In vivo immunomodulatory, cumulative skin irritation, sensitization and effect of d-limonene on permeation of 6-mercaptopurine through transdermal drug delivery.

Using skin as a port for systemic drug administration, transdermal drug delivery has expanded greatly over the last two decades. Our aim was to formulate the single layer drug-in-adhesive transdermal patch for 6-mercaptopurine (6-MP). In vitro permeation study was carried out using modified Franz diffusion cell with and without of different concentration of d-limonene in human cadaver skin.

Transdermal delivery of 5-fluorouracil for induced ehrlich ascites carcinoma tumor in BALB/c mice and pharmacokinetic study.

The purpose of this study was to determine the permeation of the hydrophilic compound 5-fluorouracil through human epidermal membranes, Ehrlich Ascites Carcinoma (EAC) cells were used as a model cell line to evaluate the cytotoxic concentration and anti-tumor activity of 5-fluorouracil (5-FU) through transdermal drug delivery for tumors. Cytotoxicity was assessed by exposing cell suspension to increased concentration of drug from 20-100 microg/ml and measuring the viable cell count by tryphan blue exclusion method. Results confirmed that 100 microg/ml of 5-FU was cytotoxic.

Development of extended zero-order release gliclazide tablets by central composite design.

The purpose of this study was to develop an extended release tablet formulation containing gliclazide as a model drug by optimization technique. A central composite design was employed with pH-dependent matrix forming polymers like keltone-HVCR (X1) and eudragit-EPO (X2) as independent variables. Five dependent variables were considered: hardness, percent drug release after 1 hr, percent drug release after 6 hr, diffusion exponent and time required for 50% of drug release.

Effect of thiazolidinediones on the erythropoeitic and germinal cells in the male wistar rats.

Hyperglycemia is the main determinant of long term diabetic complications mainly through induction of oxidative stress responsible for secondary defects including cancer, infertility etc. Thiazolidinediones (TZDs) are known to posses the antioxidant potential against the reactive oxygen species. The ability of clinically used TZDs like Rosiglitazone (RSG) and Pioglitazone (PIO) in diabetic complications is still need to be studied extensively in the literature.

Physicochemical and pharmacokinetic parameters in drug selection and loading for transdermal drug delivery.

Skin of an average adult body covers a surface of approximately 2 m2 and receives about one-third of the blood circulating through the body. The transdermal route of administration cannot be employed for a large number of drugs. The rationality of drug selection based on pharmacokinetic parameters and physicochemical properties of the drug are the important factors to be considered for deciding its suitability of drug for delivery by transdermal route.

Microwave-induced synthesis of schiff bases of aminothiazolyl bromocoumarins as antibacterials.

A fast and highly efficient method for the synthesis of some of the schiff bases of aminothiazolylbromocoumarin (4a-m) has been performed by microwave irradiation of 2'-amino-4'-(6-bromo-3-coumarinyl) thiazole (3) and substituted aromatic aldehydes (a-m). Microwave assisted reactions have resulted in better yields of the desired products than when prepared under conventional conditions. The resulting products were evaluated for their qualitative and quantitative antibacterial activity.

Liposomal formulations of serratiopeptidase: in vitro studies using PAMPA and Caco-2 models.

The feasibility of using liposomes as a potential oral delivery system for the systemic delivery of other peptides and protein-based pharmaceuticals has been studied. Serratiopeptidase, a proteolytic enzyme, was used as a model drug. Liposomes were prepared by a thin film hydration method using various lipids, namely, soya lecithin, DMPC and DMPE.

Microprocessor-controlled iontophoretic drug delivery of 5-fluorouracil: pharmacodynamic and pharmacokinetic study.

Purpose: The purpose of this study was to fabricate monolithic 5-fluorouracil (5-FU) transdermal patch with microprocessor- controlled iontophoretic delivery, to evaluate the pharmacodynamic effects on Dalton's lymphoma ascites (DLA) induced in Balb/c mice, and to study pharmacokinetics in rabbits.

Materials And Methods: The transdermal patches were prepared by solvent casting method; a reprogrammable microprocessor was developed and connected to the patches. DLA cells were injected to the hind limb of Balb/c mice (10 animals/group).

Comparative interaction of few antihypertensive drugs with cyclosporine-A in rats.

The maximal endothelial dependent relaxation of isolated aortic rings to cumulative doses of acetylcholine was significantly decreased in the Cyclosporine-A (CSA, 20 mg kg(-1) day(-1)) treated animals compared to olive oil (CSA vehicle) treated control. Administration of antihypertensive drugs like diltiazem, enalapril or propranolol to CSA treated animals augmented the endothelial damage induced by CSA. These drugs also increased the bioavailability of CSA.

Formulation and evaluation of ketorolac tromethamine-loaded albumin microspheres for potential intramuscular administration.

The objective of this work was to prepare and evaluate ketorolac tromethamine-loaded albumin microspheres using a factorial design. Albumin microspheres were prepared by emulsion cross-linking method. Selected formulations were characterized for their entrapment efficiency, particle size, surface morphology, and release behavior.

Intrastrain variations in anxiolytic effect of nitrazepam in mice.

This study investigated the individual differences in the baseline anxiety and anxiolytic effect of nitrazepam in Balb/c mice. Initially mice were sorted according into low, intermediate and high anxiety groups (LA, IA and HA) based on the number of entries to and time spent in open arms in elevated plus maze. Later, anxiolytic effect of nitrazepam (2 mg/kg, p.

Screening of selected Indian medicinal plants for acetylcholinesterase inhibitory activity.

Seventy-six plant extracts including methanolic and successive water extracts from 37 Indian medicinal plants were investigated for acetylcholinesterase (AChE) inhibitory activity (in vitro). Results indicated that methanolic extracts to be more active than water extracts. The potent AChE inhibiting methanolic plant extracts included Withania somnifera (root), Semecarpus anacardium (stem bark), Embelia ribes (Root), Tinospora cordifolia (stem), Ficus religiosa (stem bark) and Nardostachys jatamansi (rhizome).

Citral, a component of lemongrass oil inhibits the clastogenic effect of nickel chloride in mouse micronucleus test system.

Citral is a major component of Cymbopogon citratus (lemongrass oil). The aqueous suspension of citral (60 mg/kg body weight, per oral) treated for one week was tested for the anti-clastogenic effect using mouse micronucleus test system. A known mutagen nickel (Nickel chloride-10 mg/kg, b.

Role of emotionality on inter and intrastrain variations in imipramine response. a comparative study in Balb/c and Swiss mice.

Association between emotionality and effect of imipramine on immobility time in forced swimming test was investigated in Swiss and Balb/c mice. Mice of both the strains were segregated into normal emotional (mean +/- 1SD), low emotional (> mean + 1SD) and high emotional (< mean - 1SD) based on their performance with respect to each indices of emotionality in novel arena and elevated plus maze. Baseline immobility and effect of imipramine (20 mg/kg, po) on immobility time was evaluated in these emotionally different groups of mice using forced swimming test model.

Interaction effect between phosphorus and zinc on their availability in soil in relation to their contents in stevia (Stevia rebaudiana).

A greenhouse experiment was conducted at the Indian Institute of Horticultural Research (IIHR), Bangalore to study the interaction effect between phosphorus and zinc on their availability in soil in relation to their contents in stevia (Stevia rebaudiana). The results show that the amount of available P and Zn content in soil has been found to increase initially and, thereafter, the amount of the same decreased with the progress of plant growth up to 60 days irrespective of treatments. The amount of P and Zn in soils showed an increase with their separate applications either as soil or foliar spray while that of the same value significantly decreased both in soils and plants due to their combined applications, suggesting a mutual antagonistic effect between Zn and P affecting each other's availability in soil and content in the stevia plant.

Interaction between phosphorus and zinc on the biomass yield and yield attributes of the medicinal plant stevia (Stevia rebaudiana).

A greenhouse experiment was conducted at the Indian Institute of Horticultural Research (IIHR), Bangalore to study the interaction effect between phosphorus (P) and zinc (Zn) on the yield and yield attributes of the medicinal plant stevia. The results show that the yield and yield attributes have been found to be significantly affected by different treatments. The total yield in terms of biomass production has been increased significantly with the application of Zn and P in different combinations and methods, being highest (23.

Biodegradable microspheres of ketorolac tromethamine for parenteral administration.

Ketorolac tromethamine loaded microspheres were prepared using two different polyesters, namely poly (lactic acid) and poly (glycolic acid) by solvent evaporation technique. The morphology of microspheres was analysed by scanning electron microscopy. In vitro release profiles of these microspheres were studied in phosphate buffered saline pH 7.

Evaluation of carboxymethyl guar films for the formulation of transdermal therapeutic systems.

Carboxymethyl guar (CMGS), an anionic semisynthetic guar gum derivative was evaluated for its suitability of use in transdermal drug-delivery systems. Terbutaline sulfate (TS) was used as a model drug. The diffusion of terbutaline sulfate from CMGS solution was relatively slower at pH 5 than at pH 10.

Design and evaluation of matrix diffusion controlled transdermal patches of verapamil hydrochloride.

Transdermal patches of verapamil hydrochloride were prepared using four different polymers (individual and combination): Eudragit RL100 (ERL100), Eudragit RS100 (ERS100), hydroxypropyl methylcellulose 15 cps (HPMC), and ethyl cellulose (EC), of varying degrees of hydrophilicity and hydrophobicity. The effect of the polymers on the technological properties, i.e.

Pharmacokinetic profile of a new matrix-type transdermal delivery system: diclofenac diethyl ammonium patch.

A transdermal delivery system containing the anti-inflammatory analgesic diclofenac diethyl ammonium in an ethyl hexyl acrylate and vinyl acetate pressure-sensitive adhesive system was developed for percutaneous absorption. These patches were subjected to in vitro permeation and permeation enhancement studies through rat skin using a specially designed diffusion cell. Further, the work deals with percutaneous absorption studies carried out on both animals and human volunteers.

Ocular delivery systems of pefloxacin mesylate.

Ocular films of pefloxacin mesylate were prepared with the objectives of reducing the frequency of administration, to improve patient compliance, obtaining controlled release and greater therapeutic efficacy in the treatment of eye infections such as conjunctivitis, keratitis, kerato conjunctivitis, corneal ulcers etc. Polymers such as HPC, HPMC, PVP and PVA were used in different ratios to prepare the ocular films. They were evaluated for drug content which varied from 96-104%.

Comparative evaluation of mechanism of neuromuscular (n-m) blockade due to enhydrotoxin-A (EsNTx-a) and D-tubocurarine (d-TC).

Effects of major E. schistosa neurotoxin (NTx) EsNTx-a are compared with plant alkaloid d-TC for its onset (LP) and duration of action as the time required for 50% n-m blockade (DT1/2) in normal Ca2+ and modified Ca2+ Krebs Heinsleit (K-H) at two different (low and high) concentrations (conc.).