CAF and test control was found to be 89.12μg/ml and 12.59μg/ml, respectively. Further in-vitro and in-vivo studies may testify the anticancer potential of this plant

Development of the UV Spectrophotometric Method of Azithromycin in API and Stress Degradation Studies

ABSTRACT: Azithromycin (AZI) is a semi-synthetic macrolide antibiotic drug, effective against a wide variety of bacteria. The present study describes a simple, accurate, reproducible and precise UV Spectrophotometric method for the estimation of AZI (pH 6.8 Phosphate buffer). The absorbance maximum (λ max ) for AZI was found to be 208nm. The method reveals high sensitivity, with linearity in the 10 µg/ml to 50 µg/ml range. The lower limit of detection was found to be 1.6µg/ml and the limit of quantification was found to be 5µg/ml. All the calibration curves demonstrated a linear relationship between the absorbance and concentration, with the correlation coefficient higher than 0.99. The % recovery was found to be 99.72%. AZI was also subjected to stress degradation under different conditions recommended by the International Conference on Harmonization (ICH). Introduction

Antiurolithiatic activity of trans-cinnamic acid against ethylene glycol induced renal calculi in rats

Urolithiasis is a complex process characterized by supersaturation and retention of salts within the kidney and also a debilitating problem worldwide. Here, we have investigated antiurolithiatic effect of trans-cinnamic acid (t-CA) against ethylene glycol (EG) induced urolithiasis in rats. Urolithiasis was induced in Wistar albino rats using 0.75% v/v EG in drinking water for 28 days. t-CA was administered @200 and 400 mg/kg along with EG for 28 days. Biochemical, urine and histopathological analysis were performed to observe the calcium oxalate (CaC2O4) deposits and renal tissue damage. The EG group showed significant rise in urine oxalate, calcium, phosphate, and renal tissues oxalates, as compared to normal group. Serum creatinine and uric acid levels were also increased significantly in EG-treated group. Histopathological studies showed marked renal tissue damage and the presence of CaC2O4 crystals. Further, treatment of t-CA significantly ameliorated oxalate, calcium, magnesium, phosphate (urine) and creatinine, uric acid (serum) in EG-induced urolithiasis after 28 days. Moreover, t-CA-treated groups showed reversal of renal tissue damage and reduced level of CaC2O4. Interestingly, t-CA @400 mg/kg, was more effective in preventing the urolithiasis and regeneration of renal tissues in rats

(Formulation and Characterisation of Fluconazole loaded MCM-41 powder for Topical Drug Delivery)

Purpose: The use of common carriers like talc for topical drug delivery leads to diminished efficacy as a result of poor aqueous solubility and low dissolution rate. The objective of this study was to improve the efficiency of fluconazole topical dosage form using MCM-41 as a carrier material. The aim was to load fluconazole in carriers like MCM-41 as well as ß-Cyclodextrin and to compare the prepared powder formulation with the marketed formulations. Methods: Fluconazole complex was formulated with the use of MCM-41 and ß-CD as carriers in different proportions by melt, solvent evaporation and kneading method. The complex was developed into a powder formulation. These formulations were subjected to in vitro anti-fungal activity tests on candida albicans. Results: The inclusion compound was characterised by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and FTIR. The optimised method of preparation determined by in vitro dissolution was the melt method. The optimised formulation was then subjected to anti-fungal activity test. Formulation B containing MCM-41 as the bulk excipient had better performance than the marketed formulation; it showed 92.95±0.33% CDR compared to 74.96±0.47% CDR at the end of 1 hour and increased moisture adsorption. Conclusion: Thus, a fluconazole topical formulation with improved drug dissolution and moisture adsorption was designed. From in vitro tests, it was seen that the prepared formulation had better performance compared to the commercial formulation against skin mycotic infections and could be used for its treatment. result: The inclusion compound was characterised by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and FTIR. The optimised method of preparation determined by in-vitro dissolution was melt method. The optimised formulation wast hen subjected to anti fungal activity test. Formulation B containing MCM-41 as the bulk excipient had better performance than the marketed formulation; it showed 92.95±0.33 other: na </jats:sec

Self nano-emulsifying drug delivery system for Embelin: Design, characterization and in-vitro studies

AbstractCThe objective of the present study was to prepare solid self-nanoemulsifying drug delivery system (S-SNEDDS) containing Capryol-90 as oil phase for the delivery of Embelin, a poorly water soluble herbal active ingredient. Box-Behnken experimental design was employed to optimise the formulation variables, X1 (amount of oil; Capryol 90), X2 (amount of surfactant; Acrysol EL 135) and X3 (amount of co-surfactant; PEG 400). Systems were appraised for visual characteristics for self emulsifying time, globule size and drug release. Optimised liquid formulations were formulated into free flowing granules (S-SNEDDS) by adsorption on the porous materials like Aerosil 200 and Neusilin and thereby compressed into tablet. In vitro dissolution studies of SNEDDS revealed increased in the dissolution rate of the drug. FT-IR data revealed no physicochemical interaction between drug and excipients. Solid state characterization of S-SNEDDS by DSC and Powder XRD confirmed reduction in drug crystallinity which further supports the results of dissolution studies. TEM analysis exhibited spherical globules. Further, the accelerated stability studies for 6 months revealed that S-SNEDDS of Embelin are found to be stable without any significant change in physicochemical properties. Thus, the present studies demonstrated dissolution enhancement potential of porous carrier based S-SNEDDS for poorly water soluble herbal active ingredient, Embelin