Baishakhi Dey

Chitosan microspheres in novel drug delivery systems.

The main aim in the drug therapy of any disease is to attain the desired therapeutic concentration of the drug in plasma or at the site of action and maintain it for the entire duration of treatment. A drug on being used in conventional dosage forms leads to unavoidable fluctuations in the drug concentration leading to under medication or overmedication and increased frequency of dose administration as well as poor patient compliance. To minimize drug degradation and loss, to prevent harmful side effects and to increase drug bioavailability various drug delivery and drug targeting systems are currently under development. Handling the treatment of severe disease conditions has necessitated the development of innovative ideas to modify drug delivery techniques. Drug targeting means delivery of the drug-loaded system to the site of interest. Drug carrier systems include polymers, micelles, microcapsules, liposomes and lipoproteins to name some. Different polymer carriers exert different effects on drug delivery. Synthetic polymers are usually non-biocompatible, non-biodegradable and expensive. Natural polymers such as chitin and chitosan are devoid of such problems. Chitosan comes from the deacetylation of chitin, a natural biopolymer originating from crustacean shells. Chitosan is a biocompatible, biodegradable, and nontoxic natural polymer with excellent film-forming ability. Being of cationic character, chitosan is able to react with polyanions giving rise to polyelectrolyte complexes. Hence chitosan has become a promising natural polymer for the preparation of microspheres/nanospheres and microcapsules. The techniques employed to microencapsulate with chitosan include ionotropic gelation, spray drying, emulsion phase separation, simple and complex coacervation. This review focuses on the preparation, characterization of chitosan microspheres and their role in novel drug delivery systems.

Mechanistic studies of lifestyle interventions in type 2 diabetes.

AIM To investigate the effect of lifestyle interventions in the non-pharmacological management of type 2 diabetes via a mechanistic approach. METHODS A randomized controlled trial was carried out on 60 type 2 diabetic male and female volunteers that fulfilled the inclusion criteria, with their proper consent and permission of the International Electrotechnical Commission for 1 year. 30 patients were included in the test group and 30 patients in the control group. Demographic details, anthropometrical status, physical activity, food habits and blood glucose lipid profile of the volunteers were recorded at baseline, the test group was directed for lifestyle intervention and final blood glucose lipid data were collected at the end of one year of patient follow-up. RESULTS After 1 year, the test group who had a lifestyle intervention was found to show a significant improvement in blood glucose lipid profile. The fasting plasma glucose level (FPG), postprandial plasma glucose level (PPG), glycosylated hemoglobin (HbA1c) and body mass index (BMI) values of the test group were reduced significantly, up to 145 ± 2.52, 174 ± 2.59, 6.3 ± 0.32 and 25 ± 0.41 respectively at the end of the study period, in comparison to the control group where FPG, PPG, HbA1c and BMI values were 193 ± 3.36, 249 ± 4.24, 7.2 ± 0.42 and 26 ± 0.65 respectively. Improvement in the total cholesterol (TC), triglyceride (TG), high-density lipoproteins (HDL) and low-density lipoproteins (LDL) values of the test group was also remarkable in comparison to the control group. The TC, TG, HDL and LDL values of the test group were reduced significantly, up to 149 ± 3.32, 124 ± 2.16, 58 ± 0.62 and 118 ± 2.31, respectively. CONCLUSION The significant improvement in the blood glucose lipid profile of the test group after 1 year signifies the value of non-pharmacological management of type 2 diabetes via lifestyle intervention strategies.

Chemo-profiling of eucalyptus and study of its hypoglycemic potential.

Constant escalations in the number of diabetics world-wide and the failure of conventional therapy to restore normoglycemia without adverse effects, in spite of tremendous strides in modern medicine, calls for naturopathy and alternative medicine. Because diabetes is multi-factorial and has secondary complications, prevention of hyperglycemia is the central dogma for its management. To date, no oral hypoglycemic exists which can achieve tight glycemic control without side effects. Dietary adjuncts, lifestyle interventions and a resurgence of interest in phyto-therapy have consequently gained ground. Natural hypoglycemics have attracted attention due to ease of incorporation in everyday diet, affordability, less adverse effects, and long term safety. Ethno botanical literature reports more than 800 anti-diabetic plants species. Eucalyptus is well represented in the Aboriginal Pharmacopoeias for its various pharmacological activities. Its hot aqueous decoction has been used as a hypoglycemic in various regions of world. This editorial attempts to summarize the data on the hypoglycemic potential of the different eucalyptus species, highlight the value of its natural biomolecules for the prophylaxis and treatment of type 2 diabetes, describe their mechanistic actions, shed light on the posology and safety aspects of eucalyptus and assess its applicability as a reinforcement to currently used therapy.

Comparative Evaluation of Hypoglycemic Potentials of Eucalyptus Spp. Leaf Extracts and their Encapsulations for Controlled Delivery

Eucalyptus is well represented in different Pharmacopeias for its variant pharmacology and depicts a wide range of photochemicals like triterpenoids, flavonoids, polyphenols, gallotannins and macrocarpals both in its volatile and nonvolatile fractions. Hot aqueous leaf decoctions of Eucalyptus have been recommended as ‘herbal tea’ in different regions of world for its hypoglycemic potentials. However lack of definitive dosage formulations of Eucalyptus bioactive, side effects like nausea, vomiting, gastric irritation, organoleptic unacceptability have limited its application; besides data on toxicology and posology being inconsistent and variant. In the current research work firstly comparative evaluations of hypoglycemic potentials amongst three Eucalyptus spp. E. globulus, E. citriodora, E. camaldulensis have been done by in vitro a-glucosidase assay

Exploration of natural enzyme inhibitors with hypoglycemic potentials amongst Eucalyptus Spp. by in vitro assays.

AIM To investigate the presence and potency of natural enzyme inhibitors with hypoglycemic potentials amongst Eucalyptus Spp. by in vitro assays. METHODS The leaf extracts of the three different Eucalyptus species [E. globulus (EG), E. citriodora (EC), E. camaldulensis (ECA)] were subjected to in vitro assay procedures to explore the prevalence of natural enzyme inhibitors (NEIs) after preliminary qualitative and quantitative phytochemical evaluations, to study their inhibitory actions against the enzymes like α-amylase, α-glucosidase, aldose reductase, angiotensin converting enzyme and dipeptidyl peptidase 4 playing pathogenic roles in type 2 diabetes. The antioxidant potential and total antioxidant capacity of the species were also evaluated. RESULTS Major bioactive compounds like polyphenols (341.75 ± 3.63 to 496.85 ± 3.98) and flavonoids (4.89 ± 0.01 to 7.15 ± 0.02) were found in appreciable quantity in three species. Based on the IC50 values of the extracts under investigation, in all assays the effectivity was in the order of EG > ECA > EC. The results of the ferric reducing antioxidant power assay showed that the reducing ability of the species was also in the order of EG > ECA > EC. A strong correlation (R(2) = 0.81-0.99) was found between the phenolic contents and the inhibitory potentials of the extracts against the targeted enzymes. CONCLUSION These results show immense hypoglycemic potentiality of the Eucalyptus Spp. and a remarkable source of NEIs for a future phytotherapeutic approach in Type 2 diabetes.

Therapeutic Interventions in Alzheimer Disease

Alzheimer disease (AD), was first recognized in the early 1900’s by Alois Alzheimer, a German psychiatrist and neuro pathologist and named after him (Fig.1). Auguste Deter, in 1902 is a reported patient of Dr. Alois (Fig.2). AD is the most common form of dementia affecting millions of the geriatric population worldwide, mostly those above 65-85 yrs of age. Women are more commonly affected than man [1]. Alzheimer currently afflicts about 5.2 million Americans and with the rapid escalation of the prevalence of the disease, the figure is expected to double by 2020. According to WHO, there are about 18 million people worldwide with AD, the figure will be projected to nearly double by 2025 to 34 million. Developing countries like India and China will be among the countries worst hit by AD due to ageing of the population and likely some genetic factors. In 2000, India had 3.5 million Alzheimer patients, however with the fast graying of population and growth rate being fastest in the 80+ segment of the society, the number of Alzheimer patients have been growing at a phenomenal rate [2]. This neurodegenerative fatal brain disorder generally begins in late life and disease progression is gradual and continuous, the longevity of a patient is about 8-10 yrs after symptoms appear. The disease conditions range from mild, moderate to severe; in mild conditions patients have some functional impairments, in moderate conditions there’s a dependence on care givers for some important daily activities, in severe conditions there is complete neuronal and memory loss, motor impairment making the patient absolutely dependent on care givers. Age related behavioral changes and symptoms of Alzheimer should not be confused.

An Experimental Design Approach for Impurity Profiling of Valacyclovir-Related Products by RP-HPLC

Abstract Impurity profiling has become an important phase of pharmaceutical research where both spectroscopic and chromatographic methods find applications. The analytical methodology needs to be very sensitive, specific, and precise which will separate and determine the impurity of interest at the 0.1% level. Current research reports a validated RP-HPLC method to detect and separate valacyclovir-related impurities (Imp-E and Imp-G) using the Box-Behnken design approach of response surface methodology. A gradient mobile phase (buffer: acetonitrile as mobile phase A and acetonitrile: methanol as mobile phase B) was used. Linearity was found in the concentration range of 50–150 μg/mL. The mean recovery of impurities was 99.9% and 103.2%, respectively. The %RSD for the peak areas of Imp-E and Imp-G were 0.9 and 0.1, respectively. No blank interferences at the retention times of the impurities suggest the specificity of the method. The LOD values were 0.0024 μg/mL for Imp-E and 0.04 μg/mL for Imp-G and the LOQ values were obtained as 0.0082 μg/mL and 0.136 μg/mL, respectively, for the impurities. The S/N ratios in both cases were within the specification limits. Proper peak shapes and satisfactory resolution with good retention times suggested the suitability of the method for impurity profiling of valacyclovir-related drug substances.

In vitro-in vivo studies of the quantitative effect of calcium, multivitamins and milk on single dose ciprofloxacin bioavailability

Ciprofloxacin, commonly used in India as an anti-microbial for prolonged use in chronic and non-specific indications, may affect the bioavailability of the drug. The drug prescribed is commonly taken with multivitamins, calcium and milk. A simple and reliable analytical methodology obtaining a correlation with in vivo urinary excretion studies using UV and HPLC and in vitro dissolution studies (IVIVC) has shown a significant increase in elimination rate of ciprofloxacin co-administered with multivitamins, calcium and milk. Appreciable IVIVC results proved that dissolution studies could serve as an alternative to in vivo bioavailability and also support bio-waivers.

Effects of Increased Protein Intake as a Variant of Rural Diet in Human Volunteers of Rural Bengal

Constant escalations in the number of diabetics’ worldwide, associated complications and financial implications, failure of conventional therapy regimen to restore normoglycemia has brought to limelight the non-pharmacologic means like lifestyle and dietary interventions as one of the effective aids to combat type 2 diabetes. Economy, education, preference plays a role in dietary selection. Prolonged intake of carbohydrate enriched diet was found to be a causative of diabetes amongst poor rural Indian population of Bengal. Contrastingly, current research of three years RCT amongst rural Bengalis have shown that a daily increase in protein intake by 25-30% when compared with standard rural diet comprising of about 70% to 80% of carbohydrate, 10% fats and 10% protein, improved insulin sensitivity and lowered fasting blood glucose level amongst experimental population significantly (p=0.04) rather than the control group. Fasting serum insulin value decreased from 47±2.2 pmol/l to 44±2.4 pmol/l (p=0.04) in the study group but amongst controls an increment from 42±2.4 pmol/l to 43±2.4 pmol/l was observed. Fasting Blood Sugar level amongst controls was initially 103±4 mg/dl and became 105±6 mg/dl but in the experimental group initial value of 109±12 mg/dl diminished to 103±8 mg/dl (p=0.04) at the end of 3 years follow up. However blood lipid parameters (TC, LDL, HDL, and VLDL) were not significantly influenced by higher daily protein intake both in control and experimental group. Thus a conclusive fact found from the trial is that protein enriched, low carbohydrate diet can offer a positive impact on glycemic control kidney functions remaining normal. (250 words)

DEVELOPMENT AND VALIDATION OF UV AND RP - HPLC METHODS FOR THE ESTIMATION OF CEFTRIAXONE SODIUM IN PHARMACEUTICAL FORMULATIONS

The current research paper reports a validated UV and RP - HPLC method fo r routine estimations of CFTX in bulk and unit dosage formulations. For the UV estimation of CFTX, using ammonium acetate buffer as the solvent, λ max was set at 241.5 nm and linearity range obtained in the concentration range of 2 - 10 µg/mL. The optimized R P - HPLC conditions for CFTX estimation were obtained with isocratic separation mode in a C 18 inertsil column (150 mm × 4.6 mm, 3 μm) using a degassed mixture of buffer: methanol in the ratio of 74:26, injection volume (20 µL), flow rate (1 mL/min) and ru n t ime (20 min utes ), at ambient column temperature with UV detector set at 254 nm. The linearity of the method was demonstrated over the concentration range of 80 - 120 µg/mL. The percent assay of CFTX determined by UV and RP - HPLC method were 99.8 ± 0.001 and 1 01.5 ± 0.001 respectively. The recovery CFTX deter mined by UV and RP - HPLC were 99 .6 - 99.8 % and 101.1 % respectively with % RSD values of peak areas 0.2 and 0.3 respectively. Values of all other parameters of method validations in both methodologies were wi thin the acceptance limits.