Volume 3

April-June 2011

Review Articles

Prashant Singh, Dev Prakash, B Ramesh, Neha Singh, T Tamizh Mani

Microspheres are characteristically free flowing powders consisting of proteins or synthetic polymers which are biodegradable in nature and ideally having a particle size less than 200 μm. A well designed controlled drug delivery system can overcome some of the problems of conventional therapy and enhance the therapeutic efficacy of a given drug. There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion. One such approach is using microspheres as carriers for drugs. It is the reliable means to deliver the drug to the target site with specificity, if modified, and to maintain the desired concentration at the site of interest without untoward effects. This article aims to provide a comprehensive review of advantages, methods of preparation, mechanism, routs of administration, different types of microspheres based on natural and synthetic biodegradable polymers and application of biodegradable polymeric microspheres.

Keywords: Microspheres, Controlled Release, Polymers, Carriers, Target Site.

K Patidar, M D Kshirsagar, V Saini, P B Joshi, M Soni

Currently only 8% of new drug candidates have both high solubility and permeability. More than 60% of potential drug products suffer from poor water solubility. This frequently results in potentially important products not reaching the market or not achieving their full potential. Experience with solid dispersions over the last 20-30 years indicates that this is a very fruitful approach to improving the release rate and oral bioavailability of poorly water soluble drugs. So this article highlights technology various approaches for the preparation of solid dispersion, technology involved, detail description of poorly water soluble drugs & carriers.

Keywords: Solid Solution, Solid Dispersion, Dissolution, Carriers, Poor Water Soluble Drugs.

K Bhaskar Reddy, V Vaijayanthi, S Brito Raj, E Mohanambal, R Charulatha, Y Madhusudan Rao

Nanoparticles are solid colloidal particles ranging in size from 1 to 1000 nm that are utilized as drug delivery agents. The blood brain barrier represents an insurmountable obstacle for a large number of drugs including antibiotics, anti neoplastics and a variety of CNS active drugs especially neuropeptides. One of the possibilities to overcome this barrier is a drug delivery to brain using nanoparticles. The use of nanoparticles to deliver drugs to the brain across the blood brain barrier may provide a significant advantage to current strategies. The primary advantage of nanoparticles carrier technology is that nanoparticles mask the blood brain barrier limiting the characteristics of the therapeutics, drug molecules and it also decreasing peripheral toxicity by causing slow drug release in the brain. The nanoparticles may be especially helpful for the treatment of the disseminated and very aggressive brain tumors. The mechanism of nanopraticles mediated transport of drugs is mostly endocytosis by endothelial cells lining the brain blood capillaries. Physiological factors such as phagocytic activity of reticulo endothelial system and opsonization may limit the amount of brain delivered drug.

Keywords: Nanoparticles, Brain Targeting, Colloidal Particles, Neuropeptides, Endocytosis, Anti Neoplastics.

Research Articles

M Rajathi, D Modilal, Daisy P

Oral administration of aqueous extract of Elephantopus scaber leaves (300 mg/kg body weight) and roots (300 mg/kg body weight) for 84 days significantly reduced serum glucose, glycosylated hemoglobin and the activity of gluconeogenic enzyme glucose-6-phosphatase, but increased serum insulin, liver and skeletal muscle glycogen content and the activity of glycolytic enzyme glucokinase. The light microscopic studies of the pancreatic section of rats administered with the aqueous extract of of Elephantopus scaber leaves and roots showed an improvement in the histoarchitechture. For all the biochemical and histological studies performed, Elephantopus scaber roots treated rat showed a little better activity than Elephantopus scaber leaves treated diabetic rats. The present investigation suggests that Elephantopus scaber leaves and roots extract exhibit antihyperglycaemic effects and consequently may alleviate damage of pancreas and liver associated with alloxan-induced diabetes mellitus in rats.

Keywords: Alloxan, Diabetes Mellitus, Elephantopus Scaber, Glucose, Insulin, Light Microscopy.

Kuntal Das, Nilesh K Gupta, S Vijayabhaskar, Manjunath U M

The present investigation was evaluated the potential antimicrobial activity of patchouli oil (procured from fresh and dried patchouli leaf extracts, cultivated in Indian acidic soil zone). Extraction of patchouli oil was carried out by hydrodistillation method using Clevenger apparatus. The content of patchouli alcohol was estimated by Gas chromatography (GC) method. Microbiocides of patchouli oil was evaluated against several microorganisms viz. Bacillus substilis, Staphylococcus aureus, Streptococcus pyogenes, Enterobacter aerogenes, Pseudomonus aeruginosa, Escherichia coli, Klebsiella pneumoniae and Serratia marcescens by agar diffusion technique. The Minimum Inhibition Concentration (MIC) of the patchouli oil was appointed by the dilution method in the tube and the results revealed the concentration dependent (p<0.001) potential antimicrobial activity of both the oils by determined with zone of inhibition against standard ampicillin. At the dose of 300 mcg/ml patchouli oil gave maximum zone of inhibition against Staphylococcus (14.53±0.37**) followed by 12.15 ± 0.35** against Streptococcus from the second year of harvested. Such variation may be due to the effects of rich organic carbon content in acidic soil that increased the quality of oil content in patchouli leaves (collected from second year harvested fresh leaves). It proved patchouli is a strong potential antimicrobial plant. ><0.001) potential antimicrobial activity of both the oils by determined with zone of inhibition against standard ampicillin. At the dose of 300 mcg/ml patchouli oil gave maximum zone of inhibition against Staphylococcus (14.53±0.37**) followed by 12.15 ± 0.35** against Streptococcus from the second year of harvested. Such variation may be due to the effects of rich organic carbon content in acidic soil that increased the quality of oil content in patchouli leaves (collected from second year harvested fresh leaves). It proved patchouli is a strong potential antimicrobial plant.

Keywords: Antimicrobial Study, Acidic Soil, Agar Diffusion Technique, Hydrodistillation, Patchouli Oil, Patchouli Alcohol.

Fasalu Rahiman O M, Rupesh Kumar M, Tamizh Mani T, Mohamed Niyas K, Satya Kumar B, Phaneendra P, Surendra B

Aqueous extract of Asparagus racemosus root (AEAR) was evaluated for its hepatoprotective activities in rats. The plant extract (150 and 250 mg/kg, p.o.) showed a remarkable hepatoprotective and antioxidant activity against paracetamol-induced hepatotoxicity as judged from the wet liver weight, serum marker enzymes, antioxidant levels and histopathological studies on liver tissues. Paracetamol-induced a significant rise in wet liver weight, aspartate amino transferase (AST), alanine amino transferase (ALT), alkaline phosphatase (ALP), total bilirubin with a reduction of superoxide dismutase (SOD) and catalase. Treatment of rats with different doses of plant extracts (150 and 250 mg/kg) significantly altered serum marker enzymes and antioxidant levels to near normal against paracetamol-treated rats. The activity of the extracts was comparable to the standard drug, silymarin (100 mg/kg, p.o.). Histopathological changes of liver sample were compared with respective control. Results indicate the hepatoprotective properties of AEAR against paracetamol-induced hepatotoxicity in rats.

Keywords: Asparagus Racemosus Root, Hepatoprotection, Paracetamol, Serum Marker Enzymes, Biochemical Parameters, Histopathology.

Bafna Anand, Mishra Shrihari

Methanol extract (ME) of flowerheads Sphaeranthus indicus Linn. and its chromatographic methanol fraction (CMF) were screened for in-vitro antioxidant activity subjecting to DPPH free radical scavenging assay, superoxide scavenging assay, in-vitro lipid peroxidation and determination of reducing power. Both ME and CMF showed potent in-vitro antioxidant activity, whereas, CMF was more effective as free radical scavenger than ME. HPTLC fingerprint were undertaken for identification of active components. Flower-heads of Sphaeranthus indicus demonstrated in-vitro antioxidant activity in present study.

Keywords: Sphaeranthus indicus, DPPH, Superoxide, Lipid Peroxidation.

Masareddy R S, Bolmal U B, Patil B R, Shah V

Floating alginate based microsphere system of Metformin Hcl was prepared by ionotropic gelation technique, with sodium bicarbonate as gas forming agent, swellable polymers Hydroxy propyl Methylcellulose (HPMC E50), Ethyl cellulose (EC) and calcium chloride gelling agent. Alginate microspheres were formed as alginate undergoes ionotropic gelation by calcium ions and carbon dioxide develops from the reaction of bicarbonate salt with acid which permeated through alginate matrix leaving gas bubbles or pores within, providing the buoyancy. The concentration of polymer used was optimized by using 32 factorial designs. A 32 factorial design was used to elucidate the effect of variables, concentration of polymers HPMC (X1) and EC (X2) as the independent variables. The prepared microspheres were evaluated for size analysis, drug loading, drug entrapment efficiency, buoyancy study, SEM and in vitro drug release. The size of alginate microspheres was found to increase with increase in concentration of polymers. Drug loading and drug entrapment efficiency and was found to be in acceptable range. All formulations possessed good floating properties with total floating time more than 12 hrs. From the study, it was concluded that spherical and free flowing microspheres of Metformin Hcl could be successfully prepared by ionotropic gelation technique with high entrapment efficiency and prolonged release characteristics.

Keywords: Metformin Hydrochloride, Gastroretentive Drug Delivery System, Ionotropic Gelation, Floating Microspheres, Controlled Release.

Kullai Reddy Ulavapalli, J Sriramulu, Useni Reddy Mallu, Viswanath Reddy Pyreddy, Varaprasad Bobbarala

Single and reproducible RP-HPLC method has been developed for the simultaneous estimation of Levamisole, Mebendazole and Albendazole in pharmaceutical products. Chromatographic separation was achieved by using Inertsil ODS-3V C18, 250 x 4.6 mm, 5μm column, mobile phase composed of sol-A: Potassium dihydrogen phosphate (1.0 gram in 1000 ml of HPLC Water ) buffer and sol-B: Acetonitrile with gradient elution (0-5min- sol-A: 80-80; 5-7min- sol-A: 80-60; 7- 10min- sol-A: 60-30; 10-15min- sol-A: 30-80 and 15-20min- sol-A: 80-80). Flow rate was 1.00 ml per min and measured the absorbance at 210nm. The retention time of Levamisole, Mebendazole and Albendazole are 4.8min, 12.8min and 14.1min, respectively. The linearity of the method was evaluated from 5µg per mL to 100µg per mL for each ingredient and the correlation coefficient result was observed for each ingredient was not less than 0.999. The developed method has wide applicable in the quantification of Levamisole, Mebendazole and Albendazole in pharmaceutical dosage forms.

Keywords: Levamisole, Mebendazole, Albendazole, RP-HPLC Method.

Jafreen Jamal Joti, Md Ahsanul Haque, S M Ashraful Islam, Mohammad Safiqul Islam

Cilostazol is a synthetic antiplatelet and vasodilator agent. In the present study, a simple, sensitive and specific liquid chromatography (HPLC) method with UV detection was developed and validated for the quantification of cilostazol in human serum samples using diazepam as internal standard. The mobile phase consisted of water and acetronitrile (60:40%, V/V), pumped at a flow rate of 1.0 ml/min through the C-18 column at room temperature. Chromatographic separation was accompanied at 254 nm with a sensitivity of 0.0001. The developed method was selective and linear for cilostazol concentrations ranged in between 20 to 2000ng/ml for serum samples. The recovery of cilostazol ranged from 96.35 to 112.68%. The limit of quantitation (LOQ) of cilostazol was 20 ng/ml. The intraday accuracy ranged from 115.50% to 119.52%, the interday accuracy varied from 99.22 to 103.06%. For the LOQ, good values of precision (1.820 and 2.02% for intraday and interday, respectively) are also obtained. Acceptable results were obtained during stability study. This method proved to be simple, accurate and precise and can be used for pharmacokinetic and bioequivalence studies of cilostazol.

Keywords: Cilostazol, Method Validation, HPLC, Pharmacokinetic.

Short Communications

Hasanpasha N Sholapur, Fatima Sanjeri Dasankoppa

Accumulation of asiaticoside (an important bioactive compound) was determined in parent, first subcultured & second subcultured calluses obtained from leaf explants of Centella asiatica (L.) Urban. In first subcultured callus the accumulation of asiaticoside was 0.125 mg/g dry mass, using leaf explants in presence of napthelene acetic acid (NAA 1mg/l) and benzyl amino purine (BAP 2mg/l), was the highest among all the callus cultures studied, but this accumulation of asiaticoside was lower than that obtained from whole plant material (0.179 mg/g dry mass).

Keywords: Centella asiatica, Callus Culture, Subculture, Asiaticoside.

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